Publications by authors named "Jian-Rong Wang"

62 Publications

Sinusiaetone A, an Anti-inflammatory Norditerpenoid with a Bicyclo[11.3.0]hexadecane Nucleus from the Hainan Soft Coral .

Org Lett 2021 Aug 16;23(15):5621-5625. Epub 2021 Jun 16.

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

A novel norditerpenoid, sinusiaetone A (), featuring an uncommon bicyclo[11.3.0]hexadecane carbon skeleton, and four polyoxygenated cembranoids () were isolated from the Hainan soft coral . Their structures were established by spectroscopic analysis, X-ray diffraction, quantum chemical computational approaches, and/or a modified Mosher's method. A plausible biosynthetic pathway of and its biogenetic relationship with were proposed. New compounds displayed an interesting inhibitory activity against lipopolysaccharide-induced inflammation in BV-2 microglial cells.
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http://dx.doi.org/10.1021/acs.orglett.1c01601DOI Listing
August 2021

Sinueretone A, a Diterpenoid with Unprecedented Tricyclo[12.1.0.0]pentadecane Carbon Scaffold from the South China Sea Soft Coral .

J Org Chem 2021 Aug 8;86(16):10975-10981. Epub 2020 Dec 8.

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

A novel diterpenoid, sinueretone A (), featuring an unprecedented tricyclo[12.1.0.0]pentadecane carbon framework, along with two new ( and ) and one known () casbane diterpenoids were isolated from the South China Sea soft coral . The structures of the new compounds, especially their absolute stereochemistry, were established by extensive spectroscopic analysis, various quantum chemical calculations, and/or X-ray diffraction analyses. A plausible biogenetic relationship of - was proposed, which gave an insight for future biomimetic synthesis of the novel compounds. In a bioassay, compounds and displayed interesting anti-inflammatory activity by the inhibition of lipopolysaccharide-induced tumor necrosis factor-α protein release.
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http://dx.doi.org/10.1021/acs.joc.0c02397DOI Listing
August 2021

Cocrystals to tune oily vitamin E into crystal vitamin E.

Int J Pharm 2021 Jan 7;592:120057. Epub 2020 Nov 7.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address:

d-α-tocopherol (d-αToc), the most biologically active form of natural Vitamin E, is oily in appearance and unstable to oxygen. Esterification and encapsulation are generally needed to stabilize and solidify d-αToc for the purpose of its expanding applications. In this study, we propose a more effective way to stabilize and solidify d-αToc oil in one step. By cocrystallization, the melting point of d-αToc is significantly increased, such that the oily d-αToc is successfully transformed into solid form at room temperature. The single crystal structure of d-αToc was firstly uncovered and the molecular interaction in cocrystals was revealed. Crystalline Vitamin E shows high stability to light and temperature. Its spherical crystallization affords good powder flowability, which is extremely important as food or feed additives. Moreover, cocrystal Vitamin E remains the original form of tocopherol without esterification and thus has a great advantage on higher bioavailability. Cocrystallization of oily d-αToc spares the use of acetic ester and a mass of excipients, which is of great environmental importance and greatly reduces the production cost.
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http://dx.doi.org/10.1016/j.ijpharm.2020.120057DOI Listing
January 2021

Studying on the impact of media coverage on the spread of COVID-19 in Hubei Province, China.

Math Biosci Eng 2020 04;17(4):3147-3159

School of Mathematical Sciences, Shanxi University, Taiyuan, Shanxi 030006, China.

Awareness of prevention is enhanced to reduce the rate of infection by media coverage, which plays an important role in preventing and controlling infectious diseases. Based on epidemic situation of the Corona Virus Disease 2019 (COVID-19) in Hubei, an SIHRS epidemic model with media coverage was proposed. Firstly, by the basic reproduction number R0, the globally asymptotically stable of the disease-free equilibrium and the endemic equilibrium were proved. Then, based on the reported epidemic data of Hubei Province from January 26 to February 13, numerical simulations are used to verify the analysis results, and the impact of peak time and the scale of disease transmission were mainly considered with different information implementation rate and the contact rate. It was shown that with the decrease of information implementation rate, the peak of confirmed cases would be delayed to reach, and would increase significantly. Therefore, in order to do a better prevention measures after resumption of work, it is very necessary to maintain the amount of information and implementation rate of media coverage.
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http://dx.doi.org/10.3934/mbe.2020178DOI Listing
April 2020

Bloodstream infections in patients undergoing extracorporeal membrane oxygenation.

Pak J Med Sci 2020 Sep-Oct;36(6):1171-1176

Ying Zhu, MS. Department of Critical Care Medicine, The Affiliated Hangzhou Hospital of Nanjing Medical University, Zhejiang, China.

Objective: We aimed to evaluate the incidence, risk factors, and prognosis of bloodstream infections (BSIs) during extracorporeal membrane oxygenation (ECMO) treatment in a Chinese population.

Methods: Patients receiving ECMO treatment from January 2013 to August 2019 were retrospectively studied. The incidence of BSIs was calculated. The clinical characteristics between patients with a BSI (BSI group) and without a BSI (non-BSI group).

Results: Among 69 included patients, 19 (27.5%) developed at least one BSI. Gram-negative bacteria (73.7%) were mainly responsible for the BSIs, with (6/19, 31.5%) ranking as the top related pathogen. The BSI group had a greater proportion of methicillin-resistant (MRSA) prophylactic regimens (52.6% vs. 26.0%, P = 0.036), a higher pre-ECMO Sequential Organ Failure Assessment (SOFA) score (11 vs. 8, P = 0.008), more applications of continuous renal replacement therapy (CRRT) during ECMO (63.1% vs. 36.1%, P = 0.042). Longer ECMO support duration, period of ventilator use before ECMO weaning and hospital stay were observed in the BSI group. The SOFA score (OR: 1.174; 95% CI: 1.039-1.326; P = 0.010) was an independent risk factor for BSIs.

Conclusion: BSIs during ECMO therapy frequently involve Gram-negative bacteria. Stringent care and monitoring should be provided for patients with high SOFA scores.
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http://dx.doi.org/10.12669/pjms.36.6.2882DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7501021PMC
September 2020

[Effect of electroacupuncture of different acupoint groups on learning-memory ability and expression of IL-1β and TNF-α in hippocampus and prefrontal cortex in rats with Alzheimer's disease].

Zhen Ci Yan Jiu 2020 Aug;45(8):617-22

Department of Human Anatomy, Chongqing Medical University, Chongqing, 400016, China.

Objective: To compare the effect of electroacupuncture (EA) of acupoint group for "reinforcing the kidney and regulating Governor Vessel" and acopoint group for "reinforcing the kidney and lung and regulating Governor Vessel" on lear-ning-memory ability and expression of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) proteins in the hippocampus and prefrontal cortex (PFC) in Alzheimer's disease (AD) rats, so as to explore the efficacy of the two acupoint groups and mechanisms underlying improvement of AD.

Methods: Forty male SD rats were randomly divided into control, sham operation, model, "Baihui" + "Shenshu" (GV20+BL23, for "reinforcing the kidney and regulating Governor Vessel") EA and GV20+BL23+ "Feishu" (BL13, GV20+BL23+BL13, for "reinforcing the kidney and lung and regulating Governor Vessel") EA groups (=8 rats in each group). The AD model was established by bilateral injection of amyloid β peptide (Aβ,10 μL) into bilateral hippocampus, and rats of the sham operation group received injection of normal saline. After successful establishment of the model,EA (2 Hz, 2 mA) was applied to these acupoints for 15 min, once daily for 10 days. Then, the learning-memory ability was assessed by using Morris water maze tests, and the expression levels of TNF-α and IL-1β proteins in the PFC and hippocampus tissues were detected by using Western blot.

Results: Following modeling, the average escape latency of place navigation test were significantly increased (<0.05) and the platform crossing times of spatial probe test was significantly decreased in the model group than in the control and sham operation groups (<0.05). The expression levels of IL-1β and TNF-α proteins in the PFC and hippocampus were apparently up-regulated in the model group than in the control and the sham operation groups (<0.000 1, <0.001, <0.01). After the intervention, the increase of the average escape latency and expression of IL-1β and TNF-α in the PFC and hippocampus, and the decrease of space exploration test were revised in both GV20+BL23 EA and GV20+BL23+BL13 EA groups (<0.05,<0.01). No significant differences were found between the GV20+BL23 and GV20+BL23+BL13 EA groups in the above mentioned indexes (>0.05).

Conclusion: EA of both GV20+BL23 and GV20+BL23+BL13 acupoint can improve learning-memory ability of AD rats, which is associated with their effects in down-regulating the expression of IL-1β and TNF-α in the PFC and hippocampus to reduce inflammatory reaction. There were no significant differences between the two acupoint groups in the therapeutic effects.
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http://dx.doi.org/10.13702/j.1000-0607.190887DOI Listing
August 2020

Comparison of the crystal structures and physicochemical properties of novel resveratrol cocrystals.

Acta Crystallogr B Struct Sci Cryst Eng Mater 2019 Dec 23;75(Pt 6):1186-1196. Epub 2019 Nov 23.

Pharmaceutical Analytical and Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang High-Tech Park, Shanghai 201203, People's Republic of China.

Resveratrol (RSV) is one of the most extensively investigated natural polyphenol with potential cardioprotective effects and various biological activities. However, the polymorphism and solvates of RSV cocrystals have not been studied comprehensively. In addition, the relationship between the crystal packing modes and their physicochemical properties of RSV cocrystals remains poorly understood. In this paper, seven novel RSV cocrystals were prepared and characterized by powder X-ray diffraction, single-crystal X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, dynamic vapor sorption, Raman and Fourier transform infrared spectroscopy. Five RSV-4,4'-vinylenedipyridine (DPE) cocrystals were synthesized with polymorphs and solvates, such as RSV-DPE (1:2) in form (I) [RSV-2DPE form (I)], RSV-DPE (1:2) in form (II) [RSV-2DPE form (II)], RSV-DPE (1:1) (RSV-DPE), RSV-DPE (2:3)·acetone (RSV-1.5DPE·0.5ACE), RSV-DPE (1:1.5)·MeOH (RSV-1.5DPE·MeOH). However, RSV-4,4'-ethylenedipyridine (BPE) and RSV-4,4'-azobispyridine (AZPY) cocrystals were prepared as their single crystal forms, that is, RSV-BPE (1:1.5) (RSV-1.5BPE) and RSV-AZPY (1:2) (RSV-2AZPY). RSV-2DPE form (II) can be transformed from RSV-2DPE form (I) during the heating process from single crystal to single crystal. The physicochemical properties of RSV cocrystals are closely related to their crystal packing modes. Also, the conformation and molecular packing of RSV among different cocrystals is flexible. The solubility of RSV-1.5BPE and RSV-2DPE form (II) exhibit higher than RSV in the buffer solution of pH 4.6 and 2.0, respectively. This study may provide a valuable insight into the crystal packing modes of cocrystals which may affect their physicochemical properties.
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http://dx.doi.org/10.1107/S2052520619013477DOI Listing
December 2019

Enantioselective [4 + 2] Cycloaddition Reaction of Vinylquinolines with Dienals Enabled by Synergistic Organocatalysis.

Org Lett 2020 08 14;22(15):6061-6066. Epub 2020 Jul 14.

State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

An unprecedented organocatalytic enantioselective [4 + 2] cycloaddition reaction of vinyl quinolines with dienals is achieved with the synergistic activation of CHSOH and a chiral aminocatalyst. The power of the process is demonstrated by its high efficiency of the production of new synthetically and biologically valued chiral quinoline architectures in high yields and with excellent enantioselectivities.
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http://dx.doi.org/10.1021/acs.orglett.0c02137DOI Listing
August 2020

[Effect of electroacupuncture on the P35/P25-cyclin-dependent kinase 5-Tau pathway in hippocampus of rats with Alzheimer's disease].

Zhen Ci Yan Jiu 2020 Mar;45(3):194-201

Department of Human Anatomy, Chongqing Medical University, Chongqing 400016, China.

Objective: To investigate the effect of electroacupuncture on the P35/P25-cyclin-dependent kinase 5 (CDK5)-Tau pathway in rats with Alzheimer's disease (AD), as well as the mechanism of electroacupuncture in the prevention and treatment of AD.

Methods: Sprague-Dawley rats were randomly divided into control group, sham-operation group, model group, and electroacupuncture treatment group, with 12 rats in each group. A rat model of AD was established by injection of Aβ into the bilateral hippocampus. The rats in the electroacupuncture treatment group were given electroacupuncture at "Baihui" (GV20) and "Shenshu" (BL23) once a day, 15 min each time, for 10 days. Morris water maze was used to evaluate learning and memory abilities, immunohistochemistry was used to measure the distribution and expression of P35/P25, CDK5, and Tau5 in the hippocampus, and Western blot was used to measure the expression of the above mentioned proteins, phosphory-lated Tau(Ser199, Ser202).

Results: In the visual platform test, there were no significant differences in escape latency and search path between groups (>0.05). In the hidden platform test, there were no significant differences in escape latency and search path between the control group and the sham-operation group (>0.05); the model group had significantly longer escape latency and search path than the control group and the sham-operation group (<0.05). Compared with the model group, the electroacupuncture treatment group had significantly shorter escape latency and search path (<0.05). In the spatial exploration test, there was no significant difference in the number of platform crossings between the control group and the sham-operation group (<0.05). The model group had a significantly lower number of platform crossings than the control group and the sham-operation group (<0.01, <0.05). The electroacupuncture treatment group had a significantly higher number of platform crossings than the model group (<0.05). Compared with the control group and the sham-operation group, the model group had significant increases in the protein expression of P35/P25 and CDK5 (<0.001), and the electroacupuncture treatment group had significant reductions compared with the model group (<0.001). There was no significant difference in the protein expression of Tau5 between groups (>0.05). The model group had significantly higher protein expression of phosphorylated Tau(Ser199, Ser202) in the hippocampus than the control group and the sham-operation group (<0.01, <0.05). The electroacupuncture treatment group had significantly lower protein expression of phosphorylated Tau(Ser199,Ser202) than the model group (<0.05, <0.01).

Conclusion: Electroacupuncture may delay the progression of AD by affecting the expression of proteins involved in the P35/P25-CDK5-Tau pathway in the hippocampus of rats.
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http://dx.doi.org/10.13702/j.1000-0607.190415DOI Listing
March 2020

Spiroalanfurantones A-D, Four Eudesmanolide-Furan Sesquiterpene Adducts with a Pentacyclic 6/6/5/5/5 Skeleton from .

Org Lett 2019 12 12;21(23):9478-9482. Epub 2019 Nov 12.

Institute of TCM and Natural Products, School of Pharmaceutical Sciences , Wuhan University , Wuhan 430071 , People's Republic of China.

Spiroalanfurantones A-D (-), four eudesmanolide-furan sesquiterpene adducts with an unprecedented pentacyclic 6/6/5/5/5 skeleton, were isolated from the roots of . Their structures were elucidated by spectroscopic data analysis and single-crystal X-ray diffraction analysis. The plausible biosynthetic pathway for - is presented. Bioassay showed that compounds and significantly inhibited nitric oxide production in lipopolysaccharide-induced RAW264.7 macrophages with IC values of 17.3 and 9.5 μM, respectively.
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http://dx.doi.org/10.1021/acs.orglett.9b03676DOI Listing
December 2019

Isostructural Solvates of Naturally Occurring Allocryptopine Exhibit Both Mechanochromic and Hydrochromic Luminescent Properties.

ACS Omega 2018 Aug 15;3(8):9220-9226. Epub 2018 Aug 15.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

We discovered four new solvates for naturally sourced allocryptopine. The new found crystalline forms are isostructural and have similar crystal structures and packing patterns. However, they exhibit obviously different fluorescence appearance. In addition, the acetone solvate SA, ,-dimethylformamide solvate SD, and tetrahydrofuran solvate ST also present both luminescent mechanochromic and hydrochromic properties.
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http://dx.doi.org/10.1021/acsomega.8b01267DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6644465PMC
August 2018

RQ3, A Natural Rebaudioside D Isomer, Was Obtained from Glucosylation of Rebaudioside A Catalyzed by the CGTase Toruzyme 3.0 L.

J Agric Food Chem 2019 Jul 1;67(28):8020-8028. Epub 2019 Jul 1.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medical , Chinese Academy of Sciences , Shanghai 201203 , China.

In this study, a monoglucosyl rebaudioside A product was isolated from the mixture of glucosylated rebaudioside A obtained from the most reported and industrial used cyclodextrin glycosyl transferase, Toruzyme 3.0 L (CGTase, Toruzyme 3.0 L). The molecular structure of the monoglucosyl rebaudioside A was characterized using LC-MS/MS and methylation analysis combined with 1D and 2D NMR, indicating that it is 13-[(2--(3-α--D-glucopyranosyl)-β-D-glucopyranosyl-3--β-D-glucopyranosyl-β-D-glucopyranosyl)oxy] -kaur-16--19-oic acid β-D-glucopyranosyl ester (also known as RQ3, which naturally exists in Stevia extract as an isomer of rebaudioside D). This study may help to further understand the reaction mechanism of glucosylation of steviol glycoside assisted by Toruzyme 3.0 L in the aspect of molecule linkage pattern, and also benefit the application of the glucosylated rebaudiosides.
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http://dx.doi.org/10.1021/acs.jafc.9b02545DOI Listing
July 2019

Anisotropic elasticity and plasticity of an organic crystal.

Chem Commun (Camb) 2019 Jul;55(59):8532-8535

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Organic crystals are generally considered to be brittle, inelastic materials, which pose challenges for application in flexible devices. Inspired by α helical proteins for their key structural role in flexible hair, here, we describe the construction of a spring-like hydrogen bonded network through the self-assembly of a-OH/e-OH cyclohexanol derivatives.
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http://dx.doi.org/10.1039/c9cc03542gDOI Listing
July 2019

Identification of an Overlooked Halogen-Bond Synthon and Its Application in Designing Fluorescent Materials.

Chemistry 2019 May 12;25(26):6584-6590. Epub 2019 Apr 12.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, P.R. China.

Research on new supramolecular synthons facilitates the progress of materials design. Herein, the ability of sp carbonyl oxygen atoms to act as halogen-bond acceptors was established through cocrystallization. Four sets of carbonyl compounds, including aldehydes, ketones, esters, and amides, were selected as halogen-bond acceptors. In the absence of strong hydrogen bonds, 14 out of 16 combinations of halogen-bond donors and acceptors could form cocrystals, whereby the supramolecular synthon C=O⋅⋅⋅X acts as the main interaction. Further, the geometric parameters of the C=O⋅⋅⋅X interaction were statistically revealed on the basis of the crystallographic database. The bifurcated interaction mode that has been observed in other halogen-bond synthons rarely occurs in the case of C=O⋅⋅⋅X. The robustness of C=O⋅⋅⋅X makes its application in crystal engineering possible and opens up new opportunities in designing multicomponent fluorescent materials, as indicated by multicolor emission of cocrystals D through C=O⋅⋅⋅X interactions.
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http://dx.doi.org/10.1002/chem.201900371DOI Listing
May 2019

Sarcomililate A, an Unusual Diterpenoid with Tricyclo[11.3.0.0]hexadecane Carbon Skeleton, and Its Potential Biogenetic Precursors from the Hainan Soft Coral Sarcophyton mililatensis.

J Org Chem 2019 03 18;84(5):2568-2576. Epub 2019 Feb 18.

State Key Laboratory of Drug Research , Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park , Shanghai 201203 , P. R. China.

A novel diterpenoid, sarcomililate A (1), possessing a previously undescribed tricyclo[11.3.0.0]hexadecane scaffold, along with two new cembranoids, sarcomililatols A and B (2 and 3), and two known related diterpenoids (4 and 5), was isolated from the Hainan soft coral Sarcophyton mililatensis. The complete chemical structure including absolute configuration (AC) of 1 was unambiguously determined by a combination of residual dipolar coupling (RDC)-based NMR analysis, TDDFT-ECD (ECD = electronic circular dichroism) calculation, and Snatzke's method. The AC of 1 was further confirmed by a comparison with 2, whose AC was determined by anomalous X-ray diffraction. A plausible biogenetic relationship of 1-3 was further proposed. All the reported compounds exhibited interesting inhibitory effects on the ConA-induced T lymphocytes and/or lipopolysaccharide (LPS)-induced B lymphocytes proliferation.
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http://dx.doi.org/10.1021/acs.joc.8b03020DOI Listing
March 2019

Disrupted-in-schizophrenia-1 protects synaptic plasticity in a transgenic mouse model of Alzheimer's disease as a mitophagy receptor.

Aging Cell 2019 02 28;18(1):e12860. Epub 2018 Nov 28.

Department of Neurosurgery, Affiliated Bayi Brain Hospital, General Army Hospital, Southern Medical University, Beijing, China.

Mitochondrial dysfunction is an early feature of Alzheimer's disease (AD). Accumulated damaged mitochondria, which are associated with impaired mitophagy, contribute to neurodegeneration in AD. We show levels of Disrupted-in-schizophrenia-1 (DISC1), which is genetically associated with psychiatric disorders and AD, decrease in the brains of AD patients and transgenic model mice and in Aβ-treated cultured cells. Disrupted-in-schizophrenia-1 contains a canonical LC3-interacting region (LIR) motif ( FSFI ), through which DISC1 directly binds to LC3-I/II. Overexpression of DISC1 enhances mitophagy through its binding to LC3, whereas knocking-down of DISC1 blocks Aβ-induced mitophagy. We further observe overexpression of DISC1, but not its mutant (muFSFI) which abolishes the interaction of DISC1 with LC3, rescues Aβ-induced mitochondrial dysfunction, loss of spines, suppressed long-term potentiation (LTP). Overexpression of DISC1 via adeno-associated virus (serotype 8, AAV8) in the hippocampus of 8-month-old APP/PS1 transgenic mice for 4 months rescues cognitive deficits, synaptic loss, and Aβ plaque accumulation, in a way dependent on the interaction of DISC1 with LC3. These results indicate that DISC1 is a novel mitophagy receptor, which protects synaptic plasticity from Aβ accumulation-induced toxicity through promoting mitophagy.
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http://dx.doi.org/10.1111/acel.12860DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6351828PMC
February 2019

Confocal Raman micro-spectral evidence and physicochemical evaluation of triamterene salts.

Analyst 2019 Jan;144(2):530-535

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, P. R. China.

Discrimination of active pharmaceutical ingredients (APIs) existing as neutral molecules or salts is essential and complicated. However, the discrimination of pharmaceutical salts by confocal Raman micro-spectroscopy remains relatively poorly understood. In this paper, four new salts of triamterene (Tri) cocrystallized with nicotinic acid (NA), benzoic acid (BA), p-toluenesulfonic acid (TA), or isonicotinic acid (INA) were prepared and characterized comprehensively by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), polarized light microscopy (PLM), and dynamic vapor sorption (DVS). Ionized pteridine is identified by marker peaks in the confocal Raman micro-spectra that are characteristic of C[double bond, length as m-dash]N. The single crystal structures of Tri-NA·H2O and Tri-TA further demonstrate that a proton transfers from the carboxylic group of NA or TA to the pyrimidine N1 atom of Tri and their salts formation take place. The intrinsic dissolution rate (IDR) and apparent equilibrium solubility of these four salts are improved compared to the pure Tri component, especially for Tri-BA. This study provides a valuable insight into pharmaceutical salt discrimination by vibrational spectroscopy and presents that the combination of Tri with an acid can be a possible and promising alternative formulation of Tri.
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http://dx.doi.org/10.1039/c8an01579aDOI Listing
January 2019

Alveolar soft-part sarcoma of the prostate: a case report and review of the literature.

Int J Clin Exp Pathol 2018 1;11(10):5126-5132. Epub 2018 Oct 1.

Department of Pathology, Affiliated Hospital of Nanjing University of Traditional Chinese Medicine Nanjing 210029, Jiangsu Province, China.

Alveolar soft-part sarcoma (ASPS) is a rare malignant soft tissue tumor of uncertain cellular origin. We reported the case of a 21-year-old man with ASPS presenting itself as a markedly vascular tumor of the prostate. Immunohistochemistry showed positive nuclear staining for TFE3, positive cytoplasm staining for MyoD1 and neuron-specific enolase, and negative for S100, CK, synaptophysin, chromogranin A, myogenin and PSA. A dual-color, break-apart fluorescence in situ hybridization (FISH) assay identified the presence of a TFE3 gene fusion in the tumor cells. RT-PCR was performed to confirm the ASPSCR1 (ASPL)/TFE3 fusion transcript product in the tumor tissue. The patient suffered bone metastases 8 months after surgery and died of cachexia 14 months later. ASPS of the prostate should be discussed in terms of differential diagnosis from clinicopathological characteristics, immunophenotypes, and molecular genetic features.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6962941PMC
October 2018

Improving Dissolution Properties by Polymers and Surfactants: A Case Study of Celastrol.

J Pharm Sci 2018 11 12;107(11):2860-2868. Epub 2018 Jul 12.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address:

Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility and wettability of both the crystalline forms were determined. It was found that surfactant can significantly improve the solubility of celastrol up to more than 10 times. Tween 80 and sodium dodecyl sulfate largely improved the wettability of the 2 crystals. Form I shows better wettability than form II in all the buffer solutions with polymers and surfactants. Compared with form II, form I exhibits higher solubility in carboxymethylcellulose and polyvinylpyrrolidone media but much lower solubility in tween 80 and sodium dodecyl sulfate solutions. An investigation of wettability and solubility mechanisms was fully explored, and a hypothesis was proposed to understand the abnormal solubility differences.
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http://dx.doi.org/10.1016/j.xphs.2018.07.008DOI Listing
November 2018

Clavuridins A and B, two new trinor-guaiane sesquiterpenes isolated from the Xisha soft coral Clavularia viridis.

Chin J Nat Med 2017 Nov;15(11):855-859

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. Electronic address:

In the present study, two new trinor-guaiane sesquiterpenes, named clavuridins B (1), and A (2), along with three known sesquiterpenes (3-5), were isolated from the Xisha soft coral Clavularia viridis. Their structures and absolute configurations were determined on the basis of spectroscopic analysis, X-ray diffraction analysis with Cu Kα radiation and by comparison with related model compounds. Compounds 1 and 3-5 were evaluated for their cytotoxic activity.
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http://dx.doi.org/10.1016/S1875-5364(18)30019-0DOI Listing
November 2017

Taming photo-induced oxidation degradation of dihydropyridine drugs through cocrystallization.

Chem Commun (Camb) 2017 Nov;53(91):12266-12269

College of Pharmacy, Nanchang University, Nanchang 330006, China.

Cocrystallization of nifedipine (NFD) and isonicotinamide (INA) resulted in two monotropic cocrystal polymorphs. The thermodynamically more stable polymorph presents superior photostability compared to the other. Cocrystallization can be an efficient approach to address the stability deficit of dihydropyridine drugs.
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http://dx.doi.org/10.1039/c7cc06992hDOI Listing
November 2017

Serum galectin-3 levels and delirium among postpartum intensive care unit women.

Brain Behav 2017 08 21;7(8):e00773. Epub 2017 Jul 21.

Department of Intensive Care Unit The Hangzhou First People's Hospital Nanjing Medical University Hangzhou China.

Objective: Inflammation correlates with delirium. Galectin-3 is a proinflammatory protein. This study aimed to determine relation of serum galectin-3 levels to delirium of postpartum intensive care unit (ICU) women.

Materials And Methods: In this prospective observational study, serum galectin-3, S100B, and C-reactive protein levels of 412 postpartum ICU women and 412 healthy women were measured. Delirium and Acute Physiology and Chronic Health Care Evaluation II (APCHCE II) scores were recorded.

Results: Serum levels of galectin-3, S100B, and C-reactive protein were significantly elevated in the postpartum women than in the healthy women. Galectin-3 levels were highly associated with APCHCE II scores and S100B and C-reactive protein levels. Galectin-3, C-reactive protein, and S100B levels and APCHCE II scores were identified as independent predictors for delirium. Area under the curve (AUC) of serum galectin-3 levels was similar to that of S100B levels, and significantly exceeded those of C-reactive protein levels and APCHCE II scores. Moreover, galectin-3 significantly improved the AUCs of APCHCE II scores, S100B levels, and C-reactive protein levels.

Conclusions: Galectin-3, involved in inflammatory process underlying delirium-related brain injury, might be a potential biomarker to predict delirium of postpartum ICU women.
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http://dx.doi.org/10.1002/brb3.773DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5561326PMC
August 2017

pH-Switchable vitamin B gels for stoichiometry-controlled spherical co-crystallization.

Chem Commun (Camb) 2016 Nov;52(92):13452-13455

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Vitamin B gels were found to be pH-switchable by adding triethylamine or acetic acid. Such recyclable gels can be used as novel co-crystallization media, resulting in four stoichiometric vitamin C co-crystals. Under highly supersaturated conditions, uniform microspheres of (VC)·(NA) with different particle sizes were obtained through a spherical crystallization process.
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http://dx.doi.org/10.1039/c6cc07701cDOI Listing
November 2016

Mechanochromism triggered fluorescent color switching among polymorphs of a natural fluorescence pigment.

Chem Commun (Camb) 2016 Sep;52(75):11288-11291

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

A naturally occurring pigment emodin is reported here as an example to extend mechanochromic luminescent material systems. Three polymorphs, two hydrates and the amorphous state of emodin, are successfully synthesized. These solid forms exhibit significantly different fluorescence properties, which indicates its potential application in mechano-sensors and security papers.
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http://dx.doi.org/10.1039/c6cc04958cDOI Listing
September 2016

Design, synthesis and biological evaluation of novel chiral oxazino-indoles as potential and selective neuroprotective agents against Aβ25-35-induced neuronal damage.

Bioorg Med Chem Lett 2016 08 3;26(15):3765-9. Epub 2016 Jun 3.

State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China. Electronic address:

A series of chiral oxazino-indoles have been synthesized via a key intermolecular oxa-Pictet-Spengler reaction. These compounds exhibited significant and selective neuroprotective effects against Aβ25-35-induced neuronal damage. This is the first report of evaluating the influence of chiral diversity of oxazino-indoles on their neuroprotective activities, with the structure-activity relationship been analyzed. The highly active compounds 3f, 3g, 4g, 4h, and 6b all performed over 90% cell protection, providing a new direction for the development of neuroprotective agents against Alzheimer's disease.
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http://dx.doi.org/10.1016/j.bmcl.2016.05.061DOI Listing
August 2016

HPIP Silencing Prevents Epithelial-Mesenchymal Transition Induced by TGF-β1 in Human Ovarian Cancer Cells.

Oncol Res 2016 ;24(1):33-9

Department of Obstetrics and Gynecology, Dongying People's Hospital, Dongying, China.

Hematopoietic pre-B-cell leukemia transcription factor (PBX)-interacting protein (HPIP/PBXIP1) is a nucleo-cytoplasmic shuttling protein, and its expression is associated with cancer aggressiveness. However, the role of HPIP in ovarian cancer is still unclear. Here, we aimed to clarify the role of HPIP in epithelial-mesenchymal transition (EMT) process of ovarian cancer cells, stimulated by transforming growth factor (TGF)-β1. In this study, we found that HPIP was highly expressed in ovarian cancer cells, and TGF-β1 treatment induced HPIP expression in ovarian cancer cells. In addition, knockdown of HPIP suppressed TGF-β1-induced EMT and migration/invasion in ovarian cancer cells. Moreover, knockdown of HPIP significantly blocked the phosphorylated pattern of both PI3K and Akt induced by TGF-β1 in SKOV3 cells. In conclusion, the present study showed that HPIP silencing might prevent TGF-β1-induced EMT in ovarian cancer cells. Thus, HPIP may be a potential therapeutic target for the treatment of ovarian cancer.
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http://dx.doi.org/10.3727/096504016X14575597858654DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7838700PMC
March 2017

Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan.

Pharm Dev Technol 2017 Feb 6;22(1):69-76. Epub 2016 Apr 6.

a Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai , China.

Co-amorphization has recently been shown to be a promising approach for stabilizing amorphous drugs and improving the dissolution rate of poorly water-soluble drugs. In this study, three basic amino acids were chosen as small molecular weight excipients to interact with the drug to form co-amorphous combinations. The co-amorphous combinations of valsartan (VAL) with l-histidine, l-arginine, and l-lysine were prepared by vibrational ball milling. Solid-state characterization with X-ray powder diffraction and differential scanning calorimetry (DSC) revealed that all of the co-amorphous mixtures were homogeneous. The molecular interactions of the co-amorphous mixtures were investigated through the glass transition temperature (T) in the DSC measurements and Fourier transform infrared spectroscopy. The drug remained chemically stable during the milling process, and the co-amorphous formulations were generally physically stable over at least 3 months at 40 °C under dry conditions. The dissolution rate of all of the co-amorphous mixtures was significantly increased over that of the amorphous VAL alone. The results of this study demonstrated the potential of amino acids as small molecular weight excipients in co-amorphous formulations to improve the drug solubility and dissolution rate.
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http://dx.doi.org/10.3109/10837450.2016.1163390DOI Listing
February 2017

Multifocal electroretinogram in non-pathological myopic subjects: correlation with optical coherence tomography.

Int J Ophthalmol 2016 18;9(2):286-91. Epub 2016 Feb 18.

Department of Ophthalmology, Second People's Hospital, Jinan 250001, Shandong Province, China.

Aim: To investigate the changes of retinal function in non-pathological myopic subjects using multifocal electroretinography (mfERG) and to correlate the data with the central macular thickness obtained using optical coherence tomography (OCT).

Methods: One hundred and thirteen subjects (113 eyes) with age range from 18 to 35y were enrolled in the study. The subjects were divided into four groups according to spherical equivalent (SE) and axial length (AL): emmetropia group (EG, n=31; SE: +0.75 to -0.50 D; AL: 22 to 24 mm), low and medium myopia group (LMMG, n=26; SE: >-0.50 to -6.00 D; AL: >24 to 26 mm), high myopia group (HMG, n=34; SE: >-6.00 to -10.00 D; AL: >26 to 28 mm) and super high myopia group (SHMG, n=22; SE: >-10.00 D; AL:>28 mm). The P1 amplitude density, P1 amplitude, and P1 implicit time of the first-order kernel mfERG responses were obtained and grouped into five rings. The central subfield macular thickness (CST) was obtained using macular cube 512×218 scan of Cirrus HD-OCT.

Results: With the increasing of eccentricity, the first positive peak (P1) amplitude density (P=0.0000, 0.0001, 0.0021 in ring 1-3 respectively) and P1 amplitude (all P=0.0000 in ring 1-5) of each group decreased. With the increasing of myopia, P1 implicit time gradually extended (all P=0.0000 in ring 1-3). The average CST in four diagnostic groups was 241.56±12.72 µm, 244.56±12.19 µm, 254.33±11.61 µm, 261.75±11.83 µm respectively. With the increasing of myopia, CST increased (P<0.001). There was negative relationship between CST and P1 amplitude, P1 amplitude density (r=-0.402, P<0.001; r=-0.261, P=0.003). There was positive relationship between CST and P1 implicit time (r=0.34, P<0.001).

Conclusion: With the increasing of myopia, P1 amplitude density and P1 amplitude of the first-order reaction gradually reduced. This showed potential decline in retinal function in myopia. To some extent it may reflect the functional disorder or depression of the visual cells. The exact mechanism needs further study.
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http://dx.doi.org/10.18240/ijo.2016.02.21DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4761745PMC
March 2016

Drug-drug co-crystallization presents a new opportunity for the development of stable vitamins.

Chem Commun (Camb) 2016 Feb 4;52(17):3572-5. Epub 2016 Feb 4.

Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

Drug-drug co-crystallization could realize combination drugs at a molecular level. Two polymorphic co-crystals between VD2 and VD3 were successfully designed and synthesized. These enantiotropic polymorphs exhibit significantly different physicochemical stabilities.
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http://dx.doi.org/10.1039/c5cc10297aDOI Listing
February 2016
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