山银花化学成分与其生物活性的研究进展（英文）

山银花作为中国传统中药,在中国有数千年历史。目前,山银花在湖南省有广泛栽培,主要作为清热药和消毒药应用。山银花主要包括咖啡酸衍生物、挥发油、黄酮类化合物、环烯醚萜苷和萜类化合物,主要有抗炎、抗肿瘤、抗氧化、抗过敏、免疫调节及抗菌活性等。本文通过查阅相关文献,对山银花的化学成分及其生物活性进行了全面的系统总结。

南五味子属植物三萜类化合物及其药理作用研究进展（英文）

五味子科南五味子属植物在民间治疗类风湿性关节炎和胃肠疾病具有悠久历史,研究表明其主要活性成分为木脂素和三萜类化合物。三萜类化合物是五味子科五味子属和南五味子属植物的主要差异性化学成分。本文对近三十年(1987-2017年)南五味子属植物中的214种三萜类化合物的结构分类及其药理活性的研究进展进行了系统综述,以期为进一步的研究提供理论参考。

槟榔子中抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分(英文)

目的:研究槟榔子(Areca catechu)粗提取物中所含的抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分及其作用机制。方法:使用70%甲醇水溶液对槟榔子进行粗提取。使用生物发光血小板凝集仪在富血小板血浆中测定槟榔子粗提取物的抗血小板聚集作用,使用分光光度计在试管内测定槟榔子粗提取物对乙酰胆碱酯酶活性的抑制作用。检测槟榔子中的多种化合物以测定槟榔子中抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分。结果:槟榔子粗提取物能够抑制花生四烯酸、二磷酸腺苷、血小板活化因子、肾上腺素及钙离子载体引起的血小板聚集,尤其对二磷酸腺苷及钙离子载体引起的血小板聚集的抑制最为明显;槟榔子粗提取物能够显著抑制乙酰胆碱酯酶的活性。在所检测的槟榔子所含化合物中,只有儿茶素对肾上腺素引起的血小板聚集有显著的抑制作用,而这种抑制作用显著弱于槟榔子粗提取物,提示槟榔子中的其他成分参与了这种抑制作用;鞣酸、没食子酸、薯蓣皂苷元和异去甲槟榔次碱能够抑制乙酰胆碱酯酶的活性,其中鞣酸的抑制作用强于槟榔子粗提取物。结论:槟榔子中含有抗血小板聚集及抑制乙酰胆碱酯酶活性的有效成分,而发挥这些功效的确切成分有待进一步的研究证实。

<i>Fusarium lini</i>Potential for the Biotransformation of Norandrostenedione and Evaluation of Urease and Chymotrypsin Properties of the Transformed Products

Several androgenic steroids have been biotransformed by fungi into metabolites with numerous biological properties. Incubation of norandrostenedione (1) with Fusarium lini NRRL 2204 was carried out for the first time, yielding two new metabolites, 3,7β-dihydroxy-19-norandrost-1,3,5-trien-17-one (3) and 6α,10β,17β-trihydroxy-19-nor-4-androsten-3-one (4), along with three known compounds, 3-hydroxy-19-norandrost-1,3,5-trien-17-one (2), 10β, 17β-dihydroxy-19-nor-4-androsten-3-one (5) and 10β-hydroxy-19-nor-4- androsten-3,17-dione (6). Their structures were elucidated by extensive spectroscopic analyses, including 1D-, 2D-NMR, and HR-MS experiments. Substrate 1 and its derivatives 2-6 were evaluated in vitro for their urease and chymotrypsin inhibitory properties. Compounds 2 and 3 were found to have strong urease activity with IC50 = 23.7 ± 0.17 and 10.2 ± 0.28 μm, respectively, as compared to the standard drug thiourea (IC50 = 21.6 ± 0.12 μm). Compounds 4, 5 and 6 showed good chymotrypsin activity with IC50 values of 6.4 ± 0.19, 15.6 ± 0.46 and 18.4 ± 0.65 μm, respectively, as compared to standard chymostatin with IC50 = 5.7 ± 0.14 μm. These transformed metabolites may form the basis for the future development of new drugs against ulcer, inflammation, bacterial and viral diseases.

Kadsura coccinea:A rich source of structurally diverse and biologically important compounds

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family.It has been used in traditional Chinese medicine(TCM)for the treatment of rheumatoid arthritis and gastroenteric disorders.The initial phytochemical work focused on the identification of some structurally novel and diverse natural products,which turned the attention of many researchers towards this plant.Thus far,202 compounds have been reported in this plant.Lignans and terpenoids were found as the main chemical constituents of this plant.Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers.The isolated compounds of this plant have shown different bioactivities including anti-tumor,anti-HIV,anti-inflammatory,nitric oxide(NO)production inhibitory and other pharmacological effects.This review systematically summarizes all the phytochemical and pharmacological work done so far on K.coccinea,and can be used as a reference for future research on this plant.

Tsc1/Tsc2 complex: A molecular target of capsaicin for protection against testicular torsion induced injury in rats

Objective: The detailed knowledge about protective effects of capsaicin(cap) and involved mechanisms against testicular torsion(TT) is still not available completely.Methods: Male Wistar rats were assigned into four major cohorts:(i) sham,(ii) TT,(iii) three subgroups subjected to TT and different doses of cap(100, 500, and 1000 μg/mL), and(iv) three subgroups of healthy animals subjected to various concentrations of cap. The animals were decapitated at 24 h after reperfusion, and the evaluation of protein expression was performed by Western blotting assay. At 72 h after reperfusion, apoptotic cell death and tissue injury were evaluated by TUNEL nuclear and H&E staining,respectively.Results: The results showed that cap administration following TT significantly increased the expression of tuberous sclerosis proteins 1 and 2(Tsc1/Tsc2) in a dose-dependent manner(P < 0.05). Cap decreased cell apoptosis at highest dose. Likewise, cap contributed to the preservation of tubular morphology and decreased tissue injury at the highest tested concentration(1000 μg/m L).Conclusion: Collectively, our findings demonstrate the validity of cap as a therapeutic agent against TT through targeting Tsc1/Tsc2 in a dose-dependent manner.

Structural basis of AimP signaling molecule recognition by AimR in Spbeta group of bacteriophages

Dear Editor,Quorum sensing(QS)is a widespread phenomenon in bacteria which enables them to participate in cell-to-cell communication by producing and responding to small signal molecules,thus synchronously altering their behavior depending on population density(Singh et al.,2000;Miller and Bassler,2001).Through QS,bacteria coordinate processes such as expression of virulenee factors(Slamti and Lereclus,2002),biofilm formation(Parashar et al.,2011),sporulation(Perego et al.,1996),conjugation(Kozlowicz et al.,2006),antibiotic synthesis(Miller and Bassler,2001;Whiteley et al.,2017)etc.

Anti-diabetic related health food properties of traditional rice(Oryza sativa L.)in Sri Lanka

Objective:To evaluate a range of anti-diabetic related properties and some consumer preferred physicochemical properties of selected Sri Lankan traditional rice varieties.Methods:Sudu Heeneti,Goda Heeneti,Masuran and Dik Wee varieties were used in this study.Anti-diabetic related properties of bran extracts of selected varieties were studied for methylglyoxal mediated protein glycation inhibition,acetyl and butyryl-cholinesterase inhibition in vitro and anti-hyperglycemic activity in vivo.Further,selected varieties were studied for starch hydrolysis rate in vitro.Physicochemical properties including grain color,size,shape,crude protein,crude fat,ash,dietary fiber and total carbohydrate contents were studied.Results:Brans of selected varieties had significant(P<0.05)and dose dependent methylglyoxal mediated protein glycation inhibition[IC_(50):(174.77±6.65)to(342.87±0.43)μg/mL]and acetyl[IC_(50):(37.00±0.68)to(291.00±3.54)μg/mL]and butyryl-cholinesterase[IC_(50):(18.50±0.60)to(96.60±0.56)μg/mL]inhibitory activities.Further,Sudu Heeneti,Masuran and Dik Wee had low starch digestion rate(52.40±1.44 to 53.76±1.19)indicating that these varieties may be low glycemic index rices.Brans of Masuran tested in rat model showed anti-hyperglycemic activity.Physicochemical properties studied showed that selected varieties were red in color and grain size and shape were mostly medium and bold respectively.Moisture,crude protein,crude fat,ash and total carbohydrate contents varied significantly(P<0.05)among the varieties.Conclusions:It is concluded that selected varieties could be promoted as physicochemically sound rices with a range of anti-diabetic related properties in the management of diabetes and its complications.

Pd(II)and Rh(III)Complexes with Isoquinoline Derivatives Induced Mitochondria-Mediated Apoptotic and Autophagic Cell Death in HepG2 Cells

Nonplatinummetal complexes of[Pd(L^(1))Cl_(2)](C1),[Rh(L^(1))Cl_(3)(DMSO)](C2),[Pd(L^(2))Cl_(2)](C3),and[Rh(L^(3))Cl_(3)(DMSO)](C4)with isoquinoline derivatives have been prepared and characterized.C1-C4 exhibited higher in vitro anticancer activity and lower toxicity than the corresponding ligands and cisplatin against HepG2 cells.The mechanistic studies revealed that C1 arrested the cell cycle at S-phase by regulation of cyclin and cyclin-dependent kinases.C1 was accumulated in mitochondria,which increased the generation of reactive oxygen species(ROS)and endoplasmic reticulum(ER)-stress response through mitochondrial dysfunction.Moreover,C1 stimulated Ca^(2+)release,activated the caspase cascade,and triggered mitochondria-mediated apoptosis.The in vivo studies of C1 demonstrated higher safety than cisplatin and effective tumor growth inhibition.C1 is a potential anticancer drug candidate.