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Morphometric study on Leydig cells in capsulotomized testis of rats

Asian Journal of Andrology 2002年第1期4卷 49-53页

作者： QinDN lungma DepartmentofPhysiology ShantouUniversitySchoolofMedicineShantou515031Ching DepartmentofPhysiology UniversityofHongKongKHSARChina

AIM: To further clarify the changes occurred in the testicular capsulotomized rats. METHODS: In testicular capsulotomized and sham-operated rats, the cross sectional area, the nucleus diameter and the number of Leydig cells were morphologically analyzed by the Vidas Image Processing System connected to a microscope. RESULTS: In the capsulotomized animals, the cross sectional area of Leydig cells was gradually increased from 30 days onwards. There was no obvious change in the nucleus diameter of Leydig cells. However, The Leydig cell number was significantly increased from day 30 onwards. CONCLUSION: In rats, testicular capsulotomy may induce hyperplasia/hypertrophy of Leydig cells in the testis.

关键词： Animals Cell Count Cell Nucleus Image Processing, Computer-Assisted Leydig Cells Male Rats Rats, Sprague-Dawley Testis

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Pharmacophore modeling for the identification of small-molecule inhibitors of TACE

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中国药理学与毒理学杂志 2015年第S1期29卷 95-96页

作者： Li-juanLIU Ka-HoLEUNG ShengLIN DanielShiu-HinCHAN DewiSUSANTI Wei-dongRAO PhilipWaiHongCHAN Dik-lungma Chung-HangLEUNG State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical Sciences University of Macao Macao China Department of Chemistry Hong Kong Baptist University Hongkong China Division of Chemistry and Biological Chemistry School of Physical and Mathematical Sciences Nanyang Technological University Singapore 637371 Singapore School of Chemistry Monash University Ciayton 3800 Victoria Australiate

OBJECTIVE To employ pharmacophore modeling to identify a TACE inhibitor from an inhouse database of 66 organic *** To identify the common features required for TACE inhibition,we generated a pharmacophore model from a set of TACE-selective inhibitor using the Common Feature Pharmacophore Model protocol implemented in Discovery Studio 3.1.1.A fluorimetric assay was used to investigate the potential ability of compounds to inhibit TACE enzymatic *** ability of compound 1 to inhibit TACE activity in a human monocyte THP-1 cell line was evaluated by *** In this study,apharmacophore model constructed from a training set of TACE inhibitors was used to screen an in-house database of organic compounds,from which compound 1 emerged as a top *** a cell-free assay,compound 1inhibited TACE enzymatic activity in a dose-dependent ***,compound 1 inhibited the production of soluble TNF-αin human acute monocytic leukemia THP-1 cells without impacting nitric oxide production,and exhibited anti-proliferative activity against *** Compound 1 was found to inhibit TACE enzymatic activity in a cell-free system and LPS-induced TNF-αsecretion in *** envisage that compound 1 may be employed as a useful scaffold for the development of more potent TACE inhibitors.

关键词： pharmacophore TACE tumor necrosis factor virtual s

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Virtual screening and optimization of typeⅡ inhibitors of JAK2 from a natural product library

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中国药理学与毒理学杂志 2015年第S1期29卷 98-99页

作者： Dik-lungma DanielShiu-HinCHAN GuoWEI Hai-jingZHONG HuiYANG LaiToLEUNG ElizabethA.GULLEN PaulineChIU Yung-ChiCHENG Chung-hangLEUNG Department of Chemistry Hong Kong Baptist University Hong Kong China Department of Chemistry and the State Key Laboratory of Synthetic Chemistry University of Hong Kong Hong Kong China State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical Sciences University of Macao Macao China Department of Pharmacology Yale University School of Medicine New Haven CT 06520 USA

OBJECTIVE To utilize a structure-based lead optimization approach to generate novel natural product-like typeⅡ inhibitors of JAK2 using the DOLPHIN *** Initially,the DOLHPIN computational protocol was employed to convert an active(DFG-in)conformation of JAK2 into a typeⅡ-compatible conformation,which was used as a model for the structure-based virtual screening of 150 000 natural product-like compounds in *** novel biflavonoid analogues were designed and synthesized based on the structure of lead compound and then tested for JAK2 and STAT3 inhibitory activity,cytotoxicity and HCV antiviral *** The top eleven highest-scoring compounds were generated from the initial high-throughput virtual *** 1a,a biflavonoid from the Chinese plant Gingko biloba,emerged as a promising candidate for further biological *** dose-response experiments,amentoflavone 1ainhibited JAK2 activity in a concentration dependent fashion with an IC50 value of 5μmol·*** a proof-of-concept,we designed nine analogues 1b-1j with the addition of one or more aliphatic side chains to the biflavonoid scaffold of *** octyl(C8)analogue 1bdisplayed superior potency against JAK2 activity and HCV activity compared to the parent compound 1a,validating the structure-based lead optimization approach used in this ***,kinetic analysis indicated that analogue 1bexhibited a non-competitive mode of inhibition,suggesting that this compound may be a putative typeⅡ inhibitor of *** Amentoflavone 1ahas been identified as a JAK2 inhibitor by structure-based virtual screening of a natural product *** silico optimization using the DOLPHIN model yielded analogues with enhanced potency against JAK2 activity and HCV activity in *** modeling and kinetic experiments suggested that the analogues may function as typeⅡ inhibitors of JAK2.

关键词： JAK2 natural products virtual screening structure-

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Identification of a natural product-like STAT3 dimerization inhibitor by structure-based virtual screening

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中国药理学与毒理学杂志 2015年第S1期29卷 95-95页

作者： Li-juanLIU Ka-HoLEUNG DanielShiu-HinCHAN Dik-lungma Chung-HangLEUNG State Key Laboratory of Quality Research in Chinese Medicine University of Macao Macao SAR China Department of Chemistry Hong Kong Baptist University Kowloon Tong Hong Kong China

OBJECTIVE To apply molecular docking techniques to identify STAT3 inhibitors from a database of over 90 000 natural product and natural product-like *** Molecular docking was used for the virtual screening campaign and hit validation of STAT3 *** further evaluate the potency of candidates at inhibiting STAT3-DNA binding activity,a STAT3 and STAT1transcription factor ELISA was performed.A dual-luciferase reporter assay,co-immunoprecipitation assay and Western blotting were carried out for the investigation of effect of compound 1 on STAT3-driven transcription,STAT3 dimerization and STAT3 ***,the cell toxicity of compound 1 was assessed by using MTT assay on different cell *** The virtual screening campaign furnished fourteen hit compounds,from which compound 1 emerged as a top *** 1inhibited STAT3DNA-binding activity in vitro and attenuated STAT3-directed transcription in cellulo with selectivity over STAT1 and comparable potency to the wellknown STAT3 inhibitor ***,compound 1 inhibited STAT3 dimerization and decreased STAT3 phosphorylation in cells without affecting STAT1 dimerization and *** 1 also exhibited selective anti-proliferative activity against cancer cells over normal cells in *** The benzofuran derivative 1 was identified as a potential inhibitor of STAT3 dimerization using in silico *** docking analysis suggested that compound 1 might putatively function as an inhibitor of STAT3 dimerization by binding to the SH2 *** the best of our knowledge,compound 1 has not been reported as a STAT3 inhibitor and no biological activity of compound 1 has been presented in the literature.

关键词： STAT3 natural products virtual screening dimerizat

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