苦瓜水提取物对小鼠的急性经口毒性和遗传毒性实验研究

目的了解苦瓜水提取物的急性经口毒性和遗传毒性，为苦瓜的开发利用提供实验依据。方法按照GB15193—2003《食品安全性毒理学评价程序和方法》进行急性经口毒性实验、Ames实验、小鼠骨髓嗜多染红细胞微核实验及小鼠精子畸形实验。结果苦瓜水提取物的急性经口LD50〉21500mg/kg bw；三项遗传毒性实验结果均为阴性。结论苦瓜水提取物对小鼠的急性经口毒性属无毒，未见遗传毒性作用。     

苦瓜中新葫芦烷型皂苷的研究

目的研究苦瓜的化学成分。方法采用乙醇提取、大孔吸附树脂纯化和硅胶柱色谱分离,通过光谱分析鉴定化合物的结构。结果从苦瓜中分离并鉴定了2对异构体。经13C-NMR光谱分析,其中一对异构体的化学结构初步确定为19R-5β,19环氧葫芦烷-6,23,25-三烯-3β,19-二醇(Ⅰa)和19S-5β,19环氧葫芦烷-6,23,25-三烯-3β,19-二醇(Ⅰb);另一对异构体的化学结构确定为5β,19环氧葫芦烷-6,23,25-三烯-3-O-吡喃葡萄糖苷(Ⅱa)和5β,19环氧葫芦烷-6,23,25-三烯-3-O-阿洛吡喃糖苷(Ⅱb)。结论化合物Ⅰa、Ⅰb、Ⅱa、Ⅱb均为首次从苦瓜中分离得到的新化合物。     

苦瓜水提取物对大鼠毒副作用的实验研究

目的观察苦瓜水提取物对大鼠的毒副作用。方法将苦瓜水提取物按1.25 g/(kg bw)、2.50 g/(kg bw)、5.00 g/(kg bw)剂量给大鼠连续灌胃30 d,测定体重、进食量,计算食物利用率,实验末采血测定血象和血生化指标。结果苦瓜水提取物各剂量组对大鼠体重增长、总进食量及食物利用率差异无统计学意义(P>0.05)。与相应对照组比较,雄鼠5.00 g/(kg bw)剂量组白细胞总数显著降低,1.25 g/(kg bw)、5.00 g/(kg bw)剂量组天冬氨酸转氨酶显著降低,雌鼠2.50 g/(kg bw)剂量组白蛋白显著降低,雌雄鼠三个剂量组总蛋白均低于对照组,其中2.50 g/(kg bw)、5.00 g/(kg bw)剂量雌鼠组总蛋白降低有统计学意义。雄鼠总蛋白降低有剂量依赖性,相关系数为-0.964,呈显著负相关。各剂量对其他血液学、血生化指标、肝脏、脾脏、肾脏和雄鼠睾丸、雌鼠卵巢的绝对重量、脏/体比值等差异无统计学意义。大体解剖和组织病理检查未见与样品有关的异常改变。结论给大鼠喂养苦瓜水提取物30 d,可引起大鼠总蛋白降低,高达5.00 g/(kg bw)的剂量未产生其他可观察到的毒副作用。     

苦瓜粗多糖提取物降血糖作用的实验研究

目的　研究苦瓜粗多糖提取物(CPS)对正常及糖尿病小鼠血糖调节作用。方法　采用2 4只正常小鼠进行口服葡萄糖耐量试验,一次性经口给予动物葡萄糖3g kgbw ,实验组同时一次性给予CPS 1g kgbw ,对照组给予等量的生理盐水;应用1型和2型糖尿病模型小鼠,分别在随机进食和空腹情况下一次性经口给予CPS(1g kgbw) ,测定给药后2h、4h血糖水平,并与对照组血糖进行比较。结果　葡萄糖耐量试验中,实验组小鼠给予CPS 0 . 5h、1h后血糖水平显著低于对照组(分别低于对照组16 4 %和16 . 5 % ) ,差别具有显著性意义(P <0 .0 5和P <0 . 0 1)。2种糖尿病模型动物服用CPS后,各时点血糖水平较对照组显著下降(P <0 . 0 5 )。结论　苦瓜多糖粗提物对正常小鼠糖耐量有改善作用,能显著降低糖尿病模型动物随机及空腹血糖。     

木鳖子脂肪油不皂化物质的化学成分研究

目的：对木鳖子脂肪油的不皂化部分进行化学成分的研究。方法：石油醚提取脂肪油，氢氧化钾进行皂化反应，对不皂化部分进行硅胶柱色谱的分离和纯化，用IR，MS，¹H-NMR等波谱技术和对照品对照等方法进行化合物的结构鉴定。结果：分离获得并鉴定了7个化合物，分别为栝楼仁二醇(1)、异栝楼仁二醇(2)、5-脱氢栝楼仁二醇(3)、7-氧代二氢栝楼仁二醇(4)、β-谷甾醇(5)、豆甾-7-烯-3β-醇(6)和豆甾-7，22-二烯-3β-醇(7)。结论：这些化合物均系首次从木鳖子中分离获得。     

精制苦瓜提取物的制备及其降糖作用

目的:对苦瓜果汁进行精加工,得到去除其中性寒味苦成分的精制苦瓜提取物,并通过对2型糖尿病大鼠动物试验,比较未去苦味的苦瓜提取物粗品和除去苦味的精制苦瓜提取物的活性差异。方法:使用大孔树脂处理方法,得到无苦味的精制苦瓜提取物。大鼠高脂高糖饮食1个月后,ip链脲佐茵素诱导2型糖尿病。使用精制苦瓜提取物治疗2型糖尿病大鼠,测试其降糖活性作用。结果:精制苦瓜提取物没有苦味,性温;通过活性对比试验,精制苦瓜提取物和苦瓜提取物粗品对2型糖尿病大鼠作用6周后,大鼠体重均明显增加,血糖显著下降,两者无显著性差异。结论:采用大孔树脂吸附的方法既除去苦瓜提取物粗品中的苦味性寒成分,又未见其精制苦瓜提取物在降糖活性方面的明显损失。     

Antidiabetic and adaptogenic properties of Momordica charantia extract: An experimental and clinical evaluation

The hypoglycaemic properties of Mormodica charantia (bitter gourd) water extract was tested on alloxan diabetic rats experimentally. A fall of blood sugar after 3 week's treatment with aqueous extract of fruits of the herb was found to be significant (p<0.01). The aqueous extract of fruit was more effective in diabetes (fall of blood sugar 54% after 3 week's therapy) than the powder of the dried fruit (fall 25% nonsignificant). Hypoglycaemic effects in diabetic patients were found to be highly significant (p<0.01) at the end of the trial but were cumulative and gradual, unlike that produced by insulin. Adaptogenic properties are indicated by the delay in the appearance of cataracts, the secondary complications of diabetes and relief in neurological and other common symptoms even before the hypoglycaemia occurred.     

Effect of Momordica charantia on lipid profile and oral glucose tolerance in diabetic rats

In this study, the methanol extract of Momordica charantia fruit extract was administered to diabetic rats to assess the long term effect of the extract on the lipid profile and the oral glucose tolerance test. Treatment for 30 days showed a significant decrease in triglyceride, low density lipoprotein and a significant increase in high density lipoprotein level. A significant effect on oral glucose tolerance was also noted. Chronic administration showed an improvement in the oral glucose tolerance curve. The effect was more pronounced when the test was done in rats fed the extract on the day of the test compared with tests done in rats which were not fed the extract on the same day.     

Inhibition of P-glycoprotein activity and reversal of cancer multidrug resistance by <Emphasis Type="Italic">Momordica charantia</Emphasis> extract

Purpose Multidrug resistance (MDR) is known as a problem limiting the success of therapy in patients treated long term with chemotherapeutic drugs. The drug resistance is mainly due to the overexpression of the 170 kDa P-glycoprotein (Pgp), which causes a reduction in drug accumulation in the cancer cells. In this study, novel chemical modulator(s) from bitter melon (Momordica charantia L.) extracts obtained from leaves, fruits and tendrils were tested for their abilities to modulate the function of Pgp and the MDR phenotype in the multidrug-resistant human cervical carcinoma KB-V1 cells (high Pgp expression) in comparison with wildtype drug-sensitive KB-3-1 cells (lacking Pgp).Methods The KB-V1 and KB-3-1 cells were exposed to bitter melon extracts in the presence of various concentrations of vinblastine, and cytotoxicity was assessed by means of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay. Relative resistance was calculated as the ratio of the IC₅₀ value of the KB-V1 cells to the IC₅₀ value of the KB-3-1 cells. Accumulation and efflux of vinblastine in KB-V1 and KB-3-1 cells were measured using a [³H]-vinblastine incorporation assay.Results The leaf extracts increased the intracellular accumulation of [³H]-vinblastine in KB-V1 cells in a dose-dependent manner, but extracts from the fruits and tendrils had no effect. By modulating Pgp-mediated vinblastine efflux, the leaf extracts decreased the [³H]-vinblastine efflux in KB-V1 cells in a dose-dependent manner, but not in KB-3-1 cells. Treatment of drug-resistant KB-V1 cells with bitter melon leaf extracts increased their sensitivity to vinblastine, but similar treatment of KB-3-1 cells showed no modulating effect. The fruit and tendril extracts did not affect the MDR phenotype in either cell line.Conclusion The leaf extracts from bitter melon were able to reverse the MDR phenotype, which is consistent with an increase in intracellular accumulation of the drug. The exact nature of the active components of bitter melon leaf extracts remains to be identified.     

Stimulation of protein biosynthesis in rat hepatocytes by extracts of Momordica charantia

The in vivo effect of the administration of extracts of Momordica charantia on certain biochemical parameters of Sprague-Dawley rats was investigated. It was observed that there was an increase in muscle and liver protein levels, while there was a reduction in the levels of brain protein, muscle and liver glycogen. The activities of plasma L-alanine transaminase and alkaline phosphatase were reduced. The L-aspartate transaminase and adenosine triphosphatase activities were slightly elevated in whole plant extract treated rats while the L-aspartate transaminase was unaffected by the ethanol extract but reduced the adenosine triphosphatase activity.