Postnatal development and reproductive performance of F1 progeny exposed in utero to an ayurvedic contraceptive: Pippaliyadi yoga

The purpose of this study was to characterize the putative anxiolytic-like activity of an ethanolic extract prepared from the leaves of Apocynum venetum (AV) using the elevated plus maze (EPM) in mice. Male C75BL/6 mice were either treated orally with the AV extract or the positive controls diazepam and buspirone, respectively, 1 h before behavioral evaluation in the EPM. A single treatment of AV extract markedly increased the percentage time spent on and the number of entries into the open arms of the EPM in doses of 30 and 125 mg/kg p.o., respectively. This effect was comparable to that of the benzodiazepine diazepam (1.5 mg/kg p.o.) and the 5-HT_1A agonist buspirone (10 mg/kg p.o.). The effects of AV in 125 mg/kg were effectively antagonized by the benzodiazepine antagonist flumazenil (3 mg/kg i.p.). However, the effects of AV extract could only partially be blocked by the unspecific 5-HT_1A receptor antagonist WAY-100635 (0.5 mg/kg i.p.). Neither diazepam and buspirone nor the AV extract produced any overt behavioral change or motor dysfunction in the open field test. These results indicate that AV extract is an effective anxiolytic agent, and suggest that the anxiolytic-like activities of this plant are mainly mediated via the GABAergic system.     

Constituents from leaves of Apocynum venetum L.

An analysis using HPLC–MS revealed that an extract from dried leaves of Apocynum venetum L. contained more than 15 kinds of phenolic constituents. Two malonated flavonol glycosides were further isolated, and their structures were determined to be quercetin 3-O-(6′′-O-malonyl)-β-d-glucoside (1) and quercetin 3-O-(6′′-O-malonyl)-β-d-galactoside (2) by NMR spectroscopic analysis. This is the first report describing the isolation of these malonated flavonol glycosides from A. venetum L. Both glycosides showed strong scavenging activity against 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical.     

罗布麻叶黄酮类成分的研究

目的：对罗布麻叶黄酮类成分进行研究。方法：利用反复的聚酰胺柱色谱分离和Sephadex LH-20柱色谱纯化,通过波谱分析鉴定化合物的结构。结果：分离并鉴定6个化合物,分别是：槲皮素(1),山柰酚(2),山柰酚-3-O-(6″-O-乙酰基)-β-D-吡喃葡萄糖苷(3),槲皮素-3-O-(6″-O-乙酰基)-β-D-吡喃葡萄糖苷(4),槲皮素-3-O-(6″-O-乙酰基)-β-D-吡喃半乳糖苷(5),山柰酚-7-O-α-L-吡喃鼠李糖苷(6)。结论：化合物5,6为首次从该属中分离得到。     

星点设计-效应面法优选罗布麻叶总黄酮提取工艺

目的：采用星点设计-效应面法优化罗布麻总黄酮的提取工艺。方法：在预实验及单因素试验基础上,采用乙醇回流提取,并以乙醇体积分数、提取时间、料液比为自变量,罗布麻总黄酮得率为因变量,利用星点设计模型进行多元线性回归和二项式拟合,确定罗布麻的最佳提取工艺。结果：罗布麻的最佳提取工艺为23倍量65%乙醇,提取2次,150 min/次。得率实测值与预测值偏差为-1.60%,二项式拟合r=0.9870。结论：星点设计-效应面法优化罗布麻总黄酮提取工艺,方法简便,合理可行,预测性良好。     

罗布麻花化学成分研究

目的研究新疆产罗布麻花的化学成分。方法硅胶柱色谱和薄层色谱进行分离和纯化,通过理化性质和光谱分析鉴定其结构。结果从罗布麻花中分离鉴定了3个香豆素类和6个黄酮类化合物,分别为东莨菪素(Ⅰ)、异白蜡树定(Ⅱ)、秦皮甲素(Ⅲ)、山柰酚(Ⅳ)、槲皮素(Ⅴ)、槲皮素-3-O-β-D-葡萄糖苷(Ⅵ)、山柰酚-3-O-β-D-吡喃葡萄糖苷(Ⅶ)、芸香苷(Ⅷ)、β-胡萝卜苷(Ⅸ)。结论以上Ⅰ～Ⅲ、Ⅷ、Ⅸ化合物为首次从该植物花中分离而得。     

罗布麻茶毒理学安全性评价

目的评价罗布麻茶的安全性。方法依据食品安全性毒理学评价程序和方法进行急性毒性试验、Ames试验、骨髓细胞微核试验、精子畸形试验和30 d喂养试验。结果小鼠经口MTD30.0 g/kg.bw,属无毒级;Ames试验、骨髓细胞微核试验和精子畸形试验结果均为阴性;30 d喂养试验中各项指标均未见异常。结论在本试验条件下,罗布麻茶是安全的。     

罗布麻叶总黄酮提取物对小鼠的抗抑郁作用的研究

目的对传统中药罗布麻进行抗抑郁活性评价,并对其作用机制进行研究。方法采用经典抗抑郁评价模型小鼠强迫游泳实验对罗布麻叶总黄酮进行抗抑郁活性评价,在此基础上,应用皮质酮损伤PC12细胞模型,采用MTT法、LDH检测法观察罗布麻提取物对皮质酮损伤的PC12细胞是否具有神经保护作用。结果在小鼠强迫游泳实验中,罗布麻提取物100,50,26 mg/kg(i.g.)连续给药10 d后,能显著缩短小鼠的强迫游泳不动时间(分别为P<0.001,P<0.05,P<0.01);同时罗布麻叶总黄酮提取物对皮质酮损伤的PC12细胞具有神经保护作用。结论罗布麻叶总黄酮具有抗抑郁作用,其机理可能与神经细胞的保护作用有关。     

罗布麻叶水提物镇静催眠作用研究

目的 探讨罗布麻叶水提物（water extract of Apocynum venetum leaves,AVLWE）镇静催眠作用及机制。方法 随机将ICR小鼠分为对照组、右佐匹克隆（阳性药,0.40 mg·kg^-1）组和AVLWE低、中、高剂量（0.58、1.17、2.34 g·kg^-1）组,每天ig给药1次,连续4周,每周称体质量;于末次给药前1 d给药60 min后,应用旷场视频分析系统检测各组小鼠5 min自主活动;于末次给药45 min后,各组动物ip 1%戊巴比妥钠（35 mg·kg^-1,阈下催眠剂量）,记录30 min内入睡潜伏期、入睡动物数、睡眠时间;结束后麻醉处死动物,取脑称质量并计算脑系数。SD大鼠分为对照组、模型组、右佐匹克隆（阳性药,0.27 mg·kg^-1）组和AVLWE低、中、高剂量（0.40、0.81、1.62 g·kg^-1）组,每天ig给药1次,连续4周,每周称体质量;除对照组外,给药第28、29天ip对氯苯丙氨酸（PCPA）制备大鼠失眠模型,给药结束称取脑质量并计算脑系数,取下丘脑,ELISA试剂盒法测定5-羟色胺（5-HT）、多巴胺（DA）和5-羟吲哚乙酸（5-HIAA）的含量。结果 小鼠实验结果表明,与对照组比较,各给药组第1~4周体质量均显著降低（P<0.01）;右佐匹克隆片和AVLWE中、高剂量组睡眠发生率均显著增加（P<0.05、0.01）;右佐匹克隆片和AVLWE中、高剂量组睡眠时间显著延长（P<0.05）;AVLWE低、中、高剂量组脑系数均显著升高（P<0.01）。大鼠实验结果表明,与对照组比较,AVLWE高剂量组第1~4周体质量均显著降低（P<0.05、0.01）;与模型组比较,AVLWE高剂量组脑系数显著升高（P<0.05）;右佐匹克隆片组、AVLWE高剂量组DA水平显著降低（P<0.05）、5-HIAA水平显著升高（P<0.01）,AVLWE低、中、高剂量组5-HT水平显著升高（P<0.05、0.01）。结论 AVLWE具有改善睡眠的作用,机制可能与上调下丘脑5-HT水平、下调DA水平有关。     

Apocynum venetum leaf extract, an antihypertensive herb, inhibits rat aortic contraction induced by angiotensin II: A nitric oxide and superoxide connection

Ethnopharmacological relevance

The leaves extract of Apocynum venetum (AVLE), also known as “luobuma”, have long been used in traditional Chinese medicine to treat hypertension and depression in parts of China and it has been shown to possess anti-oxidant and anti-lipid peroxidation effects. AVLE (10 μg/ml) has been reported to have a long-lasting endothelium-dependent relaxant effect and this effect has been proposed to be due to its nitric oxide(NO)-releasing and superoxide anion(SOA)-scavenging properties.

Aim of the study

The present study seeks to evaluate the differential actions of AVLE extract between Ang II- and PE-induced vasoconstriction and the involvement of superoxide anions.

Materials and methods

Single dose of Ang II (100 nM and 1 nM)- or PE (0.1 μM)-induced contraction were assessed in both endothelium-intact and -denuded aortic rings after pre-incubation of AVLE (10 μg/ml) for 15 min. The experiment was repeated in either the presence of NO synthase inhibitor, l-NAME (300 μM) or selective AT₁ receptor inhibitor, losartan (0.1 nM), or superoxide scavenger, tiron (1 mM) or a combination of l-NAME and AVLE. Superoxide production was measured by using enhanced-chemiluminescence assay.

Results

We have demonstrated that AVLE (10 μg/ml) effectively suppressed the Ang II-induced contraction (100 nM and 1 nM) of both endothelium-intact and -denuded rat aortic rings. In endothelium-intact rings, l-NAME, reversed AVLE-induced inhibition of Ang II-contraction. PE-induced contraction was significantly inhibited by AVLE in endothelium-intact rings, but not in endothelium-denuded rings. The inhibition by AVLE of PE-induced contraction was totally abolished in the presence of l-NAME. Ang II-induced SOA production concentration dependently with the optimal effect seen at 100 nM of Ang II, and AVLE (0.3, 1, 10 μg/ml) reduced this effect. SOA production in Ang II-stimulated rings was significantly higher than unstimulated control rings, while PE did not stimulate SOA production at all. SOA formation in the presence of Ang II was also inhibited in the presence of SOD (superoxide scavenger), DPI (NADPH inhibitor) and losartan (specific AT₁ receptor antagonist).

Conclusion

These results collectively suggest that the ability of AVLE in inhibiting Ang II-induced contraction via its SOA scavenging properties and nitric oxide releasing effect may account for its usage as an antihypertensive treatment in traditional folk medicine.     

罗布麻叶浸膏对脑内单胺类递质含量及细胞膜流动性的影响

罗布麻叶浸膏可使脑内５－ＨＴ及ＤＡ含量升高,其水溶性成分可使５－ＨＴ、５ＨＩＡＡ及ＤＡ含量升,而ＮＥ含量降低,醇溶性成分上述作用更为明显。