生地黄中环烯醚萜苷类的纯化分离工艺

目的:寻找有效纯化分离生地黄中环烯醚萜苷类的方法.方法:生地黄水提物用高效液相色谱法,以梓醇为其环烯醚萜苷类的测定指标,比较101 果汁澄清剂和科阳1＋1天然澄清剂的纯化效果,以及乙醇和非极性大孔吸附树脂的分离效果.结果:生地黄水提物以科阳1＋1天然澄清剂纯化,用非极性大孔吸附树脂分离,可使其中的环烯醚萜苷类有效分离出来.结论:在工业生产中可用科阳1＋1天然澄清剂与非极性大孔吸附树脂联合应用来纯化分离生地黄中的环烯醚萜苷类.     

Further flavonol and iridoid glycosides from Ajuga remota aerial parts

Five new iridoid glycosides characterised as 6-keto-8-acetylharpagide (1), 6,7-dehydro-8-acetylharpagide (2), 7,8-dehydroharpagide (3), 8-acetylharpagide-6-O-β-glucoside (4), harpagide-6-O-β-glucoside (5) together with three flavonol glycosides, myricetin 3-O-rutinoside-4'-O-rutinoside (6), myricetin 3-O-rutinoside-3'-O-rutinoside (7) and isorhamnetin 3-O-rutinoside-7-O-rutinoside-4'-O-β-glucoside (8) have been isolated from the aerial parts of Ajuga remota. Also isolated were two known compounds ajugarin IV and ajugarin V. Their structures were established using spectroscopic methods including UV, IR, FAB-MS, HR-MS, 1D and 2D NMR techniques.     

中药糖肾方单体成分莫诺苷药理作用的研究进展

通过查阅近些年的国内外文献对中药糖肾方单体成分莫诺苷的药理作用及分子机制进行归纳、梳理、分析及总结。从分子机制角度阐述莫诺苷具有促进细胞生长、减轻炎性反应、抑制细胞内钙超载、抑制氧化应激、抗凋亡、抗凝等作用,以便为今后临床及实验研究提供更多科学依据。     

Protective effects of iridoid glycosides on acute colitis via inhibition of the inflammatory response mediated by the STAT3/NF-кB pathway

Morroniside and loganin are iridoid glycosides extracted from Cornus officinalis, a plant species widely used in traditional Chinese medicine. However, the anti-inflammatory effects of morroniside and loganin in colitis are barely understood. The aim of the present study was to explore the effects of morroniside and loganin on the dextran sodium sulfate (DSS)-induced murine model of colitis and an LPS-induced colorectal cancer (CRC) cell inflammation model, and to clarify the underlying mechanisms. We found that morroniside and loganin were able to ameliorate clinical features, including disease activity index (DAI), histological inflammation score and periodic acid-Schiff staining (PAS). In the mouse model, morroniside and loganin treatment increased expression of tight junction proteins (TJs) and decreased pro-inflammatory cytokine production. Moreover, our findings showed that the expression of p-STAT3 and p-p65 were suppressed compared to the disease group. In in vitro experiments, treatment with morroniside and loganin had no obvious effects on proliferative activity in HCT116 cells and HIEC-6 cells. Expression of pro-inflammatory cytokines was inhibited by morroniside and loganin treatment in comparison with the LPS-treated group. Taken together, morroniside and loganin have beneficial effects on colitis in vivo and are anti-inflammatory in vitro. Possible mechanisms of the anti-inflammatory response may include blockade of the STAT3/NF-κB pathway.     

Iridoid glycosides extracted from Zhizi (Fructus Gardeniae) decrease collagen-induced platelet aggregation and reduce carotid artery thrombosis in an in vivo rat model

Objective

To investigate the anti-platelet aggregation and antithrombotic effects in rats of iridoid glycosides extracted from Zhizi (Fructus Gardeniae).

Methods

The present study evaluated the antithrombotic activity of iridoid glycosides (IGs) in a rat model of carotid artery thrombosis. The effects on coagulation, such as thromboplastin time (APTT), thrombin time (TT) and prothrombin time (PT), and the effect on collagen-induced platelet aggregation in vivo were investigated. Rats were intragastrically administered IGs (50, 100 or 200 mg/kg) twice daily for 3 days.

Results

IGs were shown for the first time to have an antithrombotic action through the inhibition of platelet aggregation, with little effect on the coagulation time of peripheral blood. Our results also showed that IGs may significantly and dose-dependently reduce arterial thrombus load in a model of carotid artery thrombosis and inhibit collagen-induced platelet aggregation in rats. IGs (100 or 200 mg/kg) had no significant effect on APTT and PT, but did lengthen TT at a higher dose.

Conclusion

These data, together with the previously reported neuroprotective effects of IGs in rats with cerebral ischemia, suggest that the antithrombotic action of IGs may potentially contribute to the treatment of cerebral ischemic diseases, including cerebral apoplexy.     

Iridoid glucosides from Wendlandia ligustroides (Boiss. &Hohen.) Blakelock

Eight iridoid glucosides were reported from the aerial parts of Wendlandia ligustroides. 10-deoxygeniposidic acid (1), 7-deoxygardoside (2), geniposidic acid (3), 7-deoxy-8-epi-loganic acid (4), deacetyl-daphylloside (5), scandoside methyl ester (6), 6-O-methyl-deacetyl-daphylloside (7), 6-O-methyl-scandoside methyl ester (8). Compounds 3 – 8 were isolated as a pure form while 1 and 2 as a mixture. The structures of the compounds 1 – 8 were established by spectroscopic methods including 1D-NMR (¹H NMR, ¹³C NMR, DEPT-135), 2D-NMR (COSY, NOESY, HSQC, HMBC) and HRMS.     

A new iridoid and other chemical constituents from<Emphasis Type="Italic">pedicularis kansuensis</Emphasis> forma<Emphasis Type="Italic">albiflora</Emphasis> Li.

A new iridoid (1) and thirteen known compounds 2-14 were isolated from Pedicularis kansuensis forma albiflora Li., and their structures were elucidated by spectroscopic methods including 2D-NMR techniques.     

山茱萸环烯醚萜苷对冈田酸拟阿尔茨海默病细胞模型的抗凋亡作用研究

目的:研究山茱萸环烯醚萜苷(CIG)对蛋白磷酸酶抑制剂冈田酸(OA)拟阿尔茨海默病(AD)细胞模型中神经细胞凋亡的影响及其作用机制。方法:CIG与人神经母细胞瘤细胞系SK-N-SH细胞预孵育24h,再用OA10nmol与神经细胞共孵育6h,用TUNEL法观察凋亡细胞的变化,用蛋白免疫印记法观察凋亡因子B细胞淋巴瘤(Bcl-2)、Bcl-2相关X蛋白(Bax)和细胞凋亡蛋白酶(Caspase-3)的表达。结果:正常对照细胞铺展良好,未出现凋亡细胞;OA模型组凋亡细胞显著增多,Bax和Cas-pase-3的表达水平显著增高,Bcl-2的表达水平显著下降;CIG(100和200μg.mL-1)给药组凋亡细胞较OA模型组显著减少,Bax和Caspase-3表达水平显著降低,Bcl-2表达显著增高。结论:CIG能通过影响凋亡调节因子而抑制神经细胞凋亡,提示该药可能具有治疗AD的良好应用前景。     

山莱萸环烯醚萜总苷对糖尿病血管并发症大鼠血清糖基化终产物-肽（AGE-P）水平的影响

探讨环烯醚萜总苷对糖尿病血管并发症大鼠血清糖基化终产物-肽(AGE-P)水平的影响。方法:在正常进食条件下,大鼠先以30mg·kg~(-1)ip。链脲佐菌素(STZ)溶液,第二天再按0.11ml/只ip。弗氏完全性剂(FCA),每周1次,连续3周。3周后测定大鼠血糖,若血糖≥16.7mol.L~(-1)者则纳入为糖尿病大鼠,并按血糖值范围随机分为模型组、氨基胍组(0.1g·kg~(-1))和环烯醚萜总苷组(0.25、0.5g·kg~(-1)),正常组,各组连续ig.12周。实验结束后运用流动注射分析法(FIA,flow injection assay)检测血清AGE-P含量。结果:模型组血清AGE-P水平显著增加(14.3±4.3vs2.8±0.4,P<0.01),而环烯醚萜总苷及氨基胍组均能降低血清AGE-P水平,与模型组比较有显著性差异(P<0.05)。结论:环烯醚萜总苷能降低糖尿病血管并发症大鼠血清AGE-P水平,具有减轻糖尿病血管并发症的作用。