小酸浆中甾体类化学成分研究

目的研究小酸浆Physalis minima全草中甾体类化学成分。方法利用硅胶柱色谱、Sephadex LH-20凝胶柱色谱、中压ODS柱色谱及半制备高效液相色谱等方法分离纯化,根据理化常数和核磁共振谱、质谱等光谱数据鉴定化合物结构。结果从小酸浆全草的乙醇提取物中分离得到7个甾体类化学成分,其中酸浆苦素类化合物2个,分别鉴定为16,24-cyclo-13,14-secoergost-2-ene-18,26-dioicacid-14:17,14:27-diepoxy-5α,6β,13α,20α,22β,25β-hexahydroxy-1,15-dioxo-γ-lactone-δ-lactone(1)、酸浆苦素D(2);醉茄内酯类化合物5个,分别鉴定为physagulin L(3)、physagulin M(4)、physaminimin F(5)、physagulin K(6)、withagulatin A(7)。结论化合物1为新化合物,命名为25-羟基酸浆苦素D;化合物3、4、7为首次从该植物中分离得到。     

酸浆化学成分研究(Ⅱ)

目的研究酸浆Physalis alkekengivar.franchetii宿萼内活性成分。方法采用硅胶、凝胶、高效液相等色谱技术分离,利用理化性质和核磁共振光谱、MS等技术鉴定结构。结果分离得到4个化合物,分别为反式咖啡酸乙酯(1)、25,27-二脱氢酸浆苦素L(2)、酸浆苦素D(3)、大血藤苷E(cuneataside E,4)。结论化合物2为新的天然产物,化合物4为首次从该植物中分离得到。     

锦灯笼果实提取工艺优选及抗氧化活性考察

目的：优选锦灯笼果实的提取工艺并考察提取物的体外抗氧化活性。方法：以总黄酮、总酚酸提取量为指标,通过单因素试验和正交试验考察乙醇体积分数、提取时间及料液比对锦灯笼果实醇提工艺的影响,考察提取物对ABTS自由基的清除能力。结果：最佳提取工艺为加20倍量85%乙醇提取2次,每次0.5 h;总黄酮和总酚酸平均提取量分别为0.618,1.152 mg·g^-1,RSD依次为1.66%,1.19%。结论：结合药效学试验筛选的提取工艺更加科学合理,锦灯笼果实具有一定的体外抗氧化能力。     

贮藏条件对锦灯笼药材的质量影响

目的:测定不同贮藏条件下锦灯笼药材有效成分的含量变化,研究贮存条件对锦灯笼药材的质量影响。方法:采用HPLC法测定锦灯笼药材在室温、加热、冷冻、暴晒等条件下存放一定时间后酸浆苦素成分的含量变化。结果:不同贮藏条件下,酸浆宿萼中酸浆苦素类成分含量变化显著。结论:贮藏条件对锦灯笼药材的质量有很大影响应,应严格控制。     

锦灯笼和枸杞子水提液对乳酸菌的促生作用

目的研究锦灯笼和枸杞子对乳酸菌的促生作用,为微生态制剂的开发及中药合理使用提供理论依据。方法将不同浓度的锦灯笼和枸杞子水提液添加到乳酸菌的体外生长培养基中,37℃培养48h,活菌计数。结果 2%和5%的锦灯笼以及0.5%和1%的枸杞子对乳酸菌生长具有明显的促进作用(P0.01),5%的锦灯笼促进乳酸菌生长的效果最好,菌数分别是对照组的1.6倍左右,但随着药物浓度的增加,两种药物促乳酸菌生长的作用显著减弱。结论一定浓度的锦灯笼和枸杞子水提液能够促进乳酸菌的生长。     

灯笼草消炎作用的实验观察

目的 观察灯笼草的消炎作用。方法 对用完全弗氏佐剂致炎后的急性期和慢性期佐剂性关节炎大鼠，予4．2g／kg灯笼草灌胃给药1周后分别测定其致炎后爪的局部周长和厚度的改变。结果 灯笼草均能不同程度地减轻急性期和慢性期佐剂性关节炎大鼠致炎后爪的局部肿胀。结论 灯笼草具有消炎作用。     

Assessment of antidiabetic activity and acute toxicity of leaf extracts from Physalis peruviana L. in guinea-pig

Objective

To verify the antidiabetic activity of leaf extracts from Physalis peruviana L. popularly used in the Eastern part of the Democratic Republic of the Congo and to point out the possible toxicity.

Method

Aqueous decoctions prepared from dried leaves powder were administrated to guinea pigs at the dose range of 100 mg/kg to 3.2 g/kg of body weight. The hypoglycemic activity was evaluated by glucose tolerance test, loading animals with glucose 4 g/kg and measuring blood glucose concentrations at various times. The effect was compared to the control and glibenclamide as antidiabetic reference drug. Acute toxicity was evaluated by recording mortality rate, changes on blood biomarkers and damage caused to vital organs.

Results

At a dose of 100 mg/kg, the aqueous extract induced a significant reduction of peak concentration at 30 min after glucose loading as compared with control or reference (P<0.05). At doses greater than 400 mg, some alterations on blood, kidney and liver markers were observed. Upper 800 mg/kg, mortality was observed with LD₅₀ estimated at about 1 280 mg/kg. At the autopsy, vital organs were in haemorrhage and swelling state.

Conclusion

The crude aqueous extracts from the leaves of Physalis peruviana L. present hypoglycemic activity in animal model, but at high doses the plant may cause severe intoxication.     

锦灯笼中哌嗪类化学成分研究

目的 研究锦灯笼Phyysalis alkekengi var. francheti果实的化学成分。方法 采用硅胶、制备液相等色谱技术进行分离,通过NMR等波谱学方法确定化合物的结构。结果 从锦灯笼大孔吸附树脂50%乙醇洗脱组分中分离得到13个化合物,分别鉴定为 (3S, 6R)-3-异丙基-6-(2-甲基丙基)-2, 5-哌嗪二酮（1）、(3S, 6S)-3-异丁基-6-异丙基-2, 5-哌嗪二酮（2）、(3S, 6S)-3, 6-二-(2-甲基丙基)-2, 5-哌嗪二酮（3）、(3S, 6S)-3, 6-二异丙基-2, 5-哌嗪二酮（4）、(3S, 6R)-3-(2-甲基丙基)-6-苄基-2, 5-哌嗪二酮（5）、(3S, 6S)-3-异丁基-6-苄基-2, 5-哌嗪二酮（6）、(3S, 6S)-3-异丙基-6-对羟基苄基-2, 5-哌嗪二酮（7）、(3S, 6R)-3-异丙基-6-对羟基苄基-2, 5-哌嗪二酮（8）、(3S, 6R)-3-(2-甲基丙基)-6-对羟基苄基-2, 5-哌嗪二酮（9）、(3S, 6S)-3-异丁基-6-对羟基苄基-2, 5-哌嗪二酮（10）、(3S, 6S)-3-异丙基-6-苄基-2, 5-哌嗪二酮（11）、(3S, 6R)-3-异丁基-6-(2-甲基丙基)-2, 5-哌嗪二酮（12）、(3S, 6S)-3-苄基-6-对羟基苄基-2, 5-哌嗪二酮（13）。结论 化合物1～13均为首次从该属植物中分离得到。     

Display of neutralizing epitopes of Canine parvovirus and a T-cell epitope of the fusion protein of Canine distemper virus on chimeric tymovirus-like particles and its use as a vaccine candidate both against Canine parvo and Canine distemper

Expression of Physalis mottle tymovirus coat protein in Escherichia coli was earlier shown to self-assemble into empty capsids that were nearly identical to the capsids formed in vivo. Amino acid substitutions were made at the N-terminus of wild-type Physalis mottle virus coat protein with neutralizing epitopes of Canine parvovirus containing the antigenic sites 1–2, 4 and 6–7 and T-cell epitope of the fusion protein of Canine distemper virus in various combinations to yield PhMV1, PhMV2, PhMV3, PhMV4 and PhMV5. These constructs were cloned and expressed in E. coli. The chimeric proteins self-assembled into chimeric tymovirus-like particles (TVLPs) as determined by electron microscopy. The TVLPs were purified by ultracentrifugation and injected into guinea pigs and dogs to determine their immunogenicity. Initial immunogenicity studies in guinea pigs indicated that PhMV3 gave a higher response in comparison to the other TVLPs for both CPV and CDV and hence all further experiments in dogs were done with PhMV3. HI was done against different isolates obtained from various parts of the country. Protective titres indicated the broad spectrum of the vaccine. In conclusion the study indicated that the above chimeric VLP based vaccine could be used in dogs to generate a protective immune response against diseases caused by both Canine parvo and Canine distemper virus.