Publications by authors named "Chi-On Chan"

36 Publications

Water extract of Er-xian decoction selectively exerts estrogenic activities and interacts with SERMs in estrogen-sensitive tissues.

J Ethnopharmacol 2021 Jul 3;275:114096. Epub 2021 Apr 3.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong SAR, PR China; State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen, 518057, PR China. Electronic address:

Ethnopharmacological Relevance: The increasing use of "kidney"-nourishing Traditional Chinese Medicine (TCM) like Er-xian decoction (EXD) for management of menopausal symptoms and osteoporosis has aroused concerns about their safety, and whether they interact with prescription drugs as both of them act via estrogen receptors (ERs) and regulate serum estradiol.

Aim Of The Study: The present study aimed to evaluate whether EXD selectively exerted estrogenic activities and interacted with Selective Estrogen Receptor Modulators (SERMs).

Materials And Methods: In vivo, mature ovariectomized (OVX) rats were administrated with EXD or combined treatment of EXD and SERMs for 12 weeks. The tissue-selective effect of EXD and its interaction of SERMs were studied in four estrogen sensitive tissues, bone, brain, breast and uterus. In vitro, the interaction of extracts of EXD-treated serum and SERMs in four ER-positive cell lines.

Results: In OVX rats, EXD selectively alleviated estrogen deficiency-induced changes in the bone and brain without inducing any estrogenic effects in the breast or uterus. Two-way ANOVA indicated the presence of interactions between EXD and SERMs in OVX rats but EXD did not significantly alter the tissue responses to SERMs in the bone, breast or brain. Indeed, the combined use of EXD and SERMs appeared to suppress the estrogenic effect of raloxifene and tamoxifen in the uterus. Extract of EXD-treated serum directly stimulated cell proliferation or differentiation in human osteosarcoma MG-63, neuroblastoma SHSY5Y, breast cancer MCF-7, and endometrial Ishikawa cells. Two-way ANOVA revealed that EXD-treated serum interacted with SERMs at various concentrations and altered the effects of tamoxifen in MG-63 and MCF-7 cells.

Conclusions: EXD exerted estrogenic effects in a tissue-selective manner and interacted with SERMs. Combined treatment of EXD and SERMs did not hamper the beneficial effects of SERMs on the bone or brain but appeared to moderate the estrogenic effect of SERMs in the uterus.
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http://dx.doi.org/10.1016/j.jep.2021.114096DOI Listing
July 2021

The lignan-rich fraction from Sambucus Williamsii Hance ameliorates dyslipidemia and insulin resistance and modulates gut microbiota composition in ovariectomized rats.

Biomed Pharmacother 2021 May 22;137:111372. Epub 2021 Feb 22.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen 518057, PR China; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China. Electronic address:

Menopausal women are susceptible to have high risk of cardiovascular diseases, type II diabetes and osteoporosis due to the metabolic disorder caused by estrogen deficiency. Accumulating evidence supports that gut microbiota is a key regulator of metabolic diseases. Our previous metabolomics study interestingly demonstrated that the anti-osteoporotic effects of lignan-rich fraction (SWCA) from Sambucus wialliamsii Hance were related to the restoration of a series of lipid and glucose metabolites. This study aims to investigate how SWCA modulates lipid and glucose metabolism and the underlying mechanism. Our results show that oral administration of SWCA (140 mg/kg and 280 mg/kg) for 10 weeks alleviated dyslipidemia, improved liver functions, prevented glucose tolerance and insulin actions, attenuated system inflammation and improved intestinal barrier in OVX rats. It also induced a high abundance of Actinobacteria, and restored microbial composition. We are the first to report the protective effects of the lignan-rich fraction from S. williamsii on dyslipidemia and insulin resistance. Our findings provide strong evidence for the application of this lignan-rich fraction to treat menopausal lipid disorder and insulin resistance-related diseases.
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http://dx.doi.org/10.1016/j.biopha.2021.111372DOI Listing
May 2021

Selective Estrogen Receptor Modulator-Like Activities of Herba epimedii Extract and its Interactions With Tamoxifen and Raloxifene in Bone Cells and Tissues.

Front Pharmacol 2020 15;11:571598. Epub 2021 Jan 15.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China.

(HEP), a kidney-tonifying herb, has been commonly used alone or in formula for strengthening kidney function and treating bone disorders. Its bone protective activity has been demonstrated to be via estrogen receptor (ERs). HEP activates the phosphorylation of ERα in an estrogen response element- (ERE-) dependent manner. We examined the bone protective effects of HEP and its potential interactions with Selective Estrogen Receptor Modulators (SERMs, such as tamoxifen and raloxifene) as they act via the same ERs. Six-month-old mature Sprague Dawley sham-operated (Sham) or ovariectomized (OVX) rats were treated with either vehicle, 17ß-estradiol (1.0 mg/kg.day), tamoxifen (Tamo, 1.0 mg/kg.day), raloxifene (Ralo, 3.0 mg/kg.day), HEP (0.16 g/kg.day), or its combinations with respective SERMs (HEP + Tamo; HEP + Ralo) for 12 weeks. HEP and SERMs as well as their combinations significantly restored changes in bone mineral density (BMD), trabecular bone properties, and bone turnover biomarkers induced by ovarian sex hormone deficiency in ovariectomized rats. Besides the increase in serum estradiol, inhibition on follicle stimulating hormone (FSH) might also be involved in the osteoprotective activities of HEP and SERMs. HEP interacted with SERMs to protect bones from ovarian sex hormone deficiency without altering SERMs' bone protective activities. HEP neither induced changes in uterus weight nor altered the uterotrophic activity of SERMs in OVX rats. In human osteosarcoma MG-63 cells, HEP-treated serum (HEP-Ts) significantly promoted alkaline phosphatase (ALP) activity like the crude HEP extract did but did not stimulate ERE activity. Our study also reported that biologically activated HEP interacted with SERMs to promote ALP activity without altering the action of SERMs at most of the concentrations tested in MG-63 cells. HEP exerted bone protective activity and the use of HEP did not alter the bone protective activities of SERMs when they were used simultaneously in an estrogen-deficient rat model.
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http://dx.doi.org/10.3389/fphar.2020.571598DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7843570PMC
January 2021

Mass spectrometry-based untargeted metabolomics approach for differentiation of beef of different geographic origins.

Food Chem 2021 Feb 25;338:127847. Epub 2020 Aug 25.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), Shenzhen Research Institute of The Hong Kong Polytechnic University, Shenzhen 518057, China; Food Safety and Technology Research Centre and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China. Electronic address:

Beef is a common staple food in many countries, and there is a growing concern over misinformation of beef products, such as false claims of origin, species and production methods. In this study, we used a mass spectrometry-based metabolomics approach to study the metabolite profiles of beef samples purchased from local retailers in Hong Kong. Using multivariate analysis, beef samples from different a) geographical origins, namely the United States (US), Japan and Australia, and b) feeding regimes could be differentiated. We identified twenty-four metabolites to distinguish beef samples from different countries, ten metabolites to identify Angus beef samples from others and seven metabolites to discriminate Australian beef produced by the organic farming from that produced using other farming modes. Based on results of this study, it is concluded that metabolomics provides an efficient strategy for tracing and authenticating beef products to ensure their quality and to protect consumer rights.
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http://dx.doi.org/10.1016/j.foodchem.2020.127847DOI Listing
February 2021

Schwann cell-specific Pten inactivation reveals essential role of the sympathetic nervous system activity in adipose tissue development.

Biochem Biophys Res Commun 2020 10 8;531(2):118-124. Epub 2020 Aug 8.

State Key Laboratory of Chemical Biology and Drug Discovery, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong. Electronic address:

There is increasing evidence that the sympathetic nervous system (SNS) plays an important role in adipose tissue development. However, the underlying molecular mechanism(s) associated with this remains unclear. SNS innervation of white adipose tissue (WAT) is believed to be necessary and sufficient to elicit WAT lipolysis. In this current study, mice with Schwann cell (SC)-specific inactivation of phosphatase and tensin homolog (Pten) displayed enlarged inguinal white adipose tissue (iWAT). This serendipitous observation implicates the role of SCs in mediating SNS activity associated with mouse adipose tissue development. Mice with SC-specific Pten inactivation displayed enlarged iWAT. Interestingly, the SNS activity in iWAT of SC-specific Pten-deficient mice was reduced as demonstrated by decreased tyrosine hydroxylase (TH) expression level and neurotransmitters, such as norepinephrine (NE) and histamine (H). The lipolysis related protein, phosphorylated hormone sensitive lipase (pHSL), was also decreased. As expected, AKT-associated signaling pathway was hyperactivated and hypothesized to induce enlarged iWAT in SC-specific Pten-deficient mice. Moreover, preliminary experiments using AKT inhibitor AZD5363 treatment ameliorated the enlarged iWAT condition in SC-specific Pten-deficient mice. Taken together, SCs play an essential role in the regulation of SNS activity in iWAT development via the AKT signaling pathway. This novel role of SCs in SNS function allows for better understanding into the genetic mechanisms of peripheral neuropathy associated obesity.
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http://dx.doi.org/10.1016/j.bbrc.2020.07.050DOI Listing
October 2020

Qualitative and quantitative analysis of sesquiterpene lactones in Centipeda minima by UPLC-Orbitrap-MS & UPLC-QQQ-MS.

J Pharm Biomed Anal 2019 Sep 30;174:360-366. Epub 2019 May 30.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen, 518057, China; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China; Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100193, China. Electronic address:

An ultra-high performance liquid chromatography coupled with high-resolution Orbitrap mass spectrometry (UPLC-Orbitrap-MS) method has been used to identify sesquiterpene lactones in the methanolic extract of Centipeda minima. Fifteen sesquiterpene lactones were tentatively identified based on retention time and accurate mass of external standards or exact accurate mass searching (within 2 ppm) by comparison of some previous isolated sesquiterpene lactones. Meanwhile, a rapid, sensitive, precise, and reliable ultra-high performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-QQQ-MS) method has been developed to evaluate the quality of Centipeda minima through a simultaneous determination of five sesquiterpene lactones, namely brevilin A, arnicolide C, arnicolide D, microhelenin C, minimolide F. Chromatographic separation was achieved on a Waters Acquilty UPLC BEH C18 column (2.1 mm × 50 mm, 1.7 μm) with a mobile phase consisting of a) 0.1% formic acid and b) a mixture of acetonitrile and methanol 50:50 v/v under an isocratic elution (42:58) manner. Positive electrospray ionization mode with multiple reaction monitoring was applied for the detection of the five sesquiterpene lactones. Method validation for linearity, accuracy and precision was also carried out. Finally, the method was successfully used for the analysis of 10 batches of Centipeda minima samples collected in China. Brevilin A and arnicolide D were the dominant sesquiterpene lactones in Centipeda minima and could be proposed as suitable markers for the quality control of Centipeda minima.
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http://dx.doi.org/10.1016/j.jpba.2019.05.067DOI Listing
September 2019

Dihydrochalcone-derived polyphenols from tea crab apple (Malus hupehensis) and their inhibitory effects on α-glucosidase in vitro.

Food Funct 2019 May;10(5):2881-2887

Institute of Medicinal Plant Development, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100191, People's Republic of China.

Three dihydrochalcone-derived polyphenols, huperolides A-C (1-3), along with thirteen known compounds (4-16) were isolated from the leaves of Malus hupehensis, the well-known tea crab apple in China. Their chemical structures were elucidated by extensive spectroscopic analysis including NMR (HSQC, HMBC, 1H-1H COSY and ROESY), HRMS and CD spectra. Huperolide A is a polyphenol with a new type of carbon skeleton, while huperolides B and C are a couple of atropisomers, which were isolated from natural sources for the first time. The antihyperglycemic effects of the isolated compounds were evaluated based on assaying their inhibitory activities against α-glucosidase. As a result, phlorizin (4), 3-hydroxyphloridzin (5), 3-O-coumaroylquinic acid (12) and β-hydroxypropiovanillone (15) showed significant concentration-dependent inhibitory effects on α-glucosidase. Therefore, those compounds might be responsible for the antihyperglycemic effect of this herb, and are the most promising compounds to lead discovery of drugs against diabetes.
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http://dx.doi.org/10.1039/c9fo00229dDOI Listing
May 2019

HBx-K130M/V131I Promotes Liver Cancer in Transgenic Mice via AKT/FOXO1 Signaling Pathway and Arachidonic Acid Metabolism.

Mol Cancer Res 2019 07 11;17(7):1582-1593. Epub 2019 Apr 11.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), The Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen, China.

Chronic hepatitis B viral (HBV) infection remains a high underlying cause for hepatocellular carcinoma (HCC) worldwide, while the genetic mechanisms behind this remain unclear. This study elucidated the mechanisms contributing to tumor development induced by the HBV X (HBx) gene of predominantly Asian genotype B HBV and its common HBx variants. To compare the potential tumorigenic effects of K130M/V131I (Mut) and wild-type (WT) HBx on HCC, the () transposon system was used to deliver HBx Mut and WT into the livers of fumarylacetoacetate hydrolase ()-deficient mice and in the context of () deficiency. From our results, HBx Mut had a stronger tumorigenic effect than its WT variant. Also, inflammation, necrosis, and fibrosis were evident in HBx experimental animals. Reduction of forkhead box O1 (FOXO1) with increased phosphorylation of upstream serine/threonine kinase (AKT) was detected under HBx Mut overexpression. Thus, it is proposed that HBx Mut enhances disease progression by reducing FOXO1 via phosphorylation of AKT. At the metabolomic level, HBx altered the expression of genes that participated in arachidonic acid (AA) metabolism, as a result of inflammation via accumulation of proinflammatory factors such as prostaglandins and leukotriene in liver. Taken together, the increased rate of HCC observed in chronic hepatitis B patients with K130M/V131I-mutated X protein, may be due to changes in AA metabolism and AKT/FOXO1 signaling. IMPLICATIONS: Our findings suggested that HBx-K130M/V131I-mutant variant promoted HCC progression by activating AKT/FOXO1 pathway and inducing stronger inflammation in liver via AA metabolism.
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http://dx.doi.org/10.1158/1541-7786.MCR-18-1127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6610579PMC
July 2019

Altered metabolites in guinea pigs with allergic asthma after acupoint sticking therapy: New insights from a metabolomics approach.

Phytomedicine 2019 Feb 5;54:182-194. Epub 2018 Sep 5.

School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China. Electronic address:

Background: Clinical evidence gathered in Chinese communities suggested that acupoint sticking therapy could be an alternative treatment for asthma-related diseases. However, its underlying mechanism is still poorly understood.

Aim/hypothesis: In this study, we aimed to investigate the mechanism of the anti-inflammatory effect of acupoint sticking application with 'Treatment of Winter Disease in Summer' (TWDS) prescription by using metabolomics.

Methods: Allergic asthma in guinea pig was sensitized and challenged by ovalbumin (OVA). Histopathological evaluation of the lung tissue was performed by hematoxylin and eosin (H&E) staining and Masson's trichrome staining. The levels of Th2 cytokine and IgE level in serum were measured using enzyme-linked immunoassay (ELISA). The mRNA expression levels of IL-4, IL-5, IL-13 and orosomucoid-like 3 (ORMDL3) were measured using quantitative reverse transcription polymerase chain reaction (RT-qPCR). Proteins of NF-κB signaling pathway were measured using western blot. The serum metabolomics profiles were obtained by using ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC-ESI-QTOF-MS).

Results: The overall results confirmed that AST with TWDS prescription had a significant protective effect against OVA-induced allergic asthma in guinea pig. This treatment not only attenuated airway inflammation and collagen deposition in the airway, but also decreased the levels of IL-4, IL-5, IL-13 and IgE in serum. In addition, metabolomics results indicated that metabolisms of phospholipid, sphingolipid, purine, amino acid and level of epinephrine were restored back to the normal control level. Moreover, results of the gene expression of ORMDL3 in lung tissues indicated that AST using TWDS could alter the sphingolipid metabolism. Further western blotting analysis also showed that its anti-inflammatory mechanism was by decreasing the phosphorylation of p65 and IκB.

Conclusion: The study demonstrated that metabolomics provides a better understanding of the actions of TWDS acupoint sticking therapy on OVA-induced allergic asthma.
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http://dx.doi.org/10.1016/j.phymed.2018.09.021DOI Listing
February 2019

A Metabolomics Study on the Bone Protective Effects of a Lignan-Rich Fraction From Sambucus Williamsii Ramulus in Aged Rats.

Front Pharmacol 2018 21;9:932. Epub 2018 Aug 21.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen, China.

The lignan-rich fraction (SWR) of Sambucus Williamsii Ramulus, a folk herbal medicine in China for treatment of bone diseases, has previously reported to exert protective effects on bone without exerting uterotrophic effects in ovariectomized (OVX) mice. The aim of the present study was to identify the potential metabolites and the associated metabolic pathways that contribute to the beneficial effects of SWR on bone . Aged female Sprague Dawley rats (9 months old) were either sham-operated or ovariectomized for 12 weeks, before receiving treatment for another 12 weeks with the following treatment groups ( = 12 each): vehicle (Sham), vehicle (OVX), Premarin (130 μg/kg) or low (57 mg/kg), medium (114 mg/kg), and high (228 mg/kg) doses of SWR. The results showed that SWRH significantly suppressed bone loss, improved bone micro-architecture and increased bone strength on tibia without stimulating uterus weight gain in OVX rats. Premarin exerted similar bone protective effects as SWRH but elicited uterotrophic effects in OVX rats. The metabolic profiles of serum samples were analyzed by using ultra-performance liquid chromatography quadrupole time-of flight mass spectrometry and gas chromatography time-of flight mass spectrometry, and the metabolites that were significantly altered were identified by multivariate statistical analysis. Our study indicated that SWRH effectively restored the changes of 26 metabolites induced by estrogen-deficiency in OVX rats, which related to lipids, amino acids, tryptophan metabolisms, and anti-oxidative system. A subsequent validation showed that the serum level of superoxide dismutase and catalase were indeed up-regulated, while the serotonin level in a tryptophan hydroxylase 1 (TPH1) high expressing cells (rats RBL-2H3 cells) was down regulated after treatment with SWR. The results also suggested that the gut-microbiota may play an important role on the bone protective effects of SWR. The current study provides insight for understanding the unique mechanism of actions of SWR that might be involved in achieving bone protective effects .
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http://dx.doi.org/10.3389/fphar.2018.00932DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6110923PMC
August 2018

Clinical and histopathological features of chronic hepatitis B virus infected patients with high HBV-DNA viral load and normal alanine aminotransferase level: A multicentre-based study in China.

PLoS One 2018 4;13(9):e0203220. Epub 2018 Sep 4.

Department of Hepatology, Shenzhen Traditional Chinese Medicine Hospital, Shenzhen, China.

Background: The aim of this study is to reveal the clinical and histopathological features of HBsAg-positive and HBeAg-positive chronic hepatitis B infected patients with high level of HBV DNA, from 17 hospitals and medical centres in China, with alanine aminotransferase levels within the lower region of normal range versus those with levels within the upper region of normal range and to investigate the clinical risk factors for the requirement of treatment through the examination of liver biopsy.

Methods: Liver biopsy was performed on high level of HBV DNA of 455 patients with HBsAg-positive and HBeAg-positive chronic hepatitis B infection and persistently normal alanine aminotransferase level. Liver necroinflammation and fibrosis were graded per the Knodell histological activity index and Ishak's fibrosis score, respectively. Univariate analysis of the clinical parameters versus necroinflammation and fibrosis was carried out.

Results: Of the subjects in this multicentre-based study, 5.49% and 10.11% had significant necroinflammation with Knodell histological activity index ≥ 9 and hepatic fibrosis stages with Ishak scores ≥ 3, respectively. The subjects were stratified into three age groups (30-39, 40-49 and ≥ 50 years), and our data clearly suggested that age, particularly in the age group over 50, was an independent predictor of liver necroinflammation and fibrosis. Lower HBV-DNA viral levels were found in patients with Knodell histological activity index ≥ 9 or advanced fibrosis (Ishak scores ≥ 3).

Conclusion: Our results showed that histological changes in liver tissues were observed in a significant proportion of patients with persistently normal alanine aminotransferase level. According to the data evaluation results, liver biopsy is advisable for HBeAg-positive chronic hepatitis B infected patients aged older than 40 and high HBV-DNA viral load in China.
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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0203220PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6122822PMC
February 2019

Rapid differentiation of Ganoderma species by direct ionization mass spectrometry.

Anal Chim Acta 2018 Jan 9;999:99-106. Epub 2017 Nov 9.

Food Safety and Technology Research Centre, State Key Laboratory of Chirosciences and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong Special Administrative Region, China; State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation) and Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen Research Institute of The Hong Kong Polytechnic University, Shenzhen, China; Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules (Yanbian University), Ministry of Education, Yanji, Jilin 133002, China. Electronic address:

In this study, direct ionization mass spectrometry (DI-MS) has been developed for rapid differentiation of Ganoderma (known as Lingzhi in Chinese), a very popular and valuable herbal medicine. Characteristic mass spectra can be generated by DI-MS directly from the raw herbal medicines with the application of a high voltage and solvents. Rapid differentiation of the Ganoderma species that are officially stated in the Chinese pharmacopoeia from easily confused Ganoderma species could be achieved based on this method, as the acquired DI-MS spectra showed that ganoderic acids, the major active components of Ganoderma, could be found only in the official Ganoderma species but not in the confused Ganoderma species. In addition, classification of wild and cultivated Ganoderma and potential differentiation of Ganoderma from different geographical locations could be accomplished based on principal component analysis (PCA) or hierarchical clustering analysis (HCA). The method is rapid, simple and reproducible, and can be further extended to analysis of other herbal medicines.
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http://dx.doi.org/10.1016/j.aca.2017.11.006DOI Listing
January 2018

Comparative Evaluation of Chemical Profiles of Pyrrosiae Folium Originating from Three Pyrrosia Species by HPLC-DAD Combined with Multivariate Statistical Analysis.

Molecules 2017 Dec 1;22(12). Epub 2017 Dec 1.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China.

Pyrrosiae Folium (PF) is a commonly used Chinese herb medicine originating from three species for the treatment of urinary infection and urolithiasis. According to Chinese medicine practice, different specie origins led to some variations in the therapeutic effects of PF. To ensure the safety and efficacy of PF in clinical practice, it is necessary to establish a reliable and integrative method to distinguish PF occurring from the three species. In the present paper, a HPLC-DAD method was developed and applied to simultaneously analyze five major compounds in PF. Afterwards, multivariate statistical analyses including principal component analysis (PCA) and partial least squares discriminant analysis (PLS-DA) were applied for specie discrimination and integrative quality evaluation based on quantitative data. The chemical determination and pattern recognition results of 35 batches of PF samples indicated that PF samples from three species showed different chemical profiles and could be discriminated clearly. In conclusion, the present method is rapid and reliable for the quality assessment and species discrimination of PF.
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http://dx.doi.org/10.3390/molecules22122122DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6150016PMC
December 2017

Enhanced Intestinal Permeability of Bufalin by a Novel Bufalin-Peptide-Dendrimer Inclusion through Caco-2 Cell Monolayer.

Molecules 2017 Nov 29;22(12). Epub 2017 Nov 29.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), Hong Kong Polytechnic University Shenzhen Research Institute, Shenzhen 518057, China.

Bufalin (BFL) has excellent physiological activities such as defending tumors, improving cardiac function, and so on. However, due to its poor water-solubility and bioavailability, the clinical application of BFL remains limited. In order to improve bioavailability of BFL, in our previous research, a novel peptide-dendrimer (PD) was synthesized and applied to encapsulate BFL. In the present study, we investigate the absorption property and mechanism of BFL in free form and BFL-peptide-dendrimer inclusion (BPDI) delivery system by using the Caco-2 cell monolayer model in vitro. The apparent permeability coefficient () values of BFL in free or BPDI form were over 1.0 × 10 cm/s. Meanwhile, their almost equal bi-directional transport and linear transport percentage with time and concentration course indicated that BFL in both forms was absorbed mainly through passive diffusion. The most important result is that the values of BFL increased about three-fold more BPDI than those of its free form, which indicated the intestinal permeability of BFL could be improved while BFL was encapsulated in BPDI form. Therefore, PD encapsulation may be a potential delivery system to increase the bioavailability of BFL.
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http://dx.doi.org/10.3390/molecules22122088DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6149814PMC
November 2017

Chemical Analysis of Astragali Complanati Semen and Its Hypocholesterolemic Effect Using Serum Metabolomics Based on Gas Chromatography-Mass Spectrometry.

Antioxidants (Basel) 2017 Jul 21;6(3). Epub 2017 Jul 21.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong, China.

The hypocholesterolemic protective effect of the dried seed of (ACS) was investigated in rats fed with normal diet, high cholesterol diet (HCD), and HCD plus 70% ethanol extract of ACS (600 mg/kg/day) by oral gavage for four weeks. ACS extract was tested to be rich in antioxidants, which may be contributed to its high content of phenolic compounds. Consumption of ACS remarkably suppressed the elevated total cholesterol ( < 0.01) and LDL-C ( < 0.001) induced by HCD. Chemical constituents of ACS extract were analyzed by ultra-performance liquid chromatography coupled with electrospray ionization orbitrap mass spectrometry and the results showed that the ACS extract mainly consisted of phenolic compounds including flavonoids and flavonoid glycosides. In addition, based on the serum fatty acid profiles, elucidated using gas chromatography-mass spectrometry, free and esterified fatty acids including docosapentaenoic acid, adrenic acid, dihomo-γ-linolenic acid and arachidonic acid were regulated in ACS treatment group. Western blot results further indicated the protein expression of peroxisome proliferator-activated receptor alpha (PPARα) ( < 0.05) in liver was upregulated in ACS treatment group. To conclude, our results clearly demonstrated that ACS provides beneficial effect on lowering HCD associated detrimental change.
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http://dx.doi.org/10.3390/antiox6030057DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5618085PMC
July 2017

Shugan Xiaozhi Decoction Attenuates Nonalcoholic Steatohepatitis by Enhancing PPAR and L-FABP Expressions in High-Fat-Fed Rats.

Evid Based Complement Alternat Med 2016 28;2016:7870189. Epub 2016 Nov 28.

Department of Hepatology, Shenzhen Traditional Chinese Medicine Hospital, Shenzhen 518033, Hong Kong.

This study aimed to investigate the effects of Shugan Xiaozhi decoction (SX) on nonalcoholic steatohepatitis (NASH) induced by high-fat diet in rats. The rats were randomly divided into 6 groups, namely, control, model, fenofibrate, and three different dosage of SX (10, 20, and 40 g/kg/day, p.o.). After establishing the NASH model, at 8 weeks of the experiment, treatments were administrated intragastrically to the fenofibrate and SX groups. All rats were killed after 4 weeks of treatment. Compared with the model group, alanine aminotransferase (ALT), aspartate aminotransferase (AST), free fatty acid (FFA), total cholesterol (TC), triacylglycerol (TG), and low-density lipoprotein cholesterol (LDL) serum in the serum were significantly reduced in all SX treatment groups in a dose-dependent manner. Evidence showed that SX could protect the liver by upregulating the gene and protein expressions of peroxisome proliferator-activated receptor alpha (PPAR) and liver fatty acid binding protein (L-FABP) in a dose-dependent manner. Chemical constituents of SX were further analyzed by ultraperformance liquid chromatography coupled with electrospray ionization mass spectrometry (UPLC-ESI-MS) and 30 chemicals in the ethanolic extract were tentatively identified. To conclude, our results clearly indicated that SX could protect liver functions and relieve hepatic steatosis and inflammation.
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http://dx.doi.org/10.1155/2016/7870189DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5149676PMC
November 2016

Rapid authentication of Gastrodiae rhizoma by direct ionization mass spectrometry.

Anal Chim Acta 2016 Sep 28;938:90-7. Epub 2016 Jul 28.

Food Safety and Technology Research Centre, State Key Laboratory of Chirosciences and Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China; State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation) and Shenzhen Key Laboratory of Food Biological Safety Control, Shenzhen Research Institute of The Hong Kong Polytechnic University, Shenzhen, China; Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules (Yanbian University), Ministry of Education, Yanji, 133002, China. Electronic address:

In this study, direct ionization mass spectrometry (DI-MS) for rapid authentication of Gastrodiae rhizoma (known as Tianma in Chinese), a popular herbal medicine, has been developed. This method is rapid, simple and allows direct generation of characteristic mass spectra from the raw herbal medicines with the application of some solvents and a high voltage. The acquired DI-MS spectra showed that gastrodin, parishin B/parishin C and parishin, the major active components of Gastrodiae rhizoma, could be found only in genuine Gastrodiae rhizoma samples, but not in counterfeit samples, thus allowing rapid authentication of Gastrodiae rhizoma. Moreover, wild and cultivated Gastrodiae rhizoma could be classified and Gastrodiae rhizoma from different geographical locations could be differentiated based on their different intensity ratios of characteristic ions or principal component analysis (PCA). This method is simple, rapid, reproducible, and can be extended to analyze other herbal medicines.
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http://dx.doi.org/10.1016/j.aca.2016.07.028DOI Listing
September 2016

Qualitative and quantitative analysis of chemical constituents of Centipeda minima by HPLC-QTOF-MS & HPLC-DAD.

J Pharm Biomed Anal 2016 Jun 20;125:400-7. Epub 2016 Apr 20.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Shenzhen, China; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, Hong Kong, China. Electronic address:

A high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) method in both positive and negative ion modes was established to investigate the major constituents in the ethanolic extract of Centipeda minima (EBSC). Twelve common components including flavones and their glycosides, phenolic and polyphenolic acids, and sesquiterpene lactone were identified in ten batches of samples based on comparison with the retention time and accurate mass of external standards (mass accuracy within 3ppm) or the fragmentation patterns of tandem MS. Meanwhile, a simple, accurate and reliable HPLC-DAD method was also developed to determine the content of 10 chemical markers simultaneously. Results obtained from method validations including linearity, accuracy and precision showed that this new method is reliable and robust. Isochlorogenic acid A and brevilin A were found to be the most abundant in the ethanol extract of EBSC and could be served as markers for quality control of EBSC.
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http://dx.doi.org/10.1016/j.jpba.2016.04.029DOI Listing
June 2016

Discrimination between Leave of Apocynum venetum and Its Adulterant, A. pictum Based on Antioxidant Assay and Chemical Profiles Combined with Multivariate Statistical Analysis.

Antioxidants (Basel) 2015 May 8;4(2):359-72. Epub 2015 May 8.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Shenzhen 518057, China.

An integrated approach including chemical and biological assessments was developed to investigate the differences between Apocynum venetum L. (AV) and its adulterant, Apocynum pictum Schrenk (AP). Ten flavonoids were tentatively identified by ultra-visible and mass spectra data. The chemical component, hyperoside, was identified as a critical parameter for discrimination of two species from the results of principal component analysis (PCA) and quantitative analysis. The anti-oxidative power of the herbal extracts were determined using 2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazyl (DPPH) assay and H₂O₂-induced cell damage on LO2 cells. The results of the biological assays suggested that the chemical differences between AV and AP do lead to difference in activity and AV is demonstrated to have higher anti-oxidant activity.
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http://dx.doi.org/10.3390/antiox4020359DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4665472PMC
May 2015

Novel cycloartane triterpenoid from Cimicifuga foetida (Sheng ma) induces mitochondrial apoptosis via inhibiting Raf/MEK/ERK pathway and Akt phosphorylation in human breast carcinoma MCF-7 cells.

Chin Med 2016 11;11. Epub 2016 Jan 11.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China ; State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Hong Kong Polytechnic University, Hong Kong, China.

Background: Cycloartane triterpenoids exhibited anticancer effects. This study aims to identify any potential novel anticancer cycloartane triterpenoids from Cimicifuga foetida L. rhizome (Sheng ma) and the mode of actions.

Methods: Cycloartane triterpenoids were isolated from the C. foetida rhizome by a series of column chromatography and identified by IR, MS and NMR. Their anticancer effects on several human cancer cell lines, MCF-7, HepG2, HepG2/ADM, HeLa, and PC3, and normal human mammary epithelial cells MCF10A were investigated by colony formation and MTT assays. Morphological analysis of apoptosis induction was performed by acridine orange/ethidium bromide dual-staining and Hoechst 33258 nuclear staining. The cell-cycle profile and annexin V staining were evaluated by flow cytometry. Apoptosis were investigated by measuring changes in mitochondrial membrane potential and analyzing expression of cell cycle- and apoptosis-related proteins in MCF-7 cells by Western blotting.

Results: A novel cycloartane triterpenoid, 25-O-acetyl-7,8-didehydrocimigenol-3-O-β-d-(2-acetyl)xylopyranoside (ADHC-AXpn), together with the known 7,8-didehydrocimigenol-3-O-β-d-xylopyranoside (DHC-Xpn) were isolated. MCF-7 growth was significantly inhibited by ADHC-AXpn in a dose- and time-dependent manner (IC50: 27.81 µM at 48 h; P = 0.004 vs. control at 25 μM for 48 h treatment), and ADHC-AXpn was selectively cytotoxic for cancerous cells (MCF-7, HepG2/ADM, HepG2 and HELA cells) based on its higher IC50 values for normal cells MCF10A (IC50: 78.63 µM at 48 h) than for tumor cells. In MCF-7 cells, ADHC-AXpn induced G2/M cell cycle arrest by mediating cyclin-B1, and CDK1 and its phosphorylation; and induced apoptosis through the mitochondrial-mediated apoptotic pathway, with inhibition of Akt activation. As ADHC-AXpn suppressed phosphorylation of ERK1/2, Raf and Akt proteins in MCF-7 cells, its apoptotic effect might be associated with Raf/MEK/ERK signaling and Akt activation.

Conclusions: ADHC-AXpn significantly suppressed the growth of MCF-7 cells, induced mitochondrial apoptosis and cell-cycle arrest, and inhibited Raf/MEK/ERK signaling pathway and Akt phosphorylation.
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http://dx.doi.org/10.1186/s13020-015-0073-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4709995PMC
January 2016

Centipeda minima (Ebushicao) extract inhibits PI3K-Akt-mTOR signaling in nasopharyngeal carcinoma CNE-1 cells.

Chin Med 2015 18;10:26. Epub 2015 Sep 18.

Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100193 People's Republic of China ; State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Shenzhen, 518057 People's Republic of China.

Background: Centipeda minima (Ebushicao) has been used for the treatment of various diseases, such as nasal allergies, rhinitis and sinusitis, nasopharyngeal carcinoma, cough, and headache. This study aims to investigate the anticancer activities of Centipeda minima ethanol extracts (CME) against nasopharyngeal carcinoma cell CNE-1 and their underlying mechanism.

Methods: CNE-1 cells were treated with different concentrations (15-50 μg/mL) of CME for different time intervals (24, 48, and 72 h). Cytotoxicity of CME was determined by MTT assay. Cell morphological changes were observed by fluorescence microscopy after HO 33258 staining. Cell cycle status was evaluated by flow cytometry following propidium iodide staining. Apoptosis was detected by flow cytometry following annexin V-FITC/PI staining. The levels of apoptosis-associated and PI3K-Akt-mTOR signaling related proteins were measured by western blotting analysis.

Results: CME (15-50 μg/mL) significantly inhibited the proliferation of CNE-1 in a dose- and time-dependent manner (P = 0.026 for 15 μg/mL, P < 0.001 for 25, 30, 40, and 50 μg/mL, respectively); the IC50 values (μg/mL) were 41.57 ± 0.17, 30.34 ± 0.06 and 24.98 ± 0.08 for 24, 48 and 72 h treatments, respectively. Significant morphological changes of CNE-1 cells displaying apoptosis were observed after CME treatment. CME showed low cytotoxicity toward normal LO2 cells. CNE-1 cells were arrested in the G2/M phase while treated with 15, 25, 40 μg/mL of CME, respectively (P = 0.032, P = 0.0053, P < 0.001). CME (15, 25, 40 μg/mL) down-regulated Bcl-2 expression (P = 0.032, P = 0.0074, P < 0.001), and up-regulated Bax (P = 0.026, P = 0.0056, P < 0.001) with activation of caspase-3, caspase-8, caspase-9, and PARP observed in CNE-1 cells (P = 0.015, P = 0.0067, P < 0.001 for caspase 3; P = 0.210, 0.028, < 0.001 for caspase 8; P = 0.152, 0.082, 0.0080 for caspase 9; P = 0.265, 0.0072, < 0.001 for PARP). CME suppressed the activation of the PI3K-AKT-mTOR pathway (P = 0.03, 0.0007, 0.004, 0.006, 0.022 for p-PI3K, p-Akt-Ser(473), p-Akt-Thr(308), p-mTOR-Ser(2448), p-mTOR-Ser(2481), respectively after 40 μg/mL of CME treated for 24 h).

Conclusion: CME inhibited the proliferation of CNE-1 cells and activation of the PI3K-AKT-mTOR signaling pathway.
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http://dx.doi.org/10.1186/s13020-015-0058-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4575463PMC
September 2015

Identifying bioactive components in natural products through chromatographic fingerprint.

Anal Chim Acta 2015 Apr 26;870:45-55. Epub 2015 Feb 26.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hung Hom, Kowloon, SAR Hong Kong, PR China; State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Shenzhen, PR China.

Bioactive component identification is a crucial issue in search for new drug leads. We provide a new strategy to search for bioactive components based on Sure Independence Screening (SIS) and interval PLS (iPLS). The method, which is termed as SIS-iPLS, is not only able to find out the chief bioactive components, but also able to judge how many components should be there responsible for the total bioactivity. The method is totally "data-driven" with no need for prior knowledge about the unknown mixture analyzed, therefore especially suitable for effect-directed work like bioassay-guided fractionation. Two data sets, a synthetic mixture system of twelve components and a suite of Radix Puerariae Lobatae extracts samples, are used to test the identification ability of the SIS-iPLS method.
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http://dx.doi.org/10.1016/j.aca.2015.02.030DOI Listing
April 2015

Petroleum ether extractive of the hips of Rosa multiflora ameliorates collagen-induced arthritis in rats.

J Ethnopharmacol 2014 Nov 26;157:45-54. Epub 2014 Sep 26.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Shenzhen 518057, PR China; Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong China; Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China. Electronic address:

Ethnopharmacological Relevance: The hip of Rosa multiflora Thunb. (HRM) has been traditionally used as a dietary supplement and a herbal remedy for the treatment of various diseases, including inflammation, osteoarthritis, rheumatoid arthritis and chronic pain, in China. The current study was to evaluate the therapeutic efficacy of the petroleum ether extractive of HRM (PEE) on type II collagen-induced rheumatoid arthritis (CIA) in male Wistar rats. In addition, the anti-inflammatory mechanism(s) of PEE on type II CIA was explored.

Materials And Methods: Rheumatoid arthritis (RA) was induced by intradermal injection of bovine type II collagen on Day 1 and Day 8. Starting from Day 13, normal rats were treated with vehicle (serving as the control group); the CIA rats were treated with vehicle (CIA group), dexamethasone (0.25mg/kg bw per day, p.o.) (a positive control), lei-gong-teng (LGT: 10mg/kg bw per day, p.o.) (a clinically used Chinese patent medicine in RA therapy) or PEE (12, 36 or 120mg/kg bw per day, p.o.) for 28 days.

Results And Conclusions: PEE (120mg/kg bw per day) efficiently attenuated the severity of arthritis in the CIA rats by reducing the mean arthritis severity scores and the fore/hind paw swelling as well as reduced histological changes by decreasing the cartilage surface erosion and cartilage proteoglan depletion. PEE׳s therapeutic effect in RA may involve the inhibition of pro-inflammatory cytokines, such as TNF-α, IL-1β and IL-6, in serum and/or the elevation of the activities of hepatic anti-oxidative enzymes including SOD, CAT and GSH-Px. However, the detailed anti-inflammatory mechanism, the main effective components and the interaction between different ingredients in PEE are still not clear and require more studies.
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http://dx.doi.org/10.1016/j.jep.2014.09.026DOI Listing
November 2014

A review on the traditional Chinese medicinal herbs and formulae with hypolipidemic effect.

Biomed Res Int 2014 7;2014:925302. Epub 2014 Jul 7.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong ; State Key Laboratory of Chinese Medicine and Molecular Pharmacology (Incubation), Shenzhen 518057, China ; Food Safety and Technology Research Centre, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong.

Hyperlipidemia, characterized by the abnormal blood lipid profiles, is one of the dominant factors of many chronic diseases such as diabetes, obesity, and cardiovascular diseases (CVD). For the low cost, effectiveness, and fewer side effects, the popularity of using traditional Chinese medicine (TCM) to handle hyperlipidemia is increasing and its role in health care has been recognized by the public at large. Despite the importance of TCM herbs and formulations, there is no comprehensive review summarizing their scientific findings on handling hyperlipidemia. This review summarizes the recent experimental and clinical results of nine representative single Chinese herbs and seven classic TCM formulae that could improve lipid profiles so as to help understand and compare their underlying mechanisms. Most of single herbs and formulae demonstrated the improvement of hyperlipidemic conditions with multiple and diverse mechanisms of actions similar to conventional Western drugs in spite of their mild side effects. Due to increasing popularity of TCM, more extensive, well-designed preclinical and clinical trials on the potential synergistic and adverse side effects of herb-drug interactions as well as their mechanisms are warranted. Hyperlipidemic patients should be warned about the potential risks of herb-drug interactions, particularly those taking anticoagulants and antiplatelet drugs.
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http://dx.doi.org/10.1155/2014/925302DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4109135PMC
April 2015

A review of the phytochemistry and pharmacological activities of raphani semen.

Evid Based Complement Alternat Med 2013 8;2013:636194. Epub 2013 Jul 8.

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong.

The dried ripe seed of Raphanus sativus L., commonly known as radish seed (or Raphani Semen), is used as traditional Chinese medicine (TCM) to treat constipation, chronic tracheitis, and hypertension. The major active compounds in Raphani Semen are alkaloids, glucosinolates, brassinosteroids, and flavonoids. Fatty acids are its main nutritional contents. Raphani Semen has been demonstrated to have beneficial effects on hypertension, obesity, diabetes mellitus, constipation, and cough. So far, there is no report about the adverse/toxic effects of this herb on humans. However, Raphani Semen processed by roasting was reported to exhibit some adverse effects on mice. Additionally, erucic acid, the main fatty acid in Raphani Semen, was shown to enhance the toxicity of doxorubicin. Thus, Raphani Semen has a potential risk of causing toxicity and drug interaction. In summary, Raphani Semen is a valuable TCM herb with multiple pharmacological effects. More studies on Raphani Semen could help better understand its pharmacological mechanisms so as to provide clear scientific evidence to explain its traditional uses, to identify its therapeutic potential on other diseases, and to understand its possible harmful effects.
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http://dx.doi.org/10.1155/2013/636194DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3723324PMC
August 2013

Fingerprint analysis and simultaneous determination of phenolic compounds in extracts of Curculiginis Rhizoma by HPLC-diode array detector.

Chem Pharm Bull (Tokyo) 2013 ;61(8):802-8

Yancheng Institute of Health Science; Yancheng 224005, China.

Curculiginis Rhizoma (Curculigo orchioides GAERTN.) is a well-known Chinese herbal medicine, as well as an important Rasayana drug in India. Current criteria of quality control on this herb are to quantitatively analyze single compound curculigoside, which fail to comprehensively evaluate quality of this herb. In this paper, a simple and reliable HPLC coupled with diode array detector (DAD) method was developed to evaluate the quality of Curculiginis Rhizoma through establishing chromatographic fingerprint and simultaneously quantitating four phenolic compounds, orcinol glucoside, orcinol, 2,6-dimethoxybenzoic acid and curculigoside. The fingerprint displayed eleven common peaks, and the similarity index of different samples was in a range of 0.890-0.977. Validation of the method was acceptable, with 96.03-102.82% accuracy in recovery test and inter and intra-day precisions were less than 2%. This developed method by having a combination of chromatographic fingerprint and quantitation analysis could be applied to the quality control of Curculiginis Rhizoma.
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http://dx.doi.org/10.1248/cpb.c12-01058DOI Listing
February 2014

Two new antioxidant diarylheptanoids from the fruits of Alpinia oxyphylla.

J Asian Nat Prod Res 2013 22;15(10):1094-9. Epub 2013 Jul 22.

a Department of Pharmacy , Yancheng Institute of Health Science , Yancheng , 224005 , China.

Two new diarylheptanoids, 1-(3',5'-dihydroxy-4'-methoxyphenyl)-7-phenyl-3-heptanone (1) and 1-(2',4'-dihydroxy-3'-methoxyphenyl)-7-(4″-methoxyphenyl)-3-heptanone (2), along with known diarylheptanoid yakuchinone A (3), and five flavanoids, tectochrysin (4), chrysin (5), izalpinin (6), kaempferol 7, 4'-dimethyl ether (7), and kaempferide (8) were isolated from the fruits of Alpinia oxyphylla Miq. Their structures were determined by means of spectroscopic methods. Antioxidant activities of all the isolated compounds were evaluated using a 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay. Compounds 1-3 and 6-8 exhibited potent antioxidant activities in the DPPH assay.
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http://dx.doi.org/10.1080/10286020.2013.816297DOI Listing
January 2014

Gui-ling-gao, a traditional Chinese functional food, prevents oxidative stress-induced apoptosis in H9c2 cardiomyocytes.

Food Funct 2013 Apr;4(5):745-53

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Shenzhen, PR China.

Functional foods have become an increasingly popular alternative to prevent diseases and maintain body health status. Gui-ling-gao (GLG, also known as turtle jelly) is a well-known traditional functional food popular in Southern China and Hong Kong. This study aimed to investigate the antioxidative and anti-apoptotic effects of GLG, a traditional Chinese functional food, on preventing oxidative stress-induced injury in H9c2 cardiomyocytes. In this study, the antioxidative capacities of GLG were measured by using both a cell-free assay [2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl assay] and biological methods [2,2'-azobis(2-amidinopropane)-induced haemolysis assay and H(2)O(2)-induced cell damage on H9c2 cardiomyocytes]. Additionally, the total phenolic content was measured using the Folin-Ciocalteu method. Furthermore, the anti-apoptotic effect of GLG was evaluated by nuclear staining and a DNA fragmentation assay. GLG was found to have good antioxidant activities and high total phenolic content. In H(2)O(2)-induced cell damage on H9c2 cells, GLG was demonstrated to ameliorate the apoptotic effects, such as nuclear condensations, increased intracellular caspase-3 activity and inter-nucleosomal DNA cleavage, induced by H(2)O(2). The present study demonstrated for the first time that GLG possesses anti-apoptotic potential in vitro and this effect may be mediated, in part, by its antioxidative function. Additionally, the antioxidative capacities of GLG were proved both chemically and biologically. This study provides scientific evidence to prove the anecdotal health-beneficial claim that the consumption of GLG could help the body to handle endogenous toxicants such as free radicals.
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http://dx.doi.org/10.1039/c3fo30182fDOI Listing
April 2013

Suppression of diet-induced hypercholesterolemia by turtle jelly, a traditional chinese functional food, in rats.

Evid Based Complement Alternat Med 2012 31;2012:320304. Epub 2012 Oct 31.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, 518057 Shenzhen, China.

Consumption of functional foods for lowering serum cholesterol has globally gained acceptance by the general public. Turtle jelly (TJ), also called gui-ling-gao, is a popular traditional functional food in southern China. The hypocholesterolemic effect of consuming TJ was investigated in rats fed with normal diet, high-cholesterol diet or high-cholesterol diet supplemented with simvastatin (3 mg/kg bw per day, p.o.) or TJ (3.3 or 10 mL/kg bw per day, p.o.) for 30 days. TJ markedly reversed the increased serum total cholesterol, increased high-density lipoprotein, and decreased high-density lipoprotein induced by hypercholesterolemic diet with a dose-dependent improvement on the atherogenic index. It also demonstrated good hepatoprotective function by reducing fat depositions and overall lipid contents in the liver and increasing the activities of hepatic antioxidative enzymes. The blunted nitric oxide/endothelium-mediated aortic relaxation in rats fed with hypercholesterolemic diet was partially restored after TJ consumption. It is postulated that the hypocholesterolemic effect is the primary beneficial effect given by TJ; it then leads to secondary beneficial effects such as vasoprotective and hepatoprotective functions. The results revealed that TJ could block the downregulation of LDLR and PEPCK and upregulation of PPARα mRNA and protein expressions in the livers of rats fed with hypercholesterolemic diet.
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http://dx.doi.org/10.1155/2012/320304DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3514861PMC
December 2012

Anti-inflammatory activities and mechanisms of action of the petroleum ether fraction of Rosa multiflora Thunb. hips.

J Ethnopharmacol 2011 Dec 13;138(3):717-22. Epub 2011 Oct 13.

State Key Laboratory of Chinese Medicine and Molecular Pharmacology, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Shenzhen, PR China.

Ethnopharmacological Relevance: The hip of Rosa multiflora Thunb. has been traditionally used as a dietary supplement and a herbal remedy for the treatment of various diseases including cold, flu, inflammation, osteoarthritis, rheumatoid arthritis and chronic pain in China.

Aims Of The Study: To explore the anti-inflammatory ingredient of the hip of R. multiflora Thunb. and its mechanism of action.

Materials And Methods: The ethanol extract of the hip of R. multiflora Thunb. was fractioned with petroleum ether, ethyl acetate and water, and each fraction was screened for anti-inflammatory activity in xylene-induced mouse ear edema model. Three more models, acetic acid-induced mouse vascular permeation, cotton pellet-induced rat granuloma, and carrageenan-induced rat hind paw edema were also employed to verify the anti-inflammatory effect of the identified fraction. To explore the mechanism of action, the activity of inducible nitric oxide synthase (iNOS) and the level of nitric oxide (NO) in sera, as well as mRNA expression level of cyclo-oxygenase-2 (COX-2) in inflammatory tissues of rats with carrageenan-induced hind paw edema were measured. GC-MS technology was applied to identify the active components in the active fraction.

Results And Conclusions: The petroleum ether fraction (PEF) was identified to be the active fraction in inflammation animal models (i.e., oral administration of PEF (168.48, 42.12 and 10.53 mg/kg) evoked a significantly (P<0.001) dose-dependent inhibition of the xylene-induced mice ear edema). Down-regulating COX-2 expression (P<0.001) and reducing NO production (P<0.05) through inhibiting iNOS activity (P<0.001) may be the partial mechanism of action of PEF. GC-MS analysis indicated that unsaturated fatty acids are enriched in PEF and may be responsible for the anti-inflammatory activity of PEF and this herb. The results of this study provide pharmacological and chemical basis for the application of the hip of R. multiflora Thunb. in inflammatory disorders.
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http://dx.doi.org/10.1016/j.jep.2011.10.010DOI Listing
December 2011