胡芦巴药材HPLC指纹图谱的初步研究

 目的研究胡芦巴药材的高效液相指纹图谱,为科学评价及有效控制药材的质量提供了可靠的方法。方法利用高效液相色谱法,梯度洗脱,测定了14个不同产地的胡芦巴药材样品。色谱条件为:Alltech C₁₈柱(4.6 mm×250 mm,5μm),流动相:乙腈-水,流速:1 mL·min^-1,检测波长:211 nm。结果各产地胡芦巴药材指纹图谱有21个共有峰,峰面积之和大于总峰面积的90%,经相似度计算,各产地药材之间的相似性良好。结论方法灵敏度高,重现性好,可作为控制胡芦巴药材内在质量的标准。     

胡芦巴黄酮苷及其降血糖活性的研究

 目的研究胡芦巴中芹菜素黄酮苷的化学结构及其降血糖活性。方法采用萃取、制备色谱和柱色谱方法分离和纯化化合物,结合化学分析及其波谱数据进行结构鉴定。采用四氧嘧啶糖尿病小鼠模型进行抗糖尿病活性评价。有效亚组分(CⅡ-4)灌胃途径给予糖尿病小鼠,剂量为50mg·kg^-1,连续给药17d。结果CⅡ-4主要含有4个芹菜素黄酮苷,结构分别为:芹菜素6-C-β-D-葡萄糖-8-C-β-D-半乳糖苷、芹菜素-6-C-β-D-葡萄糖8-C-α-L-阿拉伯糖苷、芹菜素-6-C-β-D-半乳糖-8-C-α-L-阿拉伯糖苷和芹菜素-6、8-二-C-β-D-葡萄糖苷。CⅡ-4具有显著降血糖和降血脂作用,能提高糖尿病小鼠胰腺重量指数,促进肝糖原的合成。结论该亚组分的4个化合物首次从该植物中分离得到,可能是胡芦巴的抗糖尿病有效成分之一。     

A novel Gymnema sylvestre extract stimulates insulin secretion from human islets in vivo and in vitro

Many plant‐based products have been suggested as potential antidiabetic agents, but few have been shown to be effective in treating the symptoms of Type 2 diabetes mellitus (T2DM) in human studies, and little is known of their mechanisms of action. Extracts of Gymnema sylvestre (GS) have been used for the treatment of T2DM in India for centuries. The effects of a novel high molecular weight GS extract, Om Santal Adivasi, (OSA®) on plasma insulin, C‐peptide and glucose in a small cohort of patients with T2DM are reported here. Oral administration of OSA® (1 g/day, 60 days) induced significant increases in circulating insulin and C‐peptide, which were associated with significant reductions in fasting and post‐prandial blood glucose. In vitro measurements using isolated human islets of Langerhans demonstrated direct stimulatory effects of OSA® on insulin secretion from human ?‐cells, consistent with an in vivo mode of action through enhancing insulin secretion. These in vivo and in vitro observations suggest that OSA® may provide a potential alternative therapy for the hyperglycemia associated with T2DM. Copyright © 2010 John Wiley & Sons, Ltd.     

葫芦巴总皂苷联合磺脲类降糖药治疗2型糖尿病36例临床观察

目的:观察葫芦巴总皂苷(TFGs)与磺脲类降糖药(SU)合用对继发性失效2型糖尿病(T2DM)的临床疗效。方法:72例单纯使用SU血糖控制不良的T2DM患者,按就诊顺序随机分为对照组(36例)和治疗组(36例),在服用SU的基础上,分别加服安慰剂和TFGs,观察其疗效。结果:治疗组总有效率明显高于对照组(P<0.01);与治疗前相比,治疗组空腹血糖、餐后2 h血糖、糖化血红蛋白、临床症状积分显著下降(P均<0.01),体重指数和肝肾功能无明显变化。结论:TFGs联合SU治疗T2DM,显示了较好的降糖效果,同时能改善临床症状,且有较好的安全性。     

Contraceptive efficacy of Carica papaya seed extract in male mice (Mus musculus)

The effects of an aqueous extract of Carica papaya seeds (20 mg/kg body weight/animal/day orally and 5 mg/kg body weight/animal/day i.m. for 60 days) were investigated for contraceptive efficacy and other related side effects in male albino mice, Mus musculus. The data revealed that the extract might be causing an androgen deprived effect to target organs resulting in alterations in the internal milieu of the cauda epididymis especially. The treatment did not, however, affect the testicular sperm count suggesting that it acted at the post-testicular level which lead to a reduction of cauda epididymal sperm motility and thus the treatment brought about a significant reduction in fertility rate. The induced effects were transient and reversible upon withdrawal of the treatment, elucidating that functional sterility could be induced by the aqueous papaya seed extract in rodents.     

Mutagenicity and oral toxicity studies of Terminalia chebula

The fruit of Terminalia chebula Retz. (T. chebula), which is a member of the Combfreetaceae family, is used widely in Asian countries as a traditional folk medicine, and its extract has been reported to be an anticancer, antidiabetic and anticaries agent. In our previous study, chebulic acid isolated from T. chebula extract was confirmed to show antioxidant activity and protective action against endothelial cell dysfunction. In order to support the safety‐in‐use of the ethyl acetate (EtOAc)‐soluble portion of a T. chebula ethanol extract containing 29.4% chebulic acid content, the prepared portion was tested in an in vitro mutagenicity assay, and a single‐ and 14‐day repeated dose oral toxicity study. In the bacterial mutation assay, up to 5000 µg/mL concentration of the EtOAc‐soluble portion, the numbers of colonies did not increase whether with or without metabolic activation. In the oral toxicity study, the single oral dose of the extract at 2000 mg/kg did not produce mortality or abnormal lesions in the internal organs of rats. The results of a 14‐day orally repeated dose showed that the EtOAc‐soluble portion of T. chebula ethanol extracts gave no adverse effects at dosages of 2000 mg/kg in rats in the study. Copyright © 2011 John Wiley & Sons, Ltd.     

Screening of plants used in Danish folk medicine to treat depression and anxiety for affinity to the serotonin transporter and inhibition of MAO-A

Ethnopharmacological relevance

A number of plant species are used in Danish folk medicine for treatment of depression and anxiety.

Materials and methods

Aqueous and ethanolic extracts of 17 plant species were tested for affinity to the serotonin transporter and for inhibition of MAO-A—both targets for antidepressive treatment.

Results

An ethanolic extract of aerial parts of Borago officinalis had affinity to the serotonin transporter. Ten extracts, from eight plants, had IC₅₀ values below 25 μg/ml extract in the MAO-A assay. The most active extracts in the MAO-A assay were the ethanol extract of seeds of Trigonella foenum-graecum (IC₅₀ 4 μg/ml); ethanol extract of leaves of Apium graveolens (IC₅₀ 5 μg/ml) and the water extract of aerial parts of Calluna vulgaris (IC₅₀ 8 μg/ml).

Conclusions

Besides Borago officinalis, which toxicity profile excludes it from further development as an herbal drug, none of the plants had potential as serotonin reuptake inhibitors. Several plants had MAO-A inhibitory activity.     

Inhibition of hepatic neoglucogenesis and glucose-6-phosphatase by aqueous extract of Bauhinia megalandra leaves

An aqueons extract of Bauhinia megalandra leaves causes a decrease of nearly 50% in the glucose production, from lactate or fructose, of rat liver slices incubated in Krebs-Ringer bicarbonate buffer supplemented with oleate-saturated albumin. In intact microsomes, the B. megalandra extract acts as a mixed non-competitive inhibitor of glucose-6-phosphatase. In the histone-disrupted microsomes the extract has no effect on glucose-6-phosphate hydrolysis. However in the presence of the extract, glucose-6-phosphatase activity was linear with time, as in the control, but at a lower level, reaching a plateau after 20 min. This suggests an inhibition of the catalytic subunit by accumulation of orthophosphate and/or glucose, as a consequence of the inhibition of its translocases (T2 and/or T3 respectively). Neither the intact nor the disrupted microsomal pyrophosphatase kinetics parameters were affected by the inclusion of the leaf extract. The above results strongly suggest that the main effect of the B. megalandra extract is the inhibition of the glucose-6-phosphate transporter (T1) of the microsomal glucose-6-phosphatase system; however, an inhibition of T3 was not ruled out. The glucose-6-phosphatase inhibition might explain the decrease in the liver slices neoglucogenic capacity and in turn could reduce glucose levels in diabetic patients. © 1998 John Wiley & Sons, Ltd.     

Antinociceptive effects of Trigonella foenum-graecum leaves extract

There are some reports concerning the antinociceptive effects of the plant Trigonella foenum-graecum (TFG) in Iranian traditional medicine. Because of the side effects of nonsteroidal anti-inflammatory and antinociceptive drugs, and in search for more potent and less harmful compounds, we tried to study the antinocicptive effects of TFG leaves by using tail-flick and formalin tests. Intraperitoneal (i.p.) administration of 500 mg/kg of TFG extract and 100 and 300 mg/kg of sodium salicylate (SS), as a positive control, did not show any effect in the tail-flick test, but the 1000 and 2000 mg/kg of the extract produced significant increase in the tail-flick latency. SS (300 mg/kg, i.p.) induced antinociception in the second phase of the formalin test. TFG (500 mg/kg, i.p.) demonstrated antinociception only in the first phase, but 1000 and 2000 mg/kg, i.p. doses alleviated the pain in both phases. Preliminary LD₅₀ of the extract was very close to 4000 mg/kg, i.p. We conclude that: (1) the extract of TFG leaves produces antinociceptive effects through central and peripheral mechanisms; (2) the antinociceptive effects of 2000 mg/kg of the extract was more potent than 300 mg/kg of SS.     

Promotion of Hair Growth by Rosmarinus officinalis Leaf Extract

Topical administration of Rosmarinus officinalis leaf extract (RO‐ext, 2 mg/day/mouse) improved hair regrowth in C57BL/6NCrSlc mice that experienced hair regrowth interruption induced by testosterone treatment. In addition, RO‐ext promoted hair growth in C3H/He mice that had their dorsal areas shaved. To investigate the antiandrogenic activity mechanism of RO‐ext, we focused on inhibition of testosterone 5α‐reductase, which is well recognized as one of the most effective strategies for the treatment of androgenic alopecia. RO‐ext showed inhibitory activity of 82.4% and 94.6% at 200 and 500 µg/mL, respectively. As an active constituent of 5α‐reductase inhibition, 12‐methoxycarnosic acid was identified with activity‐guided fractionation. In addition, the extract of R. officinalis and 12‐methoxycarnosic acid inhibited androgen‐dependent proliferation of LNCaP cells as 64.5% and 66.7% at 5 µg/mL and 5 μM, respectively. These results suggest that they inhibit the binding of dihydrotestosterone to androgen receptors. Consequently, RO‐ext is a promising crude drug for hair growth. Copyright © 2012 John Wiley & Sons, Ltd.     

胡芦巴多糖及低聚糖调血脂活性研究

目的 考察胡芦巴多糖及其酶解产物低聚糖的调血脂活性,并初步探讨其作用机制.方法 体外测定胡芦巴多糖、低聚糖与胆固醇胶束结合的活性;高脂饮食制备高血脂大鼠模型,造模动物分别喂饲拌有胡芦巴多糖或低聚糖(质量分数2.5%)的高脂饲料,给药8周后收集各组大鼠粪便1周,给药9周后取各组大鼠血清和肝脏,检测血清中血脂各项指标及肝功能指标,检测血清中抗氧化活性相关指标,HE染色观察肝组织病理变化,检测粪便中胆固醇及胆汁酸(TBA)的排泄量.结果 胡芦巴多糖及低聚糖体外均表现出一定的胆固醇胶束结合活性;胡芦巴多糖及低聚糖均可降低高血脂大鼠血清总胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-C)水平,同时升高血清中高密度脂蛋白胆固醇(HDL-C)水平;胡芦巴多糖及低聚糖对高血脂大鼠肝脏脂肪变性有改善作用;同时能提高高血脂大鼠血清超氧化物歧化酶(SOD)活性,促进TBA排泄.结论 胡芦巴多糖及低聚糖均具有明确的调血脂活性,其机制与抗氧化和调节胆固醇-TBA动态平衡有关,调血脂活性酶解产物低聚糖作用较优.     

Thereapeutic response of Tribulus terrestris (gokhru) aqueous extract on hyperoxaluria in male adult rats

The effect of an aqueous extract of Tribulus terrestris (an indigenous drug) administered orally at a dose of 5 g/kg body weight was studied in six male adult rats in whom hyperoxaluria was induced and maintained by hydroxyproline and sodium glycolate respectively. Twenty-four hour urinary oxalate excretion reversed to normal, from 1.97±0.314 to 0.144±0.004 mg/mg creatinine (p<0.01) within 21 days of administration of T. terrestris extract and remained so until 15 days after withdrawal of extract and sodium glycolate.     

Red ginseng extract improves coronary flow reserve and increases absolute numbers of various circulating angiogenic cells in patients with first ST‐segment elevation acute myocardial infarction

The effects of red ginseng extract on circulating angiogenic cell mobilization and improvement of microvascular integrity were evaluated in ST‐elevation acute myocardial infarction (AMI) patients during 8‐month follow‐up. AMI patients (n = 50) were randomly assigned to the red ginseng group (3 g/day, n = 25) or the placebo group (n = 25) after coronary stenting. Coronary flow reserve (CFR) was measured at baseline and at 8 months with an intracoronary Doppler wire. Serial changes in the absolute numbers of circulating angiogenic cells such as CD34⁺, CXCR4⁺, CD117⁺, CD133⁺ and C‐met⁺ were measured at baseline, 1 day, 5 days and at 8 months. CFR were similar between the two groups at baseline, and CFR was significantly higher in the red ginseng group than in the placebo group (2.80 ± 0.91 and 2.56 ± 0.77, p < 0.05, respectively) after 8 months of red ginseng administration. The absolute numbers of circulating CD34⁺, CXCR4⁺ and CD117⁺ cells were significantly higher in the red ginseng group at 1 and 5 days after stenting. Significant positive correlations were found between the numbers of circulating angiogenic cells at day 1 and the changes from baseline in CFR for CD34⁺, CXCR4⁺, CD117⁺ and C‐met⁺ cells. Red ginseng extract increased CD34⁺, CXCR4⁺ and CD117⁺ circulating angiogenic cell mobilization and decreased inflammation in AMI patients, thereby improving CFR during the 8‐month follow‐up. Copyright © 2010 John Wiley & Sons, Ltd.     

Effects of three different doses of a fruit extract of Terminalia chebula on metabolic components of metabolic syndrome,in a rat model

There is documented evidence of the use of Terminalia chebula for various ailments in the Ayurvedic literature. The extract has been shown to possess glucose lowering activity and to improve insulin sensitivity in animal models of type 2 diabetes mellitus. The present study was carried out to study the dose response relationship of this extract in a rat model of metabolic syndrome. Six groups of rats were fed a high fructose diet (HFD) for a period of 20 days to induce metabolic syndrome. Three doses of fruit extract of T. chebula 50, 100 and 200 mg/kg were administered orally and pioglitazone 2.7 mg/kg was used as a positive control. Blood samples were collected at days 0, 20 and 40 from the tail vein. Systolic blood pressure (SBP) was measured using the tail cuff method and an oral glucose tolerance test (OGTT) was done on the day of blood collection. Administration of HFD for 20 days significantly increased fasting blood glucose (FBG), SBP and the area under the curve of OGTT. On day 40 the FBG in the 50, 100 and 200 mg/kg group was 97.33 ± 5.82 (NS), 86.83 ± 5.08 (p = 0.038) and 85.67 ± 6.74 (p = 0.15), respectively. These results show that the fruit extract of T. chebula exerts a significant and dose‐dependent glucose lowering effect in the rat model of metabolic syndrome. Copyright © 2009 John Wiley & Sons, Ltd.     

Uncaria tomentosa aqueous-ethanol extract triggers an immunomodulation toward a Th2 cytokine profile

Uncaria tomentosa (Willd.) DC (Rubiaceae) is a large woody vine that is native to the Amazon and Central American rainforests and is used widely in traditional medicine for its immunomodulatory and antiinflammatory activities. The present work used in vivo immunotoxic and in vitro immunomodulatory experiments to investigate the effects of a pentacyclic oxindole alkaloid extract from U. tomentosa bark on lymphocyte phenotype, Th1/Th2 cytokine production, cellular proliferation and cytotoxicity. For the in vivo immunotoxicity testing, BALB/c male mice were treated once a day with 125, 500 or 1250 mg/kg of U. tomentosa extract for 28 days. For the in vitro protocol, lymphocytes were cultured with 10–500 μg/mg of the extract for 48 h. The extract increased the cellularity of splenic white pulp and the thymic medulla and increased the number of T helper lymphocytes and B lymphocytes. Also, a large stimulatory effect on lymphocyte viability was observed. However, mitogen‐induced T lymphocyte proliferation was significantly inhibited at higher concentrations of U. tomentosa extract. Furthermore, an immunological polarization toward a Th2 cytokine profile was observed. These results suggest that the U. tomentosa aqueous‐ethanol extract was not immunotoxic to mice and was able to modulate distinct patterns of the immune system in a dose‐dependent manner. Copyright © 2011 John Wiley & Sons, Ltd.     

The effects of Cernitin® on inflammatory parameters and benign prostatic hyperplasia: An in vitro study

The pollen extract Cernitin® is widely used for treatment of benign prostatic hyperplasia (BPH) and non‐bacterial chronin prostatitis. However, little is known about the underlying molecular mechanisms to explain the clinical effects of Cernitin®. In this study, we sought to investigate the cellular mechanisms by which Cernitin® induces its effects on human prostatic cell lines BPH‐1 and WPMY‐1 and primary human peripheral blood mononuclear cells (hPBMCs) in vitro. We examined the effects of Cernitin® formulas T60 and GBX on the protein expression, proliferation, and cytokines production. Results revealed that Cernitin® upregulated antiinflammatory cytokine interleukin (IL)‐10 and its receptors IL‐10RA and IL‐10B in addition to the upregulation of tumour necrosis factor‐related apoptosis‐inducing ligand in hPBMC. Interestingly, the levels of proinflammatory cytokines IL‐6 and IL‐8 were also increased. Furthermore, Cernitin® had significantly increased the level of IL‐10 in BPH‐1 and WPMY‐1 cells. The level of IL‐6 was also significantly increased in these cells although both T60 and GBX inhibited STAT‐3 phosphorylation. Moreover, Cernitin® formulas had significantly reduced androgen receptor and prostate‐specific antigen protein expression in stromal cells (p < .05). Treatment with GBX and T60 had significantly inhibited proliferation of BPH (p < .001) and stromal cells (p < .05), in a dose‐dependent manner. Taken together, treatment with Cernitin® showed to regulate cytokines level in both prostatic cell lines and hPBMCs and it was associated with decreased androgen receptor and prostate‐specific antigen levels WPMY‐1 cells.     

生品和蜜炙款冬花不同提取物的镇咳祛痰作用

目的:研究款冬花生品与蜜炙品不同溶媒提取物的镇咳、祛痰作用.方法:镇咳实验:昆明种小鼠,随机分成空白、阴性(溶剂)对照、阳性枸橼酸喷托维林对照组(0.01 g·kg-1)、生品和蜜炙款冬花(按生药量计,下同)水提物高、低剂量组(6.20,3.10 g·kg-1)、醇提取物高、低剂量组(6.0,3.0 g·kg-1)、乙酸乙酯和石油醚提取物高、低剂量组(0.5,0.25 g·kg-1).给药体积为25 mL·kg-1,连续ig给药5d,然后观察25％浓氨水定量喷雾后出现咳嗽的潜伏期及2 min内的咳嗽次数.祛痰实验:SD大鼠随机分成空白、阴性、阳性氯化铵对照组(0.16 g·kg-1)、生品和蜜炙款冬花水提物高、低剂量组(2.70,1.35 g·kg-1);醇提物高、低剂量组(3.0,1.5 g·kg-1)、乙酸乙酯和石油醚提取物高、低剂量组(0.25,0.125 g·kg-1).给药体积为25mL· kg-,连续ig给药3d,毛细玻管法记录末次给药后2h大鼠痰液分泌量.结果:与模型对照组相比,生品和蜜炙款冬花醇提物镇咳效果显著,咳嗽潜伏期明显延长(P＜0.05),咳嗽次数明显减少(P＜0.01).两者水提物也有部分镇咳作用.与模型对照组痰量相比,蜜炙款冬花水提物高、低剂量组,生款冬花乙酸乙酯提取低剂量组,蜜款冬花乙酸乙酯提取物高剂量组痰量明显增多(P＜0.05).此外,生款冬花各溶媒提取物组小鼠体重下降显著(P＜0.05).结论:款冬花具有镇咳、祛痰作用.其镇咳成分极性较大,易溶于水和乙醇;祛痰成分极性较小,脂溶性较大.生款冬花各溶媒提取物可能具有一定毒性.     

Antiinflammatory activity and effects on isolated smooth muscle of extracts from different Teucrium species

The present study analyses the antiinflammatory effects and the action on in vitro motility of methanol and dichloromethanol extracts and stems of four Teucrium species (T. flavum, T. cartaginenses, T. buxifolium and T. pumillum). The antiinflammatory activity was tested in the carrageenan-induced paw oedema in rats. T. flavum methanol (200 mg/kg, i.p.) and dichloromethanol (138 mg/kg, i.p.) extracts showed a significant anti-inflammatory effect through the 24 h experimental period and reduced the E_max induced by histamine and serotonin in vitro on guinea-pig ileum and rat uterus respectively. These extracts did not modify the contractile effects induced by acetylcholine on rat duodenum and noradrenaline on rat vas deferens. The methanol extracts of T. pumillum (50 mg/kg, i.p.) and T. buxifolium (26 mg/kg, i.p.) exhibited significant antiinflammatory effects only in the acute phase of the oedema (2 h) without affecting the chronic phase (24 h). In guinea-pig ileum, rat uterus and rat vas deferens, the methanol extract of T. pumillum reduced the maximal effect induced by histamine, serotonin and noradrenaline, respectively, whereas the methanol extract of T. buxifolium lacked any effect on the contractile activity induced by various agonists in vitro. When tested for antiinflammatory activity the methanol (200 mg/kg, i.p.) and dichloromethanol (200 mg/kg, i.p.) extracts of T. cartaginenses did not modify the oedematous response induced by carrageenan administration.     

Antifertility Effects of Aqueous and Steroidal Extracts of Neem Leaf (Azadirachta indica) in Male Wistar Rats

The antifertility efficacy of both aqueous and steroidal extracts of neem ( Azadirachta indica A. Juss) leaves was studied in male Wistar rats. Intraperitoneal injections of the steroidal extract at a dose of 100 mg/kg body weight, twice a week for 10 weeks resulted in impaired spermiogenesis, increased the number of headless spermatozoa and significantly decreased ( p <0.01) motility of cauda spermatozoa, leading to a decline in the fertility index. Feeding of a 0.8% (w/v) aqueous neem leaf extract in drinking water for 7 weeks decreased serum testosterone ( p <0.01) but no effect was observed in the fertility index. © 1997 by John Wiley & Sons, Ltd.