Antidiabetic activity of Boerhaavia diffusa L.: effect on hepatic key enzymes in experimental diabetes

The purpose of this study was to investigate the effects of daily oral administration of aqueous solution of Boerhaavia diffusa L. leaf extract (BLEt) (200 mg/kg) for 4 weeks on blood glucose concentration and hepatic enzymes in normal and alloxan induced diabetic rats. A significant decrease in blood glucose and significant increase in plasma insulin levels were observed in normal and diabetic rats treated with BLEt. Treatment with BLEt resulted in a significant reduction of glycosylated haemoglobin and an increase in total haemoglobin level. The activities of the hepatic enzymes such as hexokinase was significantly increased and glucose-6-phosphatase, fructose-1,6-bisphosphatase were significantly decreased by the administration of BLEt in normal and diabetic rats. An oral glucose tolerance test (OGTT) was also performed in the same groups, in which there was a significant improvement in glucose tolerance in rats treated with BLEt. A comparison was made between the action of BLEt and antidiabetic drug-glibenclamide (600 microg/kg). The effect of BLEt was more prominent when compared to glibenclamide.     

Spasmolytic effects of nonprenylated rotenoid constituents of Boerhaavia diffusa roots

Boerhaavia diffusa is an Ayurvedic remedy used traditionally for the treatment of a number of diseases, including those affecting the gastrointestinal tract. In the current investigation, a methanol extract obtained from roots of B. diffusa exhibited a significant spasmolytic activity in the guinea pig ileum, probably through a direct effect on the smooth muscle. A detailed phytochemical analysis of this methanol extract led to the isolation of one new (12) and six known (6-11) rotenoid derivatives. The structure of the new compound was determined through interpretation of its MS and NMR data. All the isolated rotenoids were evaluated for their effect on intestinal motility in vitro, and the results obtained showed unambiguously that they are active spasmolytic constituents. Preliminary structure-activity relationships for this class of compounds are suggested.     

Studies on the immunomodulatory effects of Boerhaavia diffusa alkaloidal fraction.

The alkaloidal fraction of Boerhaavia diffusa was studied for its effect on cellular and humoral functions in mice. Oral administration of the fraction (25-100 mg/kg) significantly inhibited SRBC-induced delayed hypersensitivity reactions in mice. However, the inhibition was observed only during post-immunisation drug treatment, while no effect during pre-immunisation drug treatment was observed. A significant dose-related increase in antibody titre was observed during pre- and post-immunisation treatment. The alkaloidal fraction failed to show any blastogenic responsiveness of murine splenocytes to Concanvalin A (Con A) and lipopolysaccharide (LPS). Similarly, it did not display any mitogenic activity. Thus, the present study has shown the in vivo immunostimulatory activity of B. diffusa alkaloidal fraction without an in vitro effect.     

The juice of fresh leaves of Boerhaavia diffusa L. (Nyctaginaceae) markedly reduces pain in mice

The decoction or juice of leaves of Boerhaavia diffusa L. (Nyctaginaceae) is used in Martinican folk medicine for its analgesic and anti-inflammatory properties. In the present investigation we studied the acute oral (p.o.) toxicity of a crude extract obtained from a lyophilized decoction (DE) and from the juice (JE) of fresh leaves. We observed no signs of toxicity up to the dose of 5000 mg/kg (p.o.) in mice. At the dose of 1000 mg/kg, neither extract altered sleeping time evoked by the administration of pentobarbital sodium (i.p.). The DE and JE of B. diffusa were assessed in standard rodent models of algesia and inflammation. We investigated the antinociceptive effect of DE and JE in chemical (acetic acid) and thermal (hot plate) models of hyperalgesia in mice. Dipyrone sodium (200 mg/kg), JE (1000 mg/kg) and DE at the same dose (p.o.), produced a significant inhibition of acetic acid-induced abdominal writhing in mice (100, 50 and 47% inhibition, respectively) when compared with the negative control (P<0.001). In the hot-plate test in mice, morphine and JE produced a significant increase in latency during the observation time. The DE, however, only raised the pain thresholds during the first period (30 min) of observation (P<0.05). The extracts of B. diffusa were also investigated for their anti-edematogenic effect on carrageenan-induced edema in mice. However, neither extract inhibited the paw edema induced in mice (P>0.05). In the acetic acid-induced abdominal writhing in mice, pre-treatment of the animals with naloxone (5 mg/kg, i.p.) significantly reversed the analgesic effect of morphine and JE but not that of DE. These data show that the active antinociceptive principle of B. diffusa is present mainly in the juice of fresh leaves and has a significant antinociceptive effect when assessed in these pain models. The mechanism underlying this analgesic effect of fresh leaves of B. diffusa remains unknown, but seems to be related to interaction with the opioid system.     

多糖抗肝损伤作用及其机制研究进展

肝损伤是各种肝脏疾病共有的一种病理状态,其持续恶化会导致肝硬化、肝纤维化、肝癌。因此,寻找对抗肝损伤有效物质受到广泛关注。活性多糖广泛存在于植物、微生物、动物内,具有高效、低毒、副作用小的特点,已成为抗肝损伤天然药物制剂领域的研究热点,也取得了较多的进展。该文从抗肝损伤的多糖类型、肝损伤的发病类型及发病机制等方面对国内外相关文献进行归纳分析,并对多糖在抗肝损伤方面的开发利用前景进行了展望。研究结果显示,植物多糖、动物多糖和微生物多糖具有良好的抗肝损伤效应,主要通过抗自由基损伤、对抗肝细胞钙超载、调节线粒体功能等发挥抗化学性肝损伤功效,和通过调节细胞因子、抑制补体系统激活、抑制炎性介质产生、防止肝细胞凋亡等发挥抗免疫性肝损伤功效。可见多糖具有资源丰富、效应多样、作用靶点多、作用途径广等特性,是潜在的抗肝损伤药物制剂。     

The hepatoprotective activity of kinsenoside from Anoectochilus formosanus

Carbon tetrachloride (CCl(4)) causes chronic hepatitis, featuring an increase in hepatic hydroxyproline, spleen weight and serum GPT levels and a decrease in plasma albumin levels. Crude extracts of fresh whole plants of Anoectochilus formosanus showed inhibition of chronic hepatitis induced by CCl(4) in mice. Bioactivity-guided fractionation and spectroscopic analysis revealed that kinsenoside was the most active compound. In an in vitro study, the LD(50) values for H(2)O(2)-induced cytotoxicity in BALB/c normal liver cells were significantly higher after kinsenoside pretreatment than after vehicle alone, further confirming that kinsenoside shows significant antihepatotoxic activity.     

Anti-inflammatory and hepatoprotective activity of peh-hue-juwa-chi-cao in male rats

Peh-hue-juwa-chi-cao (PHJCC) is a common commercial name for the herbal extract of either Hedyotis diffusa (HD), H. corymbosa (HC), or Mollugo pentaphylla (MP). The present study was carried out to investigate the anti-inflammatory and hepatoprotective effects of these three extracts in rats. The results indicated that extracts of HC, HD and MP possess anti-inflammatory activity, and that MP has the greatest inhibition against carrageenan-induced paw edema. In the hepatoprotective study, results indicated that the three plant extracts significantly reduced the acute elevation of serum glutamate oxalate transaminase (sGOT) and serum glutamate pyruvate transaminase (sGPT) concentration, and alleviated the degree of liver damage 24 hours after the intraperitoneal administration of hepatotoxins.     

Possible mechanism of hepatoprotective activity of Azadirachta indica leaf extract: part II

Hepatoprotective activity of Azadirachta indica leaf extract against paracetamol induced hepatic damage in rats has already been reported. In the present investigation effects of Azadirachta indica leaf extract on blood and liver glutathione, Na+K(+)-ATPase activity and thiobarbutiric acid reactive substances against paracetamol induced hepatic damage in rats have been studied with a view to elucidate possible mechanism behind its hepatoprotective action. It was interesting to observe that Azadirachta indica leaf extract has reversal effects on the levels of above mentioned parameters in paracetamol hepatotoxicity. Possible mechanism behind the results are discussed.     

Clarification of the phenotypic characteristics and anti-tumor activity of Hedyotis diffusa

Hedyotis diffusa Willd. (Rubiaceae) is an important folk herb used to prevent and cure hepatitis and liver cancer in Taiwan. For differentiation of H. diffusa from counterfeits, macroscopic and microscopic characters of H. diffusa, H. corymbosa and H. tenelliflora were examined in this study. According to Trypan blue exclusion assay and Western blot analysis, H. diffusa had a significant inhibition of cell growth and induction of cell apoptosis in COLO 205 (colon cancer), Hep 3B (hepatocellular carcinoma) and H460 (lung cancer) cell lines. This study also used high-performance liquid chromatography (HPLC) to determine the quality control of H. diffusa. The HPLC data showed that ursolic and oleanolic acid are the components of the H. diffusa, consisting of approximately 4.66-4.80% and 1.86-1.96%, respectively. Our study also demonstrated that ursolic acid has significant anti-tumor activity in COLO 205, Hep 3B and H460 cancer cells.     

三白草酮及衍生物的溶解性和保肝活性研究

目的考察三白草酮及衍生物的溶解性和保肝活性。方法采用HPLC测定三白草酮及衍生物在常用溶剂中的溶解度和正辛醇-水/缓冲液体系中的表观脂水分配系数(P);采用CCl4小鼠肝损伤模型考察其保肝活性。结果 25℃时三白草酮及衍生物A、B、C在水中的溶解度分别为(0.161±0.007),(12.4±0.57),(0.145±0.006),(0.667±0.031)mg/L;在正辛醇/水中的lgP分别为(3.32±0.13),(2.63±0.08),(3.28±0.08),(2.76±0.09);衍生物A的保肝降酶活性较三白草酮有所提高,衍生物B与三白草酮相当,衍生物C有肝损伤作用。结论衍生物A的lgP比三白草酮降低较多,可能会通过改善体内吸收提高药效;衍生物C的lgP虽有下降,但三白草酮中一个次甲二氧基被破坏,显示出肝损伤作用。     

Anti-aromatase activity of the constituents from damiana (Turnera diffusa)

Ethnopharmacological relevance

Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac.

Aim of the study

The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from Turnera diffusa.

Materials and methods

The methanolic extract and 24 compounds isolated from the leaves of Turnera diffusa were evaluated for aromatase activity by using a tritiated-water release assay and for estrogenic activity by using yeast estrogen screen (YES) assay.

Results

The methanolic extract demonstrated a dose-dependent inhibitory activity of the aromatase enzyme with the IC₅₀ value of 63.1 μg/ml. Among the 24 tested compounds, pinocembrin and acacetin showed the most potent inhibition with IC₅₀ values of 10.8 and 18.7 μM, respectively. Estrogenic activity was also observed in the extract and three compounds including apigenin 7-glucoside, Z-echinacin and pinocembrin with EC₅₀ values of 10, 20 and 67 μM, respectively.

Conclusions

The extract of Turnera diffusa and two isolated compounds pinocembrin and acacetin could significantly suppress aromatase activity. Moreover, apigenin 7-glucoside, Z-echinacin and pinocembrin showed estrogenic activity.     

五味降酶丸保肝作用的临床研究

目的：评价五味降酶丸治疗慢性乙型肝炎的临床疗效。方法：95例慢性乙型肝炎肝功能异常的患者,采取随机、单盲、治疗前后自身对照的方法,口服五味降酶丸治疗3个月,观察治疗前后肝功能、肝纤维化血清学、肝脾影像学指标的变化。结果：在用药达3个月时,91例患者的血清学指标、影像学指标有不同程度的下降,总有效率达89％。结论：五味降酶丸保肝作用疗效确切,且性价比高,服用安全。     

Antioxidative and in vitro hepatoprotective activity of Bupleurum kaoi leaf infusion

The roots of Bupleurus spp. have been used in traditional Chinese herbal medicine for curing liver diseases. Although bioactive saikosaponins have been detected in the leaves as well as in the roots, the aerial parts of the plants are discarded as waste. In the present study, a leaf infusion of B. kaoi Liu, Chao et Chuang, an indigenous Bupleurus species in Taiwan, was prepared and the antioxidant properties and in vitro hepatoprotective activity were demonstrated. The results show that the leaf infusion exerted DPPH free radical scavenging activity, inhibitory capacity on superoxide anion formation and superoxide anion scavenging activity. The hepatotoxicity of acetaminophen (APAP) and carbon tetrachloride (CCl4) on the rat liver cells were also decreased by the leaf infusion.     

甘草总皂苷的制备及其保肝作用的研究

目的:制备甘草总皂苷,同时探讨甘草总皂苷对四氯化碳致急性肝损伤和DL-乙硫氨酸致急性脂肪肝的保护作用。方法:应用大孔树脂法,富集甘草总皂苷部位。以四氯化碳致小鼠急性肝损伤模型和DL-乙硫氨酸致急性脂肪肝模型,考察甘草总皂苷部位对小鼠血清丙氨酸氨基转移酶ALT及天冬氨酸氨基转移酶AST活性的影响,同时考察其对DL-乙硫氨酸致急性脂肪肝模型肝组织总胆固醇及甘油三酯含量的影响。结果:采用HPD400型大孔树脂,30%乙醇除杂,50%乙醇洗脱可得到总皂苷含量50%以上的甘草总皂苷部位。对四氯化碳致急性肝损伤模型,甘草总皂苷可显著降低CCl4导致的小鼠血清ALT和AST活性的升高;对DL-乙硫氨酸致急性脂肪肝模型,模型组与各治疗组小鼠血清ALT和AST活性与正常对照组之间无显著性差异,而模型组小鼠肝组织总胆固醇和甘油三酯含量显著升高,治疗后又明显降低。结论:甘草总皂苷对CCl4致小鼠急性肝损伤和DL-乙硫氨酸致小鼠急性脂肪肝具有一定的保护作用。     

Glycosmis arborea extract as a hepatoprotective agent

Glycosmis arborea is a plant possessing various medicinal properties. The aim of the present study was to investigate the hepatoprotective efficacy of the butanol extract obtained from the aerial parts of the plant. The test sample was prepared by extracting the material through different steps. The extract thus obtained was dissolved in normal saline. Albino rats were prophylactically treated with the extract (i.p.) for 3 weeks. At the end of 3rd week all the groups were injected with hepatotoxic agents. After 48 h of injection, blood was collected and livers were taken out. Different enzymes in the serum were assayed and histopathological study was performed with liver. Glycosmis arborea extract was able to overcome the toxic effects of hepatotoxic agents in terms of lowering the levels of serum GPT, alkaline phosphatase and increased level of SOD in serum. TBARS generation in liver was also altered. Moreover, necrosis of liver produced by carbon tetrachloride was reversed by the extract.     

Cochlospermum planchonii rhizome extract with hepatoprotective activity inhibits cytochrome P-450 monooxygenases

An aqueous extract of Cochlospermum planchonii rhizomes prepared in the manner used by native medical practitioners in northern Nigeria to treat jaundice protects CCI₄-treated rats from liver damage measured as elevated serum levels of diagnostic enzymes. The extract inhibits cytochrome P-450 monoxygenases aminopyrine-N-demethylase and aniline hydroxylase, suggesting a plausible hepatoprotective mechanism.     

Three new triterpenes from the seeds of Combretum quadrangulare and their hepatoprotective activity

Three new triterpenes of the lupane type, 2alpha,6beta-dihydroxybetulinic acid (1) and 6beta-hydroxyhovenic acid (2), and an oleanane type, 6beta-hydroxyarjunic acid (3), together with several known compounds, have been isolated from the MeOH extract of the seeds of Combretum quadrangulare. The structures of these compounds were elucidated on the basis of spectroscopic analysis, and their hepatoprotective activities were tested for D-GalN/TNF-alpha-induced cell death in primary cultured mouse hepatocytes.     

白花蛇舌草中一新天然成分的来源确证

从茜草科植物白花蛇舌草Oldenlandia diffusa (Willd)Roxb.中分离得一新天然成分 4,4’-二羟基-α-古柯间二酸,为环丁烷衍生物,通过光催化环丁烷加成试验验证,该化合物应为植物体内代谢形成,而不是提取分离过程产生的物质。     

In vivo wound-healing activity of oleanolic acid derived from the acid hydrolysis of Anredera diffusa

Anredera diffusa is used as a wound-healing agent in traditional Peruvian medicine. Acid hydrolysis of the bioactive ethanolic extract, followed by in vivo activity-guided fractionation, yielded oleanolic acid, with a wound-healing activity equivalent to 42.9% (p < 0.01) above the control. The highest cicatrizant activity in mice was obtained by applying 40 microg of oleanolic acid per gram of body weight.     

Phytochemical investigation of Turnera diffusa

A phytochemical investigation of Turnera diffusa afforded 35 compounds, comprised of flavonoids, terpenoids, saccharides, phenolics, and cyanogenic derivatives, including five new compounds (1-5) and a new natural product (6). These compounds were characterized as luteolin 8-C-E-propenoic acid (1), luteolin 8-C-beta-[6-deoxy-2-O-(alpha-l-rhamnopyranosyl)-xylo-hexopyranos-3-uloside] (2), apigenin 7-O-(6' '-O-p-Z-coumaroyl-beta-d-glucopyranoside) (3), apigenin 7-O-(4' '-O-p-Z-coumaroylglucoside) (4), syringetin 3-O-[beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside] (5), and laricitin 3-O-[beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside] (6). Their structures were determined by spectroscopic and chemical methods.