Diterpenoids from the Roots of Agastache rugosa

从土藿香根中得到两个二萜化合物，藿香酚（２）及异藿香酚（３）。经光谱解析（ＩＲ，ＵＶ，ＨＲＭＳ及ＮＭＲ谱），确定它们的结构分别为１１，１４ｄｉｈｙｄｒｏｘｙ１２ｍｅｔｈｏｘｙ１９（４→３）ａｂｅｏａｂｉｅｔａ４，（１８），８，１１，１３ｔｅｔｒａｅｎ７ｏｎｅ（２）和１１，１４ｄｉｈｙｄｒｏｘｙ１２ｍｅｔｈｏｘｙ１９（４→３）ａｂｅｏａｂｉｅｔａ３，８，１１，１３ｔｅｔｒａｅｎ７ｏｎｅ（３）藿香酚（２）为一新的化合物，而异藿香酚（３）系首次从天然界分离得到，二者为一对异构体。     

半边旗二萜类化合物的液-质联用图谱鉴定

用高效液相色谱-大气压化学电离源质谱联用的方法建立总离子流色谱图,以色谱保留时间和色谱峰的质谱图为依据,对不同地区和不同采集时间的半边旗LC-MS图谱中的主要色谱峰进行了对比分析和质谱鉴定.色谱分析条件:色谱柱为Diamonsil ODS、4.6 mm×150mm,流动相为30%CH3CN-70%2mmol/L NH4AC、流速1.0 ml/min,进样5 μl;质谱分析条件:APCI负离子源,质谱扫描范围m/z 50～700,扫描间隔1s.以对照品为参比,鉴定出贝壳杉烷系二萜类化合物4F、5F和6F的色谱峰;根据色谱行为和质谱行为,推测出6F的16位饱和态化合物以及4F和5F的甙.对不同地区和采集时间的半边旗LC-MS指纹图谱中的主要色谱峰进行比较分析得出,广州市郊和湛江地区以及在11～12月采集的半边旗中5F含量较高.本法简便、快速,可为半边旗中二萜类抗癌化合物的深入研究和新药资源的开发提供参考.     

阿托伐他汀联合银杏二萜内酯葡胺注射液治疗急性脑梗死的临床研究

目的探讨应用阿托伐他汀联合银杏二萜内酯葡胺注射液治疗急性脑梗死的临床效果。方法选取2015年1月—2017年12月西宁市第一人民医院收治的急性脑梗死患者82例,随机分成对照组(41例)和治疗组(41例)。对照组静脉滴注银杏二萜内酯葡胺注射液,5 m L加入250 m L生理盐水,1次/d。治疗组在对照组基础上口服阿托伐他汀钙片,20 mg/次,1次/d。两组患者均连续治疗14 d。观察两组患者临床疗效,同时比较治疗前后两组患者总胆固醇(TC)/高密度脂蛋白胆固醇(HDL-C)、载脂蛋白(Apo)B/Apo A-l比值、国立卫生研究院卒中量表(NIHSS)评分、颈动脉超声参数及白介素(IL)-1β、IL-6、超氧化物歧化酶(SOD)和丙二醛(MDA)水平。结果治疗后,对照组和治疗组临床总有效率分别为75.6%、92.7%,两组比较差异具有统计学意义(P0.05)。治疗后,两组血清TC/HDL-C、Apo B/Apo A-l比值和NIHSS评分均显著降低(P0.05),且治疗组上述指标显著低于对照组(P0.05)。治疗后,两组左、右两侧颈总动脉内径、RI及IMT值较治疗前均显著降低(P0.05),且治疗组颈动脉超声参数显著低于对照组(P0.05)。治疗后,两组血清IL-1β、IL-6、MDA浓度较治疗前显著降低低(P0.05),血清SOD水平显著升高(P0.05),且治疗组IL-1β、IL-6、SOD、MDA水平明显优于对照组(P0.05)。结论阿托伐他汀联合银杏二萜内酯葡胺注射液治疗急性脑梗死可有效改善患者神经功能,减轻机体炎性及氧化应激损伤,疗效确切。     

Isolation and analysis of bioactive diterpenoids in Salvia species (Salvia chionantha and Salvia kronenburgiii) by micellar electrokinetic capillary chromatography

In the present work, we isolated two bioactive diterpenoids, horminone and 7-O-acetylhorminone and developed a micellar electrokinetic chromatography (MEKC) method for the simultaneous quantitative analysis of them in Turkish Salvia species. The optimal separation electrolyte was 50 mmol/L SDS and 25% methanol at pH 11.5. The limits of detection (S/N = 3) were 3.269 and 4.518 μg/mL for horminone and 7-O-acetylhorminone, respectively. The method has been applied successfully to analyze these two components in Salvia chionantha and Salvia kronenburgii acetone extracts.     

卤地菊二萜化学成分研究

目的:对卤地菊全草的化学成分进行研究。方法:用色谱法和波谱分析法对卤地菊的化学成分进行分离和结构鉴定。结果:从卤地菊全草中分离得到7个化合物,分别鉴定为:对映-贝壳杉-16-烯-19-酸(Ⅰ)、对映-贝壳杉-16α,17-二羟基-19-酸(Ⅱ)、对映-贝壳杉-15α-异戊烯酰-16-烯-19-酸(Ⅲ)、β-谷甾醇(Ⅳ)、豆甾醇(Ⅴ)、豆甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅵ)和正二十六烷醇(Ⅶ)。结论:化合物Ⅰ～Ⅲ为首次从该植物中分离得到。     

尾叶香茶菜花和果实的化学成分(英文)

目的:研究尾叶香茶菜 Rabdosia excisa 花和果实的化学成分。方法:利用硅胶柱色谱法进行分离和纯化化合物。通过理化性质和波谱数据鉴定结构。结果:从尾叶香茶菜的花和果实部分共分离鉴定了 16 个化合物: 豆甾醇 (Ⅰ); α-香树脂醇棕榈酸酯 (Ⅱ);熊果酸 (Ⅲ); 2α, 3α, 19-三羟基-12-烯-28-乌索酸(Ⅳ); 2α-羟基乌苏酸(Ⅴ); 2α-羟基齐墩果酸(Ⅵ); isodonal(Ⅶ);maoyecrystalE (Ⅷ); kamebakaurin (Ⅸ); macrocalyxinG (Ⅹ); epinodosinol (Ⅺ); rabdosichuanin C (Ⅻ); kamebacetal A (ⅩⅢ); 冬凌草甲素(ⅩⅣ); enmenol-glucoside (ⅩⅤ); lasiodonin (ⅩⅥ). 结论:除了化合物Ⅰ, Ⅱ, Ⅸ , Ⅻ, ⅨⅣ, 其他化合物都是首次从尾叶香茶菜中发现。     

From local to global—Fifty years of research on Salvia divinorum

Ethnopharmacological relevance

In 1962 ethnopharmacologists, Hofmann and Wasson, undertook an expedition to Oaxaca, Mexico. These two researchers were the first scientists to collect a flowering specimen of Salvia divinorum allowing the identification of this species. While the species' traditional use is confined to a very small region of Mexico, since Hofmann and Wasson's expedition 50 years ago, Salvia divinorum has become globally recognized for its main active constituent, the diterpene salvinorin A, which has a unique effect on human physiology. Salvinorin A is a kappa-opioid agonist and the first reported psychoactive diterpene.

Methods

This review concentrates on the investigation of Salvia divinorum over the last 50 years including ethnobotany, ethnopharmacology, taxonomy, systematics, genetics, chemistry and pharmacodynamic and pharmacokinetic research. For the purpose of this review, online search engines were used to find relevant research. Searches were conducted between October 2011 and September 2013 using the search term “Salvia divinorum”. Papers were excluded if they described synthetic chemical synthesis of salvinorin A or analogues.

Results

Ethnobotanically there is a comprehensive body of research describing the traditional Mazatec use of the plant, however, the modern ethnobotanical use of this plant is not well documented. There are a limited number of botanical investigations into this plant and there are still several aspects of the botany of Salvia divinorum which need further investigation. One study has investigated the phylogenetic relationship of Salvia divinorum to other species in the genus. To date the main focus of chemistry research on Salvia divinorum has been salvinorin A, the main active compound in Salvia divinorum, and other related diterpenoids. Finally, the effects of salvinorin A, a KOR agonist, have primarily been investigated using animal models.

Conclusions

As Salvia divinorum use increases worldwide, the emerging cultural use patterns will warrant more research. More botanical information is also needed to better understand this species, including germination, pollination vector and a better understanding of the endemic environment of Salvia divinorum. As well there is a gap in the genetic knowledge of this species and very little is known about its intra-species genetics. The terpenes in Salvia divinorum are very well documented, however, other classes of constituents in this species warrant further investigation and identification. To date, the majority of the pharmacology research on Salvia divinorum has focused on the effects of salvinorin A using animal models. Published human studies have not reported any harmful effects when salvinorin A is administered within the dose range of 0.375–21 µg/kg but what are the implications when applied to a larger population? More data on the toxicology and safety of Salvia divinorum are needed before larger scale clinical trials of the potential therapeutic effects of Salvia divinorum and salvinorin A are undertaken.     

HPLC鉴定五种香茶菜属植物

唇形科香茶菜属植物,具有贝壳杉烯型,B-闭联贝壳杉烯型和螺旋贝壳杉烯型等结构的二萜化合物。药理研究表明具有抗菌及抗癌活性。该属植物大多外形类似,开花前不易鉴别。我们应用高效液相色谱法描绘五种香茶菜植物叶片乙醚提取物中二萜化合物的图谱,由于各种植物中所含的二萜结构不同而图谱亦相异,同一品种植物虽产地不同但图谱仍一致,与经     

Di- and sesqui-terpenoids isolated from the pods of<Emphasis Type="Italic">Sindora sumatrana</Emphasis> and their potential to inhibit lipopolysaccharide-induced nitric oxide production

Activity-guided fractionation of the n-hexane and CHCl3-soluble fractions of Sindora sumatrana using a bioassay based on the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production by inducible nitric oxide synthase (iNOS) in murine macrophage RAW 264.7 cells led to the isolation of the known compound, (+)-7beta-acetoxy-15,16-epoxy-3,13(16),14-clerodatriene-18-oic acid (2) as an active constituent. In addition, a new trans-clerodane diterpenoid, (+)-2-oxokolavenic acid (1), together with six known compounds, (+)-3,13-clerodadiene-16,15-olide-18-oic acid (3), (+)-7beta-acetoxy-3,13-clerodadiene-16,15-olide-18-oic acid (4), (+)-7beta-acetoxy-16-hydroxy-3,13-clerodadiene-16,15-olide-18-oic acid (5), beta-caryophyllene oxide (6), clovane-2beta,9beta-diol (7), and caryolane-1,9beta-diol (8) were isolated and found to be inactive. The structure of compound 1 was determined using physical and spectroscopic methods such as 1D and 2D-NMR experiments. The known compounds 2-8 were identified by the spectroscopic data and by comparison with the published values. Of eight isolates (1-8), only compound 2 exhibited an iNOS inhibitory activity with IC50 value of 51.6 microM.     

Skin irritant effects of esters of phorbol and related polyols

The skin irritant potencies of several naturally occurring and semisynthetic polyfunctional esters based on the tigliane hydrocarbon skeleton were studied using a mouse ear irritancy assay. The compounds used were esters of 12-deoxyphorbol, 12-deoxy-16-hydroxyphorbol, and phorbol. Observations were also made on the time interval between application of these compounds in acetone solution to the mouse ear, and the attainment of maximum response. Structure/activity relationships are discussed and compared with previous observations on the skin irritant potencies of esters based on the closely related daphnane hydrocarbon skeleton. The possible nature of the site of action in the target membrane is also discussed.