Triterpenoid saponins, new metalloprotease snake venom inhibitors isolated from Pentaclethra macroloba.

We report here the antiproteolytic and antihemorrhagic properties of triterpenoid saponin inhibitors, named macrolobin-A and B, from Pentaclethra macroloba, against Bothrops snake venoms. The inhibitors were able to neutralize the hemorrhagic, fibrin(ogen)olytic, and proteolytic activities of class P-I and P-III metalloproteases isolated from B. neuwiedi and B. jararacussu venoms. Clotting and fibrinogenolytic activities induced by snake venoms and isolated thrombin-like enzymes were partially inhibited. Furthermore, the potential use of these inhibitors to complement antivenom therapy as an alternative treatment and/or used as molecular models for development of new therapeutical agents in the treatment of snake bite envenomations needs to be evaluated in future studies.     

西洋参茎叶皂甙单体Rb_3对大鼠血流动力学及单钙通道活动的影响

单体皂甙Ｒｂ３自西洋参茎叶皂甙中提取。Ｒｂ３３０ｍｇ·ｋｇ－１可使麻醉大鼠在体心脏的ＭＡＰ，±ｄＰ／ｄｔｍａｘ和ＬＶＳＰ减少。用斑片钳的连细胞电压钳法证明．Ｒｂ３３００ｍｇ·Ｌ－１使Ｌ、Ｂ、Ｔ型钙通道的开放时间缩短、开放概率减少，其作用与异搏定３７．５ｍｇ·Ｌ－１相似，与ＢａｙＫ８６１１５μｍｏｌ·Ｌ－１作用相反。确切地证明Ｒｂ３对钙通道有阻滞作用。     

黑柴胡中新三萜皂甙的结构鉴定

从黑柴胡(Bupleurum smithii Wolff)根中分离出10个化合物,均为首次由该植物中获得。其中二个新三萜皂甙,即柴胡皂甙k和l(saikosaponin k and l),其结构经紫外、红外、核磁共振氢谱,碳谱和质谱等波谱测定和解析,分别确定为3β,16β,23,28-四羟基齐墩果烷-11,13(18)-二烯-3-O-β-D-吡喃木糖基-(1→2)-β-D-吡喃葡萄糖基-(1→3)-β-D-吡喃呋糖甙和3β,16α,23,28,30-五羟基齐墩果烷-11,13(18)-二烯-3-O-β-D-吡喃葡萄糖基-(1→3)-β-D-吡喃呋糖甙。     

岗梅全长转录组测序及其三萜皂苷生物合成相关基因的挖掘

目的:获得岗梅全长转录组数据库,为深入挖掘岗梅功能基因奠定基础。方法:采用基于PacBio Sequel平台的单分子实时测序技术获取岗梅的根、茎、叶样品的转录组数据,并利用非冗余蛋白(NR)、核苷酸序列(NT)、SwissProt蛋白序列数据库、京都基因与基因组百科全书(KEGG)、真核生物相邻类的聚簇(KOG)、蛋白家族(Pfam)、基因本体(GO)进行注释,分析并鉴定编码三萜皂苷生物合成的关键酶的转录本。结果:全长转录组共获得89629个转录本,其中81313个在公共数据库进行了注释。KEEG代谢通路富集分析表明,623个转录本参与岗梅中三萜皂苷合成相关的3条代谢通路,其中263个转录本编码了三萜皂苷生物合成途径的21个关键酶。此外,还预测了2471个转录因子、40421个简单重复序列位点、22119个长链非编码RNA(lncRNA)和29131个mRNA。结论:丰富了岗梅的转录组数据,并为鉴定参与三萜皂苷和其他次生代谢物生物合成的候选基因提供参考,促进其分子生物学和基因组学的研究。     

痹祺胶囊治疗类风湿性关节炎的药效研究及网络机制预测

目的 基于Ⅱ型胶原诱导的类风湿性关节炎（rheumatoid arthritis,RA）大鼠模型和网络药理学方法探讨痹祺胶囊的药效作用及作用机制。方法 SD大鼠采用Ⅱ型胶原蛋白造模,造模成功大鼠随机分为模型组,痹祺胶囊（0.05、0.10、0.20、0.40 g/kg）组及泼尼松（10 mg/kg）组和雷公藤总苷（10 mg/kg）组,连续给药15 d。持续监测大鼠体质量、足趾肿胀度和关节炎评分,苏木素-伊红染色考察大鼠踝关节病理变化,ELISA法测定血清细胞因子含量,初步评价痹祺胶囊治疗效果。选择痹祺胶囊中39个化合物为研究对象,依据反向药效团匹配方法和TCMSP、Uniprot等数据库预测化合物作用靶点,与通过OMIM、Dis Ge Net等数据库收集的RA相关靶点相互交互,将交互靶点借助Omicsbean、STRING等数据库平台对获得靶点进行基因本体功能和京都基因与基因组百科全书（Kyoto encyclopedia of genes and genomes,KEGG）通路富集分析,利用Cytoscape软件构建“药材-化合物-靶点-通路-功效-疾病”网络,预测其可能的作用机制...     

HPLC-ELSD法测定湖北麦冬中主要皂苷的含量

采用蒸发光散射检测器（ＥＬＳＤ）测定了湖北麦冬中山麦冬皂苷Ｂ的含量,结果表明,ＥＬＳＤ是皂苷类化合物较为适宜的检测器。经对不同采收期样品的含量考察,认为湖北麦冬的最佳采收期与传统采收期（清明）相一致。     

人参二醇皂甙对小鼠急性脑缺血损伤的保护作用

目的：探讨人参二醇皂甙（PDS）对小鼠急性脑缺血损伤的影响。方法：部分结扎带迷走神经的颈总动脉制备急性脑缺血模型,记录6h内的卒中指数,12h内的死亡率。于缺血90min时断头取脑,测定脑组织中乳酸（LA）、乳酸脱氢酶（LDH）、丙二醛（MDA）及超氧化物歧化酶（SOD）含量。结果：PDS缺血前30min ip能降低卒中指数,减少死亡率,PDS尚能降低缺血脑组织中LA和MDA含量,提高LDH和SOD活性。结论：PDS对小鼠急性脑缺血损伤具有保护作用,其作用机制与减轻组织酸中毒,抑制脂质过氧化损伤有关。     

Ginsenoside Rs3, a genuine dammarane-glycoside from Korean red ginseng

A genuine dammarane-glycoside, named as ginsenoside Rs₃, was isolated from the MeOH extracts of Korean red ginseng (Panax ginseng C.A. Meyer) through repeated silica gel column chromatographies and its chemical structure was determined as (20S)-protopanaxadiol 3-O-[6″-O-acetyl-β-D-glucopyranosyl (1→2)-β-D-glucopyranoside on the basis of several spectral and physical evidences including HMBC and FAB-MS.     

倒卵叶五加总皂苷对心肌缺血再灌注大鼠左心功能和血清一氧化氮及血浆内皮素的影响

目的　观察倒卵叶五加总皂苷对心肌缺血再灌注大鼠左心功能和血清一氧化氮 (NO)及血浆内皮素 (ET)的影响。方法　建立在体大鼠缺血再灌注损伤模型 ,用心功能分析系统测定左室心功能 ,用酶法测定血清NO水平及放免法测定血浆ET水平。实验分假手术组 (sham)、心肌缺血再灌注损伤组 (IR)和倒卵叶五加总皂苷 (SAOH ,10 0mg·Kg-1)治疗组。结果　IR组左室LVSP ,+dp/dtmax,-dp/dtmax,+dp/dtmax/IP明显下降 (P <0 .0 0 1) ,血清NO水平明显降低 ,而血浆ET水平则显著升高(P <0 .0 0 1) ;SAOH能够明显改善缺血再灌注损伤大鼠左心LVSP ,+dp/dtmax,-dp/dtmax,+dp/dtmax/IP ,提高血清NO ,降低血浆ET ,恢复NO/ET平衡 (P <0 .0 0 1)。结论　倒卵叶五加总皂苷能提高心肌缺血再灌注损伤大鼠血清NO水平和降低血浆ET含量 ,恢复NO/ET平衡 ,改善左心舒缩功能。     

Assignments of ^1H and ^13C NMR Signals of Mogroside IVa

Aim To investigate the structure of mogroside IVa isolated from traditional Chinese medicine fructus momordicae [fruits of Siraitia grosvenori (Swingle) C. Jeffery] and summarize the NMR characteristics of the structure. Methods Cormnon extraction, separafion and purification methods were used. Various NMR techniques including ^1H NMR,^13C NMR, DEPT, ^1H-^1H COSY, HSQC, HMBC, NOESY and molecular model simulated by comtmter were used to elucidate the structure. Results ^1H and ^13C NMR signals of mogroside IVa were assigned, and spectroscopic basis was obtained for identification of such type of compounds. Conclusion 1D and 2D NMR techniques including ^1H-^1H COSY, HSQC, HMBC, NOESY spectra are powerful tools for structure analysis. The structure determined by NMR methods is identical with energy minimized conformation simulated by computer.