Bioactivity studies on beta-sitosterol and its glucoside

Beta-sitosterol and beta-sitosteryl-beta-D-glucoside were isolated as analgesic constituents from the leaves of Mentha cordifolia Opiz. The acetic acid-induced writhing test showed that beta-sitosterol and beta-sitosteryl-beta-D-glucoside decreased the number of squirms induced by acetic acid by 70.0% and 73.0%, respectively, at a dose of 100 mg / kg mouse. Statistical analysis using the Kruskall Wallis one-way analysis of variance by ranks showed that these isolates approximate the analgesic activity of mefenamic acid at a 0.001 level of significance. The hot plate method confirmed their analgesic activities, as beta-sitosterol and beta-sitosteryl-beta-D-glucoside exhibited a 300% and 157% increase in pain tolerance, respectively, while mefenamic acid, a known analgesic, showed a 171% increase. Neither isolate exhibited antiinflammatory activity using the carrageenan-induced mouse paw oedema assay. Beta-sitosterol also exhibited anthelminthic and antimutagenic activities. In vitro tests using live Ascaris suum as test animals showed that the behaviour of worms treated with beta-sitosterol approximated that of the positive controls, Combantrin and Antiox. An in vivo micronucleus test showed that beta-sitosterol inhibited the mutagenicity of tetracycline by 65.3% at a dose of 0.5 mg /kg mouse. At the same dose, it did not exhibit chromosome-breaking activity.     

胆木茎中一个新的吲哚生物碱苷

目的研究中药胆木水溶性部位的化学成分。方法采用大孔吸附树脂，硅胶柱色谱和Sephadex LH20凝胶柱色谱分离纯化，通过光谱分析鉴定化合物的结构。结果从胆木水溶性部位中分离得到7个化合物，分别鉴定为： naucleamide A-10-O-β-D-glucopyranoside (I)， 5-β-carboxystrictosidin (II)， 獐牙菜苷(III)， 番木鳖苷A(IV)， 3,4-dimethoxyphenyl-β-D-glucopyranoside (V)， 3,4,5-trimethoxyphenyl-β-D-glucopyranoside (VI)， 2-phenethylrutinoside (VII)。结论化合物I为新的吲哚类生物碱苷，化合物I～VII均为首次从该植物中分得。     

炮制对何首乌主要化学成分含量的影响

目的:对何首乌中主要化学成分大黄素、大黄素甲醚、大黄素-8-O-β-D-吡喃葡萄糖苷、大黄素甲醚-8-O-β-D-吡喃葡萄糖苷以及2,3,5,4′-四羟基反式二苯乙烯-2-O-β-D-吡喃葡萄糖苷的含量在炮制过程中不同时间的动态变化进行研究,并分析探讨它们的变化规律。方法:采用反相高效液相色谱法,对炮制前后何首乌中5种主要成分进行含量测定。结果:所测5种成分的含量均明显降低。结论:炮制使何首乌中主要化学成分的含量均明显降低,提示临床上应用制首乌是否必要值得探讨。     

胡黄连苷对小鼠急性化学性肝损伤的保护作用

目的研究胡黄连苷(GP)对小鼠急性化学性肝损伤的保护作用。方法灌胃给予乙醇或腹腔注射四氯化碳(CCl4)以制备小鼠急性化学性肝损伤模型,检测血清丙氨酸氨基转移酶(ALT)和天门冬氨酸氨基转移酶(AST)活性、肝脏重量指数。结果连续6d灌胃给予15.0、30.06、0.0 mg/(kg.d)GP能明显抑制肝损伤小鼠血清ALT、AST活性的升高(P<0.05),减轻增加的肝脏重量指数。结论GP对四氯化碳及乙醇引起的小鼠急性肝损伤具有保护作用。     

虎杖晶4号对人血PMNs呼吸暴发和氧自由基的作用

应用化学发光法测定①人血PMNs受PMA刺激产生的化学发光;②黄嘌呤—黄嘌呤氧化酶体系产生O_2;③VitC—CU~(2+)—酵母多糖产主·OH;④H_2O_2的释放。观察虎杖晶4号对上述体系产生自由基的影响。结果提示.虎杖晶4号对PMN呼吸暴发的早期(1～6 min)有明显的抑制作用,呈剂量依赖性;而在12min时发光强度均高于空白对照.表明因虎杖晶4号而使呼吸暴发滞后。其对O_2.·OH.H_2O_2均有清除作用.且呈剂量依赖性.IC_(50)分别为14.6.29.6和13.0μmol·L~(-1).     

旱莲草化学成分旱莲甙A和旱莲甙B的分离和鉴定

自旱莲草全草（Eclipta alba (L.)Hassk）中分得4个三萜化合物，经理化常数测定和光谱（IR，MS，UV，^1HNMR,^13CNMR和^13C-^1H COSY）解析，2个已知的三萜化合物分别为囊酸（echinocystic acid,1）和齐墩果酸（oleanolic acid,2），另2个为新化合物，分别命名为旱莲甙A（ecliptasaponin A,3）和旱莲甙B（ecliptasaponin B,4），Ⅰ和Ⅱ为首次从鳢肠属植物中获得。     

Minimization of photooxidative insult to calf lens protein irradiated with near UV-light in the presence of pigmented glucosides derived from human lens protein

An aqueous solution of a pigmented glucoside associated with human lens protein, 2-amino-3-hydroxyacetophenone-O-beta-D-glucoside (AHA-Glc), was irradiated with near UV-light. The near UV-irradiated glucoside was shown to generate a much lower level of active species of molecular oxygen as compared to the level of the active species generated from the irradiated aglycon, 2-amino-3-hydroxyacetophenone (AHA). This result suggests that the glycon of the glucoside is functioning as a scavenger for active oxygen generated from the aglycon of the irradiated glucoside. Superoxide dismutase (SOD) was shown to remove a large portion of the active oxygen generated from the irradiated AHA, so the bulk of the active species generated is assumed to be superoxide anion. The small portion of active oxygen remains after removal of superoxide anion may include singlet oxygen. The photooxidation of tryptophan residues of calf alpha-crystallin irradiated with near UV-light in the presence of AHA-Glc or AHA was investigated to confirm the role that the glycon plays in diminution of the active species of oxygen generated through the photosensitized aglycon of the glucoside. A decrease with time in the fluorescence intensity of the tryptophan residues irradiated with AHA-Glc was shown to be much slower as compared to the time-dependent decrease with AHA, indicating that the photooxidation proceeds with an increase in accumulation of active oxygen generated through the aglycon and that the glycon of the glucoside deactivates the active species as it is formed in the photodynamic process. Similar effects have also been observed in calf lens crystallin irradiated with either 3-hydroxykynurenine-O-beta-D-glucoside (HKN-Glc) or 3-hydroxykynurenine (HKN). Furthermore, effects of near UV-irradiation on calf lens soluble protein in the presence of AHA-Glc or AHA were studied by monitoring changes in the SDS-PAGE profile of the irradiated protein. Near UV-irradiation with AHA-Glc was shown to bring about a slight change in cross-linking of the polypeptides, while irradiation with AHA was shown to give rise to a significant increase in cross-linking of the polypeptides. In conclusion, pigmented glucoside associated with human lens protein is not only a photosensitizer for near UV-light but also an anti-photooxidant to deactivate active oxygen formed through the in situ photosensitizer, in order that photooxidative insults to lens proteins may be minimized during aging.     

复方甘草酸苷在皮肤科中的临床应用

复方甘草酸苷是以甘草中的活性物质甘草甜素为主要成分,并以0.2%甘草酸苷、0.1%L-半胱氨酸和2%甘氨酸而制成的复方制剂,具有抗炎、抗过敏和糖皮质激素样作用,同时还具有免疫调节作用。而变态反应(包括Ⅰ、Ⅱ、Ⅲ型)常是许多皮肤病如银屑病、儿童水痘、过敏性紫癜、带状疱疹、湿疹、慢性荨麻疹、特应性皮炎、玫瑰糠疹、掌跖脓疱病、白癜风等的重要的发病机制,文章综述了复方甘草酸苷在皮肤科中的临床应用近况。     

HPLC法测定公英健胃合剂中橙皮苷的含量

目的:建立HPLC法测定公英健胃合剂中橙皮苷含量的方法.方法:采用ODS-2 HYPERSIL C18色谱柱,甲醇-0.5%冰醋酸(40:60)为流动相;流速1.0ml·min-1;检测波长283nm.结果:橙皮苷在5.246～52.46鸺·ml"范围内线性关系良好(r=0.9999),平均回收率为99.07%,RSD=0.61%(n=6).结论:本方法操作筒便,专属性强,结果准确,可用于公英健胃合剂的质量控制.