Publications by authors named "Ashik Mosaddik"

24 Publications

  • Page 1 of 1

Unfolding the apoptotic mechanism of antioxidant enriched-leaves of Tabebuia pallida (lindl.) miers in EAC cells and mouse model.

J Ethnopharmacol 2021 Oct 10;278:114297. Epub 2021 Jun 10.

Department of Pharmacy, University of Rajshahi, Rajshahi, 6205, Bangladesh. Electronic address:

Ethnopharmacological Relevance: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. The leaves and barks of T. pallida are used as traditional medicine in the form of herbal or medicinal tea to manage cancer, fever, and pain. Moreover, extracts from the leaves of T. pallida showed anticancer activity. However, the chemical profile and mechanism of anticancer activity of T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) remain unexplored.

Aim Of The Study: The present study was designed to explore the regulation of apoptosis by T. pallida using Ehrlich Ascites Carcinoma (EAC) cultured cells and an EAC mouse model. LC-ESI-MS/MS was used for compositional analysis of T. pallida extracts.

Materials And Methods: Dried and powdered TPL, TPSB, TPRB and TPF were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from active extracts. Computer aided analyses was undertaken to sort out the best-fit phytoconstituent of total ten isolated compounds of this plant for antioxidant and anticancer activity.

Results: In EAC mice compared with untreated controls, the TPL extract exhibited the highest cancer cell toxicity with significant tumor cell growth inhibition (p < 0.001), reduced ascites by body weight (p < 0.01), increased the life span (p < 0.001), normalized blood parameters (RBC/WBC counts), and increased the levels of superoxide dismutase and catalase. TPL-treated EAC cells showed increased apoptotic characteristics of membrane blebbing, chromatin condensation and nuclear fragmentation, and caspase-3 activation, compared with untreated EAC cells. Moreover, annexin V-FITC and propidium iodide signals were greatly enhanced in response to TPL treatment, indicating apoptosis induction. Pro- and anti-apoptotic signaling after TPL treatment demonstrated up-regulated p53, Bax and PARP-1, and down-regulated NFκ-B, Bcl-2 and Bcl-xL expression, suggesting that TPL shifts the balance of pro- and anti-apoptotic genes towards cell death. LC-ESI-MS data of TPL showed a mixture of glycosides, lapachol, and quercetin antioxidant and its derivatives that were significantly linked to cancer cell targets. The compound, pelargonidin-3-O-glucoside was found to be most effective in computer aided models.

Conclusions: In conclusion, the TPL extract of T. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.
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http://dx.doi.org/10.1016/j.jep.2021.114297DOI Listing
October 2021

Traditional foods with their constituent's antiviral and immune system modulating properties.

Heliyon 2021 Jan 14;7(1):e05957. Epub 2021 Jan 14.

Department of Pharmacy, University of Rajshahi, Rajshahi, 6205, Bangladesh.

Background: Viruses are responsible for several diseases, including severe acute respiratory syndrome, a condition caused by today's pandemic coronavirus disease (COVID-19). A negotiated immune system is a common risk factor for all viral infections, including COVID-19. To date, no specific therapies or vaccines have been approved for coronavirus. In these circumstances, antiviral and immune boosting foods may ensure protection against viral infections, especially SARS-CoV-2 by reducing risk and ensuring fast healing of SARS-CoV-2 illness.

Scope And Approach: In this review, we have conducted an online search using several search engines (Google Scholar, PubMed, Web of Science and Science Direct) to find out some traditional foods (plant, animal and fungi species), which have antiviral and immune-boosting properties against numerous viral infections, particularly coronaviruses (CoVs) and others RNA-virus infections. Our review indicated some foods to be considered as potential immune enhancers, which may help individuals to overcome viral infections like COVID-19 by modulating immune systems and reducing respiratory problems. Furthermore, this review will provide information regarding biological properties of conventional foods and their ingredients to uphold general health.

Key Findings And Conclusions: We observed some foods with antiviral and immune-boosting properties, which possess bioactive compounds that showed significant antiviral properties against different viruses, particularly RNA viruses such as CoVs. Interestingly, some antiviral and immune-boosting mechanisms were very much similar to the antiviral drug of COVID-19 homologous SARS (Severe Acute Respiratory Syndrome Coronavirus) and MERS (Middle East Respiratory Syndrome Coronavirus). The transient nature and the devastating spreading capability of COVID-19 lead to ineffectiveness of many curative therapies. Therefore, body shielding and immune-modulating foods, which have previous scientific recognition, have been discussed in this review to discern the efficacy of these foods against viral infections, especially SARS-CoV-2.
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http://dx.doi.org/10.1016/j.heliyon.2021.e05957DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7806454PMC
January 2021

Indole bearing thiadiazole analogs: synthesis, β-glucuronidase inhibition and molecular docking study.

BMC Chem 2019 Dec 4;13(1):14. Epub 2019 Feb 4.

4Department of Chemistry, College of Sciences and Humanities, Prince Sattam Bin Abdulaziz University, P.O. Box 83, Al-Kharj, 11942 Saudi Arabia.

Indole based thiadiazole derivatives (-) have synthesized, characterized by NMR and HREI-MS and evaluated for β-Glucuronidase inhibition. All compounds showed outstanding β-glucuronidase activity with IC values ranging between 0.5 ± 0.08 to 38.9 ± 0.8 µM when compared with standard d-saccharic acid 1,4 lactone (IC value of 48.1 ± 1.2 µM). The compound , a 2,3-dihydroxy analog was found the most potent among the series with IC value 0.5 ± 0.08 µM. Structure activity relationship has been established for all compounds. To confirm the binding interactions of these newly synthesized compounds, molecular docking study have been carried out which reveal that these compounds established stronger hydrogen bonding networks with active site residues.
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http://dx.doi.org/10.1186/s13065-019-0522-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6661955PMC
December 2019

2,5-Disubstituted thiadiazoles as potent β-glucuronidase inhibitors; Synthesis, in vitro and in silico studies.

Bioorg Chem 2019 10 12;91:103126. Epub 2019 Jul 12.

Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box1982, Dammam 31441, Saudi Arabia; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

Twenty-five thiadiazole derivatives 1-25 were synthesized from methyl 4-methoxybenzoate via hydrazide and thio-hydrazide intermediates, and evaluated for their potential against β-glucuronidase enzyme. Most of the compounds including 1 (IC = 26.05 ± 0.60 μM), 2 (IC = 42.53 ± 0.80 μM), 4 (IC = 38.74 ± 0.70 μM), 5 (IC = 9.30 ± 0.29 μM), 6 (IC = 6.74 ± 0.26 μM), 7 (IC = 18.40 ± 0.66 μM), and 15 (IC = 18.10 ± 0.53 μM) exhibited superior activity potential than the standard d-saccharic acid-1,4-lactone (IC = 48.4 ± 1.25 μM). Molecular docking studies were conducted to correlate the in vitro results and to identify possible mode of interaction with enzyme active site.
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http://dx.doi.org/10.1016/j.bioorg.2019.103126DOI Listing
October 2019

Synthesis of oxadiazole-coupled-thiadiazole derivatives as a potent β-glucuronidase inhibitors and their molecular docking study.

Bioorg Med Chem 2019 07 4;27(14):3145-3155. Epub 2019 Jun 4.

Department of Computer Information Systems, College of Computer Science & Information Technology (CCSIT) Imam Abdulrahman Bin Faisal University P.O. Box 1982, Dammam 31441, Saudi Arabia.

A new series of oxadiazole with thiadiazole moiety (6-27) were synthesized, characterized by different spectroscopic techniques and evaluated for β-glucuronidase inhibitory potential. Sixteen analogs such as 6, 7, 8, 9, 10, 12, 13, 14, 17, 18, 20, 23, 24, 25, 26 and 27 showed IC values in the range of 0.96 ± 0.01 to 46.46 ± 1.10 μM, and hence were found to have excellent inhibitory potential in comparison to standard d-saccharic acid 1,4-lactone (IC = 48.4 ± 1.25 μM). Two analogs such as 16 and 19 showed moderate inhibitory potential while analogs 11, 15, 21 and 22 were found inactive. Our study identifies new series of potent β-glucuronidase inhibitors for further investigation. Structure activity relationships were established for all compounds which showed that the activity is varied due to different substituents on benzene ring. The interaction of the compounds with enzyme active site were confirmed with the help of docking studies, which reveals that the electron withdrawing group and hydroxy group make the molecules more favorable for enzyme inhibition.
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http://dx.doi.org/10.1016/j.bmc.2019.05.049DOI Listing
July 2019

Synthesis, Molecular Docking and β-Glucuronidase Inhibitory Potential of Indole Base Oxadiazole Derivatives.

Molecules 2019 Mar 8;24(5). Epub 2019 Mar 8.

Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, 31441 Dammam, Saudi Arabia.

β-glucuronidase is a lysosomal glycosidase enzyme which catalyzes the extracellular matrix of cancer and normal cells and the glycosaminoglycans of the cell membrane, which is important for cancer cell proliferation, invasion, and metastasis. Liver cancer, colon carcinoma, and neoplasm bladder are triggered by the increase of the level of β-glucuronidase activity. The most valuable structures are indole and oxadiazole which has gain immense attention because of its pharmacological behavior and display many biological properties. Twenty-two (⁻) analogs of indole based oxadiazole were synthesized and screened for their inhibitory potential against β-glucuronidase. Majority of the compounds showed potent inhibitory potential with IC values ranging between 0.9 ± 0.01 to 46.4 ± 0.9 µM, under positive control of standard drug d-saccharic acid 1,4 lactone (IC = 48.1 ± 1.2 µM). Structural activity relationship (SAR) has been established for all synthesized compounds. To shed light on molecular interactions between the synthesized compounds and β-glucuronidase, , , and compounds were docked into the active binding site of β-glucuronidase. The obtained results showed that this binding is thermodynamically favorable and β-glucuronidase inhibition of the selected compounds increases with the number of hydrogen bonding established in selected compound-β-glucuronidase complexes.
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http://dx.doi.org/10.3390/molecules24050963DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6429331PMC
March 2019

Synthesis of novel quinoline-based thiadiazole, evaluation of their antileishmanial potential and molecular docking studies.

Bioorg Chem 2019 04 21;85:109-116. Epub 2018 Dec 21.

College of Computer Science & Information Technology (CCSIT), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

New series of quinoline-based thiadiazole analogs (1-20) were synthesized, characterized by EI-MS, H NMR and C NMR. All synthesized compounds were subjected to their antileishmanial potential. Sixteen analogs 1-10, 12, 13, 16, 17, 18 and 19 with IC values in the range of 0.04 ± 0.01 to 5.60 ± 0.21 µM showed tremendously potent inhibition as compared to the standard pentamidine with IC value 7.02 ± 0.09 µM. Analogs 11, 14, 15 and 20 with IC 8.20 ± 0.35, 9.20 ± 0.40, 7.20 ± 0.20 and 9.60 ± 0.40 µM respectively showed good inhibition when compared with the standard. Structure-activity relationships have been also established for all compounds. Molecular docking studies were performed to determine the binding interaction of the compounds with the active site target.
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http://dx.doi.org/10.1016/j.bioorg.2018.12.025DOI Listing
April 2019

Synthesis of benzothiazole derivatives as a potent α-glucosidase inhibitor.

Bioorg Chem 2019 04 15;85:33-48. Epub 2018 Dec 15.

College of Computer Science & Information Technology (CCSIT), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

Diabetes is one of the pre-dominant metabolic disorders all over the world. It is the prime reason of mortality and morbidity due to hyperglycemia which is link with numerus obstacles. Delaying absorption and digestion of carbohydrate has great therapeutic impact for governing postprandial hyperglycemia. Consequently, alpha glucosidase is one of the potential therapeutic approaches that reduce absorption of glucose and delay carbohydrate digestion hence maintaining blood glucose level. In this regard we have synthesized benzothiazole based oxadiazole in search of potent anti-diabetic agent as α-glucosidase Inhibitors. Benzothiazole based oxadiazole derivatives 1-23 have been synthesized, characterized by HNMR, CNMR, and MS and evaluated for α-glucosidase Inhibition. All analogs exhibited a varying degree of α-glucosidase inhibitory activity with IC values ranging in between 0.5 ± 0.01-30.90 ± 0.70 μM when compared with the standard acarbose (IC = 866.30 ± 3.20 μM). Structure activity relationship has been established for all compounds. Molecular docking studies were performed to predict the binding interaction of the compounds with the active site of enzyme.
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http://dx.doi.org/10.1016/j.bioorg.2018.12.021DOI Listing
April 2019

Synthesis of Bis-indolylmethane sulfonohydrazides derivatives as potent α-Glucosidase inhibitors.

Bioorg Chem 2018 10 2;80:112-120. Epub 2018 Jun 2.

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan; Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

In search of better α-glucosidase inhibitors, a series of bis-indolylmethane sulfonohydrazides derivatives (1-14) were synthesized and evaluated for their α-glucosidase inhibitory potential. All derivatives exhibited outstanding α-glucosidase inhibition with IC values ranging between 0.10 ± 0.05 to 5.1 ± 0.05 μM when compared with standard drug acarbose having IC value 856.28 ± 3.15 μM. Among the series, analog 7 (0.10 ± 0.05 μM) with tri-chloro substitution on phenyl ring was identified as the most potent inhibitor of α-glucosidase (∼ 8500 times). The structure activity relationship has been also established. Molecular docking studies were also performed to help understand the binding interaction of the most active analogs with receptors. From the docking studies, it was observed that all the active bis-indolylmethane sulfonohydrazides derivatives showed considerable binding interactions within the active site (acarbose inhibition site) of α-glucosidase. We also evaluated toxicity of all derivatives and found none of them are toxic.
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http://dx.doi.org/10.1016/j.bioorg.2018.06.001DOI Listing
October 2018

Synthesis, SAR elucidations and molecular docking study of newly designed isatin based oxadiazole analogs as potent inhibitors of thymidine phosphorylase.

Bioorg Chem 2018 09 17;79:323-333. Epub 2018 May 17.

Department of Neuroscience Research, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam 31441, Saudi Arabia.

Thymidine phosphorylase is an enzyme involved in pyrimidine salvage pathway that is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. It is enormously up regulated in a variety of solid tumors. Furthermore, surpassing of TP level protects tumor cells from apoptosis and helps cell survival. Thus TP is identified as a prime target for developing novel anticancer therapies. A new class of exceptionally potent isatin based oxadiazole (1-30) has been synthesized and evaluated for thymidine phosphorylase inhibitory potential. All analogs showed potent thymidine phosphorylase inhibition when compared with standard 7-Deazaxanthine, 7DX (IC = 38.68 ± 1.12 µM). Molecular docking study was performed in order to determine the binding interaction of these newly synthesized compounds, which revealed that these synthesized compounds established stronger hydrogen bonding network with active site of residues as compare to the standard compound 7DX.
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http://dx.doi.org/10.1016/j.bioorg.2018.05.011DOI Listing
September 2018

Synthesis, in vitro α-glucosidase inhibitory potential and molecular docking study of thiadiazole analogs.

Bioorg Chem 2018 08 20;78:201-209. Epub 2018 Mar 20.

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

α-Glucosidase is a catabolic enzyme that regulates the body's plasma glucose levels by providing energy sources to maintain healthy functioning. 2-Amino-thiadiazole (1-13) and 2-amino-thiadiazole based Schiff bases (14-22) were synthesized, characterized by H NMR and HREI-MS and screened for α-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of α-glucosidase inhibitory potential with IC values ranging between 2.30 ± 0.1 to 38.30 ± 0.7 μM, when compare with standard drug acarbose having IC value of 39.60 ± 0.70 μM. Among the series eight derivatives 1, 2, 6, 7, 14, 17, 19 and 20 showed outstanding α-glucosidase inhibitory potential with IC values of 3.30 ± 0.1, 5.80 ± 0.2, 2.30 ± 0.1, 2.70 ± 0.1, 2.30 ± 0.1, 5.50 ± 0.1, 4.70 ± 0.2, and 5.50 ± 0.2 μM respectively, which is many fold better than the standard drug acarbose. The remaining analogs showed good to excellent α-glucosidase inhibition. Structure activity relationship has been established for all compounds. The binding interactions of these compounds were confirmed through molecular docking.
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http://dx.doi.org/10.1016/j.bioorg.2018.03.022DOI Listing
August 2018

Comparative study of antidiabetic activity of Cajanus cajan and Tamarindus indica in alloxan-induced diabetic mice with a reference to in vitro antioxidant activity.

Pharmacognosy Res 2014 Apr;6(2):180-7

Department of Pharmacy, University of Rajshahi, Rajshahi, Bangladesh.

Background: Oxidative stress not only develops complications in diabetic (type 1 and type 2) but also contributes to beta cell destruction in type 2 diabetes in insulin resistance hyperglycemia. Glucose control plays an important role in the pro-oxidant/antioxidant balance. Some antidiabetic agents may by themselves have antioxidant properties independently of their role on glucose control.

Objective: The present investigation draws a comparison of the protective antioxidant activity, total phenol content and the antihyperglycemic activity of the methanolic extract of Cajanus cajan root (MCC) and Tamarindus indica seeds (MTI).

Materials And Methods: Antidiabetic potentials of the plant extracts were evaluated in alloxan-induced diabetic Swiss albino mice. The plant extracts at the doses of 200 and 400 mg/kg body weight was orally administered for glucose tolerance test during 1-hour study and hypoglycemic effect during 5-day study period in comparison with reference drug Metformin HCl (50 mg/kg). In vitro antioxidant potential of MCC and MTI was investigated by using 1, 1- diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity at 517 nm. Total phenolic content, total antioxidant capacity and reducing power activity was also assayed.

Results: There was a significant decrease in fasting serum glucose level (P < 0.001), reduction in blood glucose level (P < 0.001) in 5-days study, observed in the alloxan-induced diabetic mice. The reduction efficacy of blood glucose level of both the extracts is proportional to their dose but MCC is more potent than MTI. Antioxidant study and quantification of phenolic compound of both the extracts revealed that they have high antioxidant capacity.

Conclusion: These studies showed that MCC and MTI have both hypoglycemic and antioxidant potential but MCC is more potent than MTI. The present study suggests that both MCC and MTI could be used in managing oxidative stress.
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http://dx.doi.org/10.4103/0974-8490.129043DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3996756PMC
April 2014

Induction of apoptosis by ethanolic extract of mango peel and comparative analysis of the chemical constitutes of mango peel and flesh.

Food Chem 2012 Jul 25;133(2):416-22. Epub 2012 Jan 25.

Faculty of Biotechnology, College of Applied Life Sciences, Jeju National University, 66 Jejudaehakno, Jeju 690-756, Republic of Korea; Subtropical Horticulture Research Institute, Jeju National University, Jeju 690-756, Republic of Korea. Electronic address:

The underlying mechanisms of the anticancer activity of the ethanolic extract of mango peel (EEMP) and its constituents were investigated. EEMP induced death of human cervical carcinoma HeLa cells through apoptosis, as evidenced by the increased cell population in the sub-G1 phase and the appearance of fragmented nuclei. Treatment of the cells with EEMP also downregulated anti-apoptotic Bcl-2 expression, resulting in the proteolytic activation of caspase-3, 7, 8, and 9 and the degradation of poly (ADP-ribose) polymerase (PARP) protein. The major components of mango peel were identified by liquid chromatography-electrospray ionisation tandem mass spectrometry and gas chromatography-mass spectrometry. Our data suggest that EEMP is an excellent source of quercetin 3-O-galactoside, mangiferin gallate, isomangiferin gallate, quercetin-3-O-arabinopyranoside, and mangiferin along with unsaturated fatty acids oleic acid, linoleic acid, and ethyl linoleate, which may help to prevent cervical cancer and may be a useful agent for the treatment of some other malignancies.
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http://dx.doi.org/10.1016/j.foodchem.2012.01.053DOI Listing
July 2012

A hexane fraction of guava Leaves (Psidium guajava L.) induces anticancer activity by suppressing AKT/mammalian target of rapamycin/ribosomal p70 S6 kinase in human prostate cancer cells.

J Med Food 2012 Mar 26;15(3):231-41. Epub 2012 Jan 26.

College of Oriental Medicine, Kyung Hee University, Seoul, Korea.

This study was carried out to evaluate the anticancer effects of guava leaf extracts and its fractions. The chemical compositions of the active extracts were also determined. In the present study, we set out to determine whether the anticancer effects of guava leaves are linked with their ability to suppress constitutive AKT/mammalian target of rapamycin (mTOR)/ribosomal p70 S6 kinase (S6K1) and mitogen-activated protein kinase (MAPK) activation pathways in human prostate cancer cells. We found that guava leaf hexane fraction (GHF) was the most potent inducer of cytotoxic and apoptotic effects in PC-3 cells. The molecular mechanism or mechanisms of GHF apoptotic potential were correlated with the suppression of AKT/mTOR/S6K1 and MAPK signaling pathways. This effect of GHF correlated with down-regulation of various proteins that mediate cell proliferation, cell survival, metastasis, and angiogenesis. Analysis of GHF by gas chromatography and gas chromatography-mass spectrometry tentatively identified 60 compounds, including β-eudesmol (11.98%), α-copaene (7.97%), phytol (7.95%), α-patchoulene (3.76%), β-caryophyllene oxide (CPO) (3.63%), caryophylla-3(15),7(14)-dien-6-ol (2.68%), (E)-methyl isoeugenol (1.90%), α-terpineol (1.76%), and octadecane (1.23%). Besides GHF, CPO, but not phytol, also inhibited the AKT/mTOR/S6K1 signaling pathway and induced apoptosis in prostate cancer cells. Overall, these findings suggest that guava leaves can interfere with multiple signaling cascades linked with tumorigenesis and provide a source of potential therapeutic compounds for both the prevention and treatment of cancer.
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http://dx.doi.org/10.1089/jmf.2011.1701DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3282482PMC
March 2012

The butanol fraction of guava (Psidium cattleianum Sabine) leaf extract suppresses MMP-2 and MMP-9 expression and activity through the suppression of the ERK1/2 MAPK signaling pathway.

Nutr Cancer 2012 2;64(2):255-66. Epub 2012 Jan 2.

College of Oriental Medicine and Institute of Oriental Medicine, Kyung Hee University, Seoul, Republic of Korea.

The leaf extract of guava (Psidium cattleianum Sabine) has traditionally been used for the treatment of diarrhea and diabetes in East Asia and other countries. Recently, the leaf extract has been employed in the therapy of cancer, bacterial infections, and inflammation in experimental models. However, the exact mechanisms of how guava leaf extract inhibits tumor metastasis and invasion are still unknown. In the present study, we investigated in detail the molecular mechanism(s) responsible for the potential antimetastatic and antiinvasive effects of the butanol fraction of guava leaf extract (GBF). Interestingly, we observed for the first time that GBF suppressed both matrix metalloproteinases (MMP)-9 and MMP-2 expression and activity in part through the downregulation of the ERK1/2 activation in lung cancer cells. Also, importantly, the major components of the GBF were identified as d-glucuronic acid, quercetin 3-glucuronide, loganin, and xanthyletin by LC-ESI-MS/MS. Collectively, our data indicate that the guava leaf could reduce the metastasis of lung cancer cells and therefore suggest that it could be advantageously used to control the metastatic process.
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http://dx.doi.org/10.1080/01635581.2012.642455DOI Listing
June 2012

Antimicrobial, antileishmanial and cytotoxic compounds from Piper chaba.

Nat Prod Res 2012 11;26(11):979-86. Epub 2011 Aug 11.

Department of Pharmacy, University of Rajshahi, Rajshahi 6205, Bangladesh.

The petroleum ether and chloroform extracts of the root of Piper chaba showed antimicrobial, antileishmanial and cytotoxic activities. Further bioactivity-guided fractionation led to the isolation of Bornyl piperate (1), piperlonguminine (2) and piperine (3). This is the first report of isolation of compounds (1) and (2) from P. chaba. It was observed that the isolated compounds (1 and 2) showed potent antifungal activity when compared with standard drug Nystatin, and significant cytotoxic activity with the IC₅₀ values of 0.76 and 0.83 µg mL⁻¹, respectively. These compounds were also found to have weak antibacterial and antileishmanial activities. This is the first report about the antileishmanial activity of Piper isolates.
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http://dx.doi.org/10.1080/14786419.2010.535166DOI Listing
September 2012

Comparative antioxidant and antiproliferative activities of red and white pitayas and their correlation with flavonoid and polyphenol content.

J Food Sci 2011 Jan-Feb;76(1):C38-45. Epub 2010 Nov 29.

Faculty of Biotechnology, College of Applied Life Sciences, Jeju Natl. Univ., Jeju 690-756, Republic of Korea.

Pitaya, commonly known as dragon fruit, has generated considerable consumer interest because of its attractive color and micronutrient content. The present study investigated the total polyphenol and flavonoid content, antioxidant activity against various free radicals, and antiproliferative effect on several cancer cell lines of extracts of flesh and peel of white and red pitayas, collected from Jeju Island, Korea. The total polyphenol and flavonoid contents of 80% methanol extracts of red pitaya peel (RPP) and white pitaya peel (WPP) were approximately 3- and 5-fold higher than those of red pitaya flesh (RPF) and white pitaya flesh (WPF), respectively. Overall, the total flavonoid and polyphenol contents of these extracts were RPP>WPP>RPF>WPF and WPP>RPP>RPF>WPF, respectively. In addition, a study involving nontargeted high-performance liquid chromatography coupled with a photodiode array and electrospray ionization mass spectrometry (HPLC-PDA-ESI-MS) of different pitaya extracts indicated the presence of phenolic, hydroxycinnamic acid derivatives, flavonol glycosides, betacyanin, and its derivatives with a few unknown compounds. Separately, peel extracts of both red and white pitayas showed higher 2,2-diphenyl-1-picrylhydrazyl, hydroxyl, and alkyl radical-scavenging activity than did the corresponding flesh extracts. Both peel extracts also showed stronger antiproliferative activity against AGS and MCF-7 cancer cells than either flesh extract. There was a direct correlation between the phenolic content and antioxidant effect, but no correlation observed between antioxidant activity and antiproliferative activity. These results suggest that the peel of white and red pitaya may be a valuable ingredient in foods and may also be useful in cosmetic, nutraceutical, and pharmaceutical applications.
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http://dx.doi.org/10.1111/j.1750-3841.2010.01908.xDOI Listing
September 2011

Mosquitocidal triterpenes from the stem of Duranta repens.

Pharm Biol 2010 Mar;48(3):264-8

Department of Biochemistry and Molecular Biology, University of Rajshahi, Bangladesh.

Two triterpenes, beta-amyrin and 12-oleanene 3beta, 21beta-diol, were isolated as a mixture from the chloroform soluble fraction of an ethanol extract of Duranta repens Linn (Verbenaceae) stem. The structures of the two compounds were confirmed by analysis of their IR, (1)H-NMR, (13)C-NMR and LC-MS spectral data. The mixture of beta-amyrin and 12-oleanene 3beta, 21beta-diol (compound 1) was highly effective against the larvae of the mosquito, Culex quinquefasciatus Say (Diptera: Culicidae), as a mosquitocide.
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http://dx.doi.org/10.3109/13880200903096570DOI Listing
March 2010

Induction of apoptosis in human cervical carcinoma HeLa cells by polymethoxylated flavone-rich Citrus grandis Osbeck (Dangyuja) leaf extract.

Food Chem Toxicol 2010 Aug-Sep;48(8-9):2435-42. Epub 2010 Jun 9.

Faculty of Biotechnology, College of Applied Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.

Citrus grandis Osbeck (Dangyuja) has a high content of flavonoids with health-related properties. Although previous data have revealed the anticancer potency of some Citrus species, the underlying molecular mechanisms of this activity by leaf extracts have not been studied in detail. The purpose of this study was to evaluate the cytotoxic effects of citrus leaves on five human cancer cell lines and to determine the possible mechanisms of cell death elicited by the chloroform fraction (CF) of the Dangyuja leaf. The CF of Dangyuja strongly decreased the survival rate of HeLa cells, among the tested cell lines. CF treatment induced the down-regulation of anti-apoptotic Bcl-2 expression, resulting in the proteolytic activation of caspases and the degradation of poly (ADP-ribose) polymerase (PARP) protein. Arrested cell growth and induction of apoptosis were confirmed by flow cytometry and DNA fragmentation analysis, respectively. The major components of the CF were identified as isosinensetin, sinensetin, tetramethyl-O-isoscutellarein, nobiletin, tangeretin, and 5-hydroxy-6,7,8,3',4'-pentamethoxyflavone by liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). Our results suggest that the CF of Dangyuja leaves is an excellent source of functional polymethoxylated flavones, which may help prevent cervical cancer and may potentially be a useful agent for the treatment of certain malignancies.
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http://dx.doi.org/10.1016/j.fct.2010.06.006DOI Listing
November 2010

Antishigellosis and Cytotoxic Potency of Crude Extracts and Isolated Constituents from Duranta repens.

Mycobiology 2008 Sep 30;36(3):173-7. Epub 2008 Sep 30.

Department of Biochemistry and Molecular Biology, University of Rajshahi-6205, Bangladesh.

The crude ethanol extracts (stem and fruits), their fractions and two triterpenes, β-Amyrin and 12-Oleanene 3β, 21β-diol, isolated as a mixture from the chloroform soluble fraction of an ethanolic extract of Duranta repens stem, were evaluated for antibacterial, antifungal activities by the disc diffusion method and cytotoxicity by brine shrimp lethality bioassay. The structures of the two compounds were confirmed by IR, (1)H-NMR, (13)C-NMR and LC-MS spectral data. The chloroform soluble fraction of stem and ethanol extract of fruits possess potent antishigellosis activity and also exhibited moderate activity against some pathogenic bacteria and fungi but the isolated compound 1 (mixture of β-Amyrin and 12-Oleanene 3β, 21β-diol) showed mild to moderate inhibitory activity to microbial growth. The minimum inhibitory concentrations (MICs) of the extracts (stem and fruits), their fractions and compound 1 were found to be in the range of 32~128 µg/ml. The chloroform soluble fractions of stem and ethanol extract of fruit showed significant cytotoxicity with LC50 value of 0.94 µg/ml and 0.49 µg/ml, respectively against brine shrimp larvae.
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http://dx.doi.org/10.4489/MYCO.2008.36.3.173DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3755189PMC
September 2008

Three new 3-benzylbenzofuran-2-one derivatives from Homalium brachybotrys (Flacourtiaceae/Salicaceae s. l.).

Nat Prod Res 2007 Nov;21(13):1191-8

Centre for Phytochemistry and Pharmacology, Southern Cross University, Lismore, NSW 2480, Australia.

Eight phenolic compounds, including two mixtures of two compounds, were isolated from the ethyl acetate extract of leaves and stems of Homalium brachybotrys. They were identified on the basis of spectroscopic data as quercetin-3-O-beta-glucopyranoside, luteolin-7-O-beta-glucopyranoside, 5,6-dihydro-6-beta-glucopyranosyloxy-3-(hydroxyphenyl-methyl)-2(4H)-benzofuranone (cochinolide 6-O-beta-glucopyranoside) (1), 2-(6-benzoyl-beta-glucopyranosyloxy)-5-hydroxybenzyl alcohol (poliothrysoside) (2), 2-(beta-glucopyranosyloxy)-5-hydroxybenzyl alcohol (salirepin) (3), 4,5-dihydro-7a-beta-glucopyranosyloxy-3-(hydroxyphenylmethyl)-2(7aH)-benzofuranone (isocochinolide-7a-O-beta-glucopyranoside) (4), 5,6-dihydro-3-(hydroxyphenylmethyl)-2(4H)-benzofuranone (6-deoxycochinolide) (5) and 3-benzylidine-6-hydroxy-2-benzofuranone (1'deoxy-4,5,6-dehydrocochinolide) (6). Benzofuranones (4), (5) and (6) are new natural products. The compounds isolated support the argument that Homalium is best placed in the Salicaceae s.l.
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http://dx.doi.org/10.1080/14786410601130679DOI Listing
November 2007

A new triterpenoid from roots of Laportea crenulata and its antifungal activity.

Nat Prod Res 2007 Sep;21(11):959-66

Department of Pharmacy, University of Rajshahi, Rajshahi 6205, Bangladesh.

A new triterpenoid 2alpha,3beta,21beta,23,28-penta hydroxyl 12-oleanene and two known compounds were isolated from the roots of Laportea crenulata Gaud. The structures of all compounds were elucidated on the basis of various spectroscopic data. The two known compounds beta-sitosterol and beta-sitosterol 3-beta-D-glucopyranoside are also the first report of isolation from this plant. The antifungal activity of new triterpenoid was studied against Aspergillus flavus, Aspergillus niger, Candida albicans, and Rhizopus aurizae, and compared with the activity of nystatin (30 microg disc(-1)). This compound has shown moderate activity against tested fungi.
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http://dx.doi.org/10.1080/14786410701371470DOI Listing
September 2007

In vitro antimicrobial and cytotoxic activities of ferrocene derivative compounds.

Pak J Biol Sci 2007 Aug;10(15):2423-9

Department of Pharmacy, University of Rajshahi, Rajshahi-6205, Bangladesh.

The aim of the present study was to investigate the biocidal activity of four new ferrocene derivative based coordination complexes, [1,2,3-trithia-/3/-ferrocenophane, C1]; [disodium-1,1'-ferrocenedithiolate, C2]; [1,1'-(ferrocene-1,1'-diyl)-diethanol, C3]; [ferrocenyl(ethyl-phenyl)-methanol, C4]; against microbes (bacteria and fungi) and brine shrimp (Artemia salina Lech.) nauplii. C2 showed modest antibacterial activity at the concentration of 200 microg disc(-1) and gave its Minimum Inhibitory Concentration values at 32-64 microg mL(-1) against the tested bacteria. These complexes gave comparatively better antibacterial activity against the Gram-positives than the Gram-negatives. C3, C1 and C4 showed moderate antifungal activity at concentration of 200 microg disc(-1). Brine shrimp eggs were hatched in artificial sea water and exposed to the complexes. Median lethal concentration (LC50) values were calculated. Both complexes showed toxicity against brine shrimp but complex C3 explored its potent cytotoxicity having LC50 values at 6.031 microg mL(-1) (ppm).
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http://dx.doi.org/10.3923/pjbs.2007.2423.2429DOI Listing
August 2007

Cytotoxicity and antimicrobial activity of goniothalamin isolated from Bryonopsis laciniosa.

Phytother Res 2003 Dec;17(10):1155-7

Centre for Phytochemistry, Southern Cross University, Lismore, NSW 2480, Australia.

The cytotoxicity and antimicrobial activity of goniothalamin isolated from Bryonopsis laciniosa was investigated. Goniothalamin showed potent cytotoxicity with LC50 values (5.03 microg/mL) comparable with the reference standard agent, gallic acid. It also showed weak antibacterial and significant antifungal activity against a wide range of gram positive and gram negative bacteria and fungi. The antibacterial (minimum inhibitory concentration) effect against Bacillus cereus and Shigella shiga was found to be 64 microg/mL.
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http://dx.doi.org/10.1002/ptr.1303DOI Listing
December 2003
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