Triterpene Glycosides from Sea Cucumber Holothuria scabra with Cytotoxic Activity

Objective To study the new triterpene glycosides from sea cucumber Holothuria scabra with cytotoxic activity. Methods Triterpene glycosides from H. scabra were separated and purified by chromatography on DA-101, silica gel, and reversed-phase silica gel column, as well as RP-HPLC. Their structures were elucidated on the basis of spectral data and chemical evidence. Results Three triterpene glycosides were identified as scabraside D (1), fuscocineroside C (2), and 24-dehydroechinoside A (3). Their inhibition on P-388, A549, MKN-28, HCT116, and MCF-7 cells were significant. Conclusion Scabraside D (1) is a new triterpene glycoside, and compounds 2 and 3 are isolated from H. scabra for the first time. The glycosides 1－3 show the in vitro cytotoxicity against five human tumor cell lines in comparison to 10-hydroxycamptothecin.     

窄谱UVB联合雷公藤多甙片治疗玫瑰糠疹的疗效观察

目的观察窄谱UVB联合雷公藤多甙片治疗玫瑰糠疹的临床疗效。方法 78例患者随机分为治疗组（40例,窄谱UVB照射联合口服雷公藤多甙片治疗）和对照组（38例,口服雷公藤多甙片治疗）,观察两组疗效。结果 1个疗程后,治疗组总有效率95.0%,对照组65.8%,组间差异有统计学意义（P〈0.01）。结论窄谱UVB联合雷公藤多甙片治疗玫瑰糠疹安全有效,值得临床推广应用。     

南山藤的化学成分研究

从萝藦科南山藤属植物南山藤的干燥茎中分离鉴定了6个化合物:β-D-黄夹吡喃糖基-(1→4)-β-D-磁麻吡喃糖基-(1→4)-β-D-阿洛吡喃糖苷(1),β-D-黄夹吡喃糖基-(1→4)-β-D-磁麻吡喃糖苷(2),marsectohexol(3),drevogenin D 3-O-β-D-磁麻吡喃糖苷(4),dregeosides Da1(5),dregeosides A11(6)。其中,化合物1为新低聚糖,化合物4为首次从属内分得C21甾体苷。     

Herbal modulation of drug bioavailability: enhancement of rifampicin levels in plasma by herbal products and a flavonoid glycoside derived from Cuminum cyminum

The bioavailability of rifampicin (RIF) in a fixed dose combination (FDC) used for the treatment of tuberculosis remains an area of clinical concern and several pharmaceutical alternatives are being explored to overcome this problem. The present study presents a pharmacological approach in which the bioavailability of a drug may be modulated by utilizing the herb-drug synergism. The pharmacokinetic interaction of some herbal products and a pure molecule isolated from Cuminum cyminum with RIF is shown in this paper. An aqueous extract derived from cumin seeds produced a significant enhancement of RIF levels in rat plasma. This activity was found to be due to a flavonoid glycoside, 3',5-dihydroxyflavone 7-O-beta-D-galacturonide 4'-O-beta-D-glucopyranoside (CC-I). CC-I enhanced the Cmax by 35% and AUC by 53% of RIF. The altered bioavailability profile of RIF could be attributed to a permeation enhancing effect of this glycoside.     

大黄5种饮片中2个二苯乙烯苷类成分含量测定

目的:进行大黄5种饮片中2个二苯乙烯苷类成分的含量测定。方法:采用HPLC法,对大黄生、酒、醋、熟、炭饮片中反-3,5,4′-三羟基二苯乙烯基-4′-O-β-D-葡萄糖苷(a)、反-3,5,4′-三羟基二苯乙烯基-4′-O-β-D-(6″-O-没食子酰基)葡萄糖苷(b)进行含量测定。流动相为甲醇-1%冰醋酸溶液,柱温35℃,流速1.0 mL.m in-1,检测波长分别为280,300 nm。结果:大黄5种饮片中均能检测到上述2种成分,且2种成分的变化趋势相同。大黄生、酒、醋片中2种成分含量较高且较接近,炮制为熟片和炭片后,2种成分的含量,与生片相比均降低80%以上。结论:a,b均为苷类成分,高温加热炮制对其含量均有显著的影响,进一步分析比较苷类成分及其相应苷元的含量变化,将为科学阐释炮制前后大黄物质基础的变化规律提供科学依据。     

黄皮叶的化学成分研究

目的:对黄皮Clausena lansium叶的化学成分进行分离和鉴定。方法:采用正相(硅胶)、反相(ODS)、凝胶柱色谱和高效液相制备方法进行分离纯化,利用波谱数据和理化常数鉴定化合物的结构。结果:从乙醇提取物中分离鉴定了7个化合物,分别为corchoionoside C(1),1′-O-β-D-glucopyranosyl(2R,3S)-3-hydroxynodakenetin(2),槲皮素-3-O-刺槐双糖(3),芦丁(4),槲皮素-3-O-β-D-吡喃葡萄糖-(1→4)-α-L-吡喃鼠李糖苷(5),山柰酚-3-O-α-L-吡喃鼠李糖-(1→2)-[α-L-吡喃鼠李糖-(1→6)]-β-D-吡喃葡萄糖苷(6),山柰酚-3-O-α-L-吡喃鼠李糖-(1→2)-[α-L-吡喃鼠李糖-(1→6)]-β-D-吡喃半乳糖苷(7)。结论:化合物1~7均为首次从该属植物中分离得到。     

女贞子的化学成分研究

目的:研究女贞Ligustrum lucidum的干燥成熟果实的化学成分。方法:采用硅胶柱色谱,Sephadex LH-20凝胶柱色谱和ODS柱色谱等色谱方法进行分离纯化,并根据NMR,MS等波谱方法和理化性质鉴定其化学结构。结果:从女贞子中分离得到20个化合物,其中三萜类化合物15个,分别鉴定为齐墩果酸(1),2α-羟基齐墩果酸(2),乙酰齐墩果酸(3),羽扇豆醇(4),白桦脂醇(5),达玛烯二醇(6),3β-乙酰氧基-20,25-环氧-24α-羟基-达玛烷(7),20,25-环氧-3β,24α-二羟基-达玛烷(8),3β-乙酰氧基-达玛烯二醇(9),3β,20S-二羟基-24R-过氧羟基-25-烯-达玛烷(10),fouquierol(11),oliganthas A(12),达玛烯二醇3-O-棕榈酸酯(13),拟人参皂苷元II 3-O-棕榈酸酯(14),3β,20S-二羟基-25-过氧羟基-23E-烯-达玛烷(15);苯乙醇类化合物5个,分别为毛蕊花苷(16),北升麻宁(17),2-(3,4-二羟基苯基)乙基-O-β-D吡喃葡萄糖苷(18),osmanthuside H(19),3,4-二羟基苯基乙醇(20)。结论:化合物4,16,17,19为首次从本植物中分离得到,化合物12~15为首次从本属植物中分离得到。     

山茱萸大孔吸附树脂富集物中环烯醚萜苷含量的测定

目的：评价大孔吸附树脂富集山茱萸有效成分的应用效果。方法：UV法测定总苷的含量,RP-HPLC法测定莫诺苷及马钱苷的含量。结果：莫诺苷由药材含量的1.58%提高到51.00%,马钱苷由药材含量的0.62%提高到16.09%,总环烯醚萜苷由药材含量的4.54%提高到91.57%,结论：大孔吸附树脂富集工艺稳定,可显著提高成药的质量,从而生产出剂量小和质量稳定的可控制剂。     

半边旗中二萜类化合物5F葡糖糖苷的分离鉴定及其抗肿瘤作用

目的:进一步研究半边旗的抗肿瘤活性成分。方法:运用反复硅胶柱层析的方法对半边旗中的化学成分进行分离纯化,以LC-MS及各种有机波谱法鉴定化学单体结构;并通过MTT法对分离鉴定的单体化合物及其苷元进行抗肿瘤活性研究。结果:从中分离鉴定1个二萜苷类化合物,为11β-hydroxy-15-oxo-ent-kaur-16-en-19-oic acid 19-β-D-glucoside(Ⅰ);化合物Ⅰ及其苷元5F均可抑制两种肿瘤细胞A549和CNE-2Z的生长,且它们对两种肿瘤细胞的抑制作用呈一定剂量依赖关系和时间依赖关系,化合物5F的活性强于化合物Ⅰ。结论:α,β不饱和环戊酮结构是其活性部位,5F中19位碳上的羧基与糖连接形成酯苷,成为化合物Ⅰ后,其抗肿瘤活性大大降低。     

细柱五加茎中的一个新的贝壳杉烷型二萜苷

目的研究细柱五加Acanthopanax gracilistylus茎的化学成分。方法应用色谱方法分离纯化,通过波谱技术结合理化性质的方法鉴定化合物结构。结果 从正丁醇部位分离并鉴定了1个新的贝壳杉烷型二萜苷,命名为贝壳杉烷酸苷A(16α,17-dihydroxy-en-tkauran-19-oic 19-[β--Dglucopyranosyl-(1→2)-β-D-glucopyranosyl]ester)(1)。结论化合物1为新化合物。