探讨基于谱效关系的中药质量评价的物元分析新方法

通过分析现行中药质量控制模式的局限性,引入"价值工程"中为产品评价提供的简便实用的物元分析数学模型,以中药材为例简述基于谱效关系建立中药质量评价物元模型的研究方法.提出的中药质量控制与评价的新模式,首先以中药"谱-效"关系的研究结果作为合理评价中药质量的主要依据,以物元模型来分析和评价中药的质量,提供了相对合理的计算方法.构建符合中药特点的质量控制新模式,以期为保证中药安全性、有效性和质量稳定性,促进中药现代化发展提供新的科学对策和技术支持.     

苦瓜中新化合物的化学研究

目的 研究苦瓜的新活性成分.方法 采用乙醇提取、微波萃取、D-101型大孔树脂纯化、硅胶柱色谱以及制备液相色谱等方法分离,通过理化常数及光谱数据鉴定化合物的结构.结果 分离并鉴定了8个化合物,分别为charantadiol A(5β,19-epoxycucurbita-6,23(E),25(26)-triene-3β,19(R)-diol,Ⅰ)、(+)-eduesmin(Ⅱ),blueme-nol A(Ⅲ)、宽叶葱苷元D(karatavilagenin D.Ⅳ)、5β,19-epoxycucurbita-6,23-diene-3β-19,23-triol(Ⅴ)、苦瓜皂苷元Ⅰ(5,19-epoxy-5β-cucurbita-6,23(E)-diene-3β,25-diol,Ⅵ)、苦瓜皂苷L昔元(aglycone of momordicoside L,3β,7β,25-trihydroxy-cucurbita-5,23(E)-diene-19-al,Ⅶ)、β-谷甾醇(β-sitosterol,Ⅷ ).结论 化合物Ⅰ为新化合物,命名为苦瓜二醇A(charantadiol A),化合物Ⅱ、Ⅲ为从苦瓜中首次分离得到.     

Proximate and mineral composition of the leaves of Momordica balsamina L.: an under-utilized wild vegetable in Botswana

Proximate and mineral analyses were conducted on the leaves of Momordica balsamina L., an under-utilized wild vegetable in Botswana. The protein, fibre, fat and ash contents were 288, 37, 54 and 127 g/kg, respectively. Potassium was the most abundant mineral at 27.05 g/kg, followed by magnesium (3.82 g/kg), phosphorus (3.24 g/kg), calcium (2.22 g/kg) and sodium (0.06 g/kg). Other minerals were zinc (0.39 g/kg), manganese (0.15 g/kg) and iron (0.14 g/kg). Compared with cabbage, lettuce and spinach, this wild vegetable contained more protein and fat, while the fibre content was less. Among the minerals analysed, the leaves of M. balsamina had higher values than those reported for the exotic vegetables, except for sodium. The wild vegetable could be promoted as a protein supplement for cereal-based diets in poor rural communities, while its high potassium content could be utilized for the management of hypertension and other cardiovascular conditions. The relatively high concentrations of zinc, iron and manganese could contribute towards combating the problem of micronutrient deficiencies.     

The effects of Momordica charantia on obesity and lipid profiles of mice fed a high-fat diet

BACKGROUND/OBJECTIVES

The present study was conducted to investigate the effects of dried Momordica charantia aqueous extracts (MCA) and ethanol extracts (MCE) on obesity and lipid profiles in mice fed a high-fat diet.

MATERIALS/METHODS

Forty two ICR mice were randomly divided into six groups. The normal group was fed a basal diet, and other groups were fed a 45% high-fat diet (HFD) for 7 weeks. The normal and HFD groups were also orally administered distilled water each day for 7 weeks. The remaining groups received Momordica charantia extract (0.5 or 1.0 g/kg/day MCA, and 0.5 or 1.0 g/kg/day MCE). In order to measure the anti-obesity and lipid profile improvement effects, body and visceral tissue weight, lipid profiles, plasma insulin levels, hepatic malondialdehyde (MDA) levels and superoxide dismutase (SOD) activity were measured.

RESULTS

Both MCA and MCE significantly decreased body and visceral tissue weight relative to those of the HFD group (P < 0.05). Additionally high doses of MCE and MCA significantly reduced the plasmatic insulin levels compared to the HFD groups (P < 0.05) to concentrations comparable to those found in the normal group. MCA and MCE supplementation also significantly modulated the lipid profiles in plasma, liver, and feces compared to mice fed the HFD (P < 0.05). Furthermore MCA and MCE significantly increased hepatic SOD activity, and reduced MDA generation in the liver of the HFD mice (P < 0.05).

CONCLUSIONS

Results from the present study suggest that Momordica charantia extracts have anti-obesity effects and the ability to modulate lipid prolife of mice fed a HFD by suppressing body weight gain, visceral tissue weight, plasma and hepatic lipid concentrations, and lipid peroxidation along with increasing lipid metabolism.     

苦瓜中新化合物的化学研究

目的 研究苦瓜的新活性成分。方法 采用乙醇提取、微波萃取、D-101型大孔树脂纯化、硅胶柱色谱以及制备液相色谱等方法分离,通过理化常数及光谱数据鉴定化合物的结构。结果 分离并鉴定了8个化合物,分别为charantadiol A (5β,19-epoxycucurbita-6,23(E),25(26)-triene-3β,19(R)-diol,Ⅰ)、(+)-eduesmin(Ⅱ)、bluemenol A(Ⅲ)、宽叶葱苷元D(karatavilagenin D,Ⅳ)、5β,19-epoxycucurbita-6,23-diene-3β-19,25-triol(Ⅴ)、苦瓜皂苷元Ⅰ(5,19-epoxy-5β-cucurbita-6,23(E)-diene-3β,25-diol,Ⅵ)、苦瓜皂苷L苷元(aglycone of momordicoside L,3β,7β,25-trihydroxy-cucurbita-5, 23(E)-diene-19-al,Ⅶ)、β-谷甾醇(β-sitosterol,Ⅷ)。结论 化合物Ⅰ为新化合物,命名为苦瓜二醇A(charantadiol A),化合物Ⅱ、Ⅲ为从苦瓜中首次分离得到。     

苦瓜蛋白酶抑制剂对苦瓜降糖多肽活性的保护作用

目的 探讨苦瓜蛋白酶抑制剂对苦瓜降糖多肽口服降糖活性的保护作用。方法 单次 iv 四氧嘧啶 80 mg/kg 给药建立糖尿病小鼠模型。以降糖多肽 (20、10、5 mg/kg) iv 给药,于 0.5、2、4、6、8 h 尾静脉取血测定空腹血糖;测定在不同降糖多肽与蛋白酶抑制剂配伍剂量下,ig 给药 21 d 后的空腹血糖值;以降糖作用显著的配伍比例,ig 给药 7、14、21 d 和停止给药 7 d 后测定血糖。结果 降糖多肽于 iv 给药 4 h 后,高、中、低3个剂量均表现出显著降血糖效应 (P ＜0.05、0.01);降糖多肽与抑制剂 (300+300)、(100+100)、(100+50)、(100+25) mg/kg 4 个配伍剂量组 ig 给药 21 d 后表现出显著降血糖效应,且以后两个剂量组 ig 给药的降血糖作用为更佳,停药 7 d 后给药组血糖值与模型组无显著差异。结论 苦瓜蛋白酶抑制剂在 ig 给药过程中能够使苦瓜降糖多肽免遭消化系统的蛋白水解酶破坏而起保护作用,维持其降血糖药效,该作用与两者间的配伍剂量有关。     

MAP30全长基因的克隆及在巴斯德毕赤酵母中的高效表达研究

目的研究毕赤酵母中高效表达全长MAP30蛋白及其生物活性。方法根据GeneBank公布的MAP30全序列设计特异性引物,以苦瓜基因组为模板,PCR扩增MAP30全长基因,将该基因插入pPIC9k载体中,经SacI酶切线性化后,电转化至GS115细胞,再通过G418筛选,最终获得了高拷贝重组GS115菌株。重组菌株在甲醇诱导下,SDS-PAGE分析表达的特异性条带,运用Pharmacia VDS图像分析软件进行条带密度扫描,得到各条带的扫描曲线图,计算出同一泳道目的蛋白条带峰面积相对于整个曲线所占的百分比,即蛋白纯度,并根据蛋白纯度和上清蛋白总量(Lowry法)计算出发酵上清液中目标蛋白含量。纯化时首先用75%的饱和硫酸铵盐析,然后用Phenyl Sepharose6FF疏水层析,再用CM-sepharoseFF阳离子层析。采用MTT法检测MAP30蛋白对人胃癌细胞株SGC7901的抑制作用。为验证重组MAP30蛋白结构的正确性,采用EDMAN降解法分析N末端8个氨基酸。结果重组菌株在甲醇诱导下,SDS-PAGE分析可见相对分子质量32000的特异性条带,重组蛋白占上清液总蛋白的67%;发酵液经硫酸铵沉淀、疏水和阳离子交换层析后,目的蛋白总回收率为32.4%。MTT法检测结果表明,重组MAP30蛋白具有明显的抑制人胃癌细胞SGC7901的活性,IC50为30μg/ml。N端的8个氨基酸测序进一步证实与理论一致。结论重组MAP30蛋白在毕赤酵母中正确表达,表达产物具有抑制肿瘤细胞的活性。     

纤维素酶提高苦瓜降血糖有效物质含量的研究

目的:利用纤维素酶对苦瓜进行水解,来提高苦瓜降血糖有效物质含量.方法:利用纤维素酶在不同条件下对苦瓜进行水解,确定最佳实验条件.结果:温度为50℃,pH为4.3～4.4的条件下,反应72h,纤维素酶对苦瓜进行水解的效果最好.结论:纤维素酶在本实验条件下可提高苦瓜降血糖有效物质含量.     

罗汉果脱毒苗的快速繁殖研究

目的筛选适宜的罗汉果脱毒苗茎段增殖培养基,研究培养温度与光照对茎段增殖培养的影响。方法采用正交试验设计和完全随机实验设计筛选罗汉果脱毒苗茎段增殖培养基。正交L9(34)实验以在M S BA 0.1 m g/L NAA 0.1 m g/L上培养30 d的罗汉果脱毒苗单芽姊妹系的单节茎段为外植体,以培养基中BA,NAA,IBA及蔗糖为试验因子,各因子设3个水平,以在不同处理得到的增殖系数为测定指标;在此基础上进一步研究了培养基中BA和蔗糖质量浓度对增殖效果的影响;采用完全随机实验设计研究温度,光照对茎段增殖培养生成试管苗的影响。结果通过对正交实验结果的极差分析及方差分析表明,在4个因子中,对罗汉果茎段增殖系数影响最大的是BA,其次是蔗糖的NAA,IBA的影响最小;BA,NAA,IBA及蔗糖对增殖系数的影响都达到极显著。根据新复极差检验的结果,当前研究得到的罗汉果离体茎段的最佳增殖培养基为M S BA 0.5 m g/L NAA 0.01 m g/L IBA 0.1 m g/L 蔗糖40 g/L,罗汉果茎段在此培养基上培养30 d后增殖系数为13.13;不同浓度BA与蔗糖对茎段培养的研究结果表明,BA在1.0 m g/L增殖系数最大。考虑为保持试管苗的遗传稳定性,BA为0.5 m g/L为宜。增殖培养基中的蔗糖适宜质量浓度为4.0%;罗汉果茎段培养适宜条件为培养温度25℃,培养光强1 000~3 000lx。结论增殖培养基的成功筛选及培养温度与光强的选择,有助于实现罗汉果脱毒苗的工厂化生产。     

山苦瓜的抗癌活性成分

对葫芦科植物山苦瓜Ｍｏｍｏｒｉｄｉｃａ ｄｉｏｉｃａ干燥块根的浸膏进行了分离、提纯,用Ｌ１２１０、ＣＣＥＲ－ＣＥＭ、ＬＳ１７４５癌细胞对其成分进行了体外筛选,５个化合物具有抗癌活性,经光谱鉴定,它们是拜俄尼酸（Ⅷ）、雪胆甲素（Ⅸ）、α－菠甾醇－３Ｏ－β－Ｄ－吡喃葡萄糖苷、线石竹皂元（Ⅴ）及常春藤皂苷元（Ⅶ）。