Comparative pharmacokinetic investigation on baicalin and wogonoside in type 2 diabetic and normal rats after oral administration of traditional Chinese medicine Huanglian Jiedu decoction

Ethnopharmacological relevance

Huanglian Jiedu decoction (HLJDD) is used traditionally in China for the treatment of diabetes mellitus in clinical practice, which has been proved to be effective. The purpose of this study was to investigate the pharmacokinetic characteristics (especially the area under the curve, AUC) of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract and to explore its possible mechanism.

Materials and methods

HLJDD extract and Radix scutellariae extract were prepared and the contents of baicalin and wogonoside contained in two extracts were assayed with high performance liquid chromatography (HPLC). Type 2 diabetic rats were induced by high fat diet and intraperitoneal injection of streptozotocin. Pharmacokinetics of baicalin and wogonoside in type 2 diabetic and normal control rats after oral administration of HLJDD extract or Radix scutellariae extract were investigated. Pharmacokinetics of baicalin in type 2 diabetic and normal rats after oral administration of pure baicalin was also investigated.

Results

The pharmacokinetic parameters (especially AUCs) of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract were remarkably different from those in normal rats. And the alterations of the AUCs of baicalin and wogonoside in type 2 diabetic rats after oral administration of Radix scutellariae extract were similar to those after oral administration of HLJDD extract. Moreover, the increase of the AUC of baicalin in type 2 diabetic rats after oral administration of pure baicalin was similar to that after oral administration of HLJDD extract or Radix scutellariae extract.

Conclusion

The pharmacokinetic behaviors of baicalin and wogonoside (especially the systemic exposure [AUCs] of baicalin and wogonoside) were significantly altered in type 2 diabetic rats after orally administrated HLJDD extract. And the increased AUCs of baicalin and wogonoside in type 2 diabetic rats after oral administration of HLJDD extract resulted from neither the effects of other herbs contained in HLJDD nor the effects of other components contained in Radix scutellariae. It might result from the effects of the pathological status of type 2 diabetes mellitus.     

Yeast exposure in the preparation of steamed rehmannia root improving its effects on alloxan-induced diabetic rats

Ethnopharmacological relevance

The root of Rehmannia glutinosa (Gaertn.) DC. has been used in China for more than 2000 years to treat various diseases including diabetes mellitus (DM) and its complications. Steamed rehmannia root (SRR) is one of the mainly used forms. During its preparation, the material has the chance to be exposed to microorganisms, particularly yeast. The aim of this study is to verify the effect of SRR on diabetes complications and the necessity of yeast exposure.

Materials and methods

Water extract of SRR was incubated with alcohol yeast to obtain fermented SRR (FSRR). Alloxan-induced diabetic rats were administrated with medicated animal chows for 8 weeks. Urine volume, fasted blood glucose and food intake were monitored, and open field test and tail immersion test were conducted in the last week, plasma and urine samples were subjected to biochemical examinations.

Results

In DM rats, defecation in open field test was found reduced, and tail flick latency in tail immersion test increased. In the meantime, urinary excretions of Na⁺, K⁺, aldosterone, albumin and creatinine increased, and plasma concentrations of Na⁺, K⁺ and creatinine reduced and those of aldosterone, TXB₂/6-Keto-PGF_1α and urea nitrogen elevated. Most of these indicators were significantly improved by FSRR administration, but the effects of SRR were relatively inferior in several aspects. However, SRR and FSRR could not improve the typical symptoms of DM.

Conclusions

Our data demonstrated that both SRR and FSRR have no obvious hypoglycemic effect, but have the potential to prevent the onset and development of diabetes complications, and this function can be improved by yeast exposure.     

Pharmacological investigation on the wound healing effects of Radix Rehmanniae in an animal model of diabetic foot ulcer

Ethnopharmacological relevance

Radix Rehmanniae (RR) has a very long history of usage in traditional Chinese medicine and is usually one of the principal herb found in many herbal formulae used in diabetic foot ulcer.

Aim of the study

RR aqueous extract was investigated for its wound healing effects in a diabetic foot ulcer rat model and its detailed mechanism of actions.

Materials and methods

A previously established diabetic foot ulcer rat model was used to assess the effect of RR extract on wound area reduction, tissue regeneration and angiogenesis. Carrageenan-induced inflammation rat model was used for inflammation study; and diabetic control was evaluated using a neonatal streptozotocin-induced diabetic rat model.

Results

In the RR treated group, a trend of reduction of the wound area was observed from days 8 to 18 and a significant difference (as compared with control group) was found on day 8. The ulcer healing effect of RR extract was further supported by better developed scars and epithelialization as well as good formation of capillaries with enhanced VEGF expression. Carrageenan-induced inflammation was also significantly alleviated with RR extract.

Conclusions

Our results demonstrated for the first time that Radix Rehmanniae was effective in promoting diabetic foot ulcer healing in rats through the processes of tissue regeneration, angiogenesis and inflammation control, but not glycemia control. The present study provided scientific basis to support the traditional use of Radix Rehmanniae in diabetic foot ulcer.     

黄连对乙酰苯肼所致小鼠红细胞氧化性溶血的影响及作用机制

目的:观察黄连对小鼠红细胞氧化性溶血的影响并探讨相关机制。方法:采用乙酰苯肼(APH)诱导小鼠红细胞氧化性溶血模型,以伯氨喹啉为对照药,观察不同浓度的黄连对血浆游离血红蛋白、血清间接胆红素、全血网织红细胞、红细胞内脂质过氧化产物和抗氧化系统相关酶和蛋白以及全血总抗氧化能力的影响。结果:0.03 g.kg-1APH能引起正常小鼠血浆游离血红蛋白和血清间接胆红素含量及外周血网织红细胞数量显著升高,也能明显提高红细胞丙二醛(MDA)含量和降低红细胞超氧化物歧化酶(SOD)、6-磷酸葡萄糖脱氢酶(G6PD)活力、还原型谷胱甘肽(GSH)含量以及全血总抗氧化能力。0.058 g.kg-1伯氨喹啉能明显加重APH所引起的红细胞氧化性溶血和氧化系统破坏;0.6 g.kg-1黄连能明显降低血清间接胆红素含量,1.2 g.kg-1黄连尚能显著减少血浆游离血红蛋白量和全血网织红细胞数,同时明显降低红细胞MDA含量、增加SOD活力和GSH含量、提高全血总抗氧化能力。结论:黄连能一定程度减轻APH引起的小鼠红细胞氧化性溶血,其机制可能与降低脂质过氧化产物和提高红细胞抗氧化酶的量和能力有关。     

Anti-hyperglycemic effect,inhibition of inflammatory cytokines expression,and histopathology profile in streptozotocin-induced diabetic rats treated with Arracacia tolucensis aerial-parts extracts

Ethopharmacological relevance

Arracacia tolucensis is a medicinal plant used in northeast of Mexico as a remedy to treat people with Diabetes mellitus (DM); however, there are no scientific studies that support this information. Thus, we evaluated the anti-hyperglycemic effect of the hexane, ethyl acetate and ethanol extracts from aerial parts in streptozotocin-induced diabetic rats.

Materials and methods

DM was induced in Wistar male rats by single intraperitoneal injection of streptozotocin (STZ 50 mg/kg). After STZ-induction, hyperglycemic rats were treated with all three extracts orally at a single dose (250 mg/kg) each 48 h for 21 days. Glibenclamide (1 mg/kg) was used as a reference drug. The fasting blood glucose levels, the hematic biometry and biochemical profiles, and the inhibition of inflammatory cytokines expression were estimated. Histopathology analysis of pancreas, liver, spleen, and kidney tissue was carried out.

Results

Ours results showed that ethyl acetate extract decreased blood glucose levels significantly (75%, p< 0.05) when compared to diabetic rats and controlled the body weight loss; the lipids level did not change, but the enzyme levels of aspartate aminotransferase and alanine aminotransferase decreased significantly (60.83% and 66.16%, respectively, p< 0.05) and inhibited the expression of inflammatory cytokines,with respect to diabetic rats. Histopathology injury was not observed; by contrast repair of islet of Langerhans was exhibited.

Conclusion

These results validate the use of Arracacia tolucensis as a treatment against DM and suggests it is suitable to continue studies for its safe therapeutic use.     

Comparison between ethanolic and aqueous extracts from Chinese juniper berries for hypoglycaemic and hypolipidemic effects in alloxan-induced diabetic rats

AIM OF THE STUDY: Hypoglycaemic and hypolipidemic properties of the ethanolic and aqueous extracts, respectively, from Chinese juniper (Juniperus chinensis L.) berries were investigated in alloxan-induced diabetic rats. MATERIALS AND METHODS: After oral administration of each extract singly or repeatedly to alloxan-induced diabetic rats, the blood glucose, glutamate-pyruvate transferase (GPT), glutamate-oxaloacetate transaminase (GOT), total cholesterol (TC) and triglyceride (TG) levels were assayed. RESULTS: The blood glucose levels after a single oral administration of the ethanolic extract significantly reduced in a time-dependent manner, which is much faster and more than that of glibenclamide. The blood glucose levels of alloxan-induced diabetic rats treated with the ethanolic extract were reduced to 94, 81%, 66%, 45% and 40% at 1, 3, 5, 7 and 9h, respectively (p<0.05), while the aqueous extract had no effect at all. Repeated oral administration of the ethanolic extract also effectively reduced the GPT value to 58% of the diabetic rats, but slightly reduced the GOT value to 87% of the diabetic rats (p<0.05). On the other hand, the repeated oral administration of aqueous extract effectively reduced the GOT value to 43% of the diabetic rats, without affecting the GPT level. Effects of both extracts on the TC and TG levels were different. There was no significant difference in the TC and TG levels between diabetic control and diabetic groups when repeatedly administered orally with ethanolic extract. On the other hand, the aqueous extract brought down the TC value to 57% and the TG value to 37% of the diabetic control rats (p<0.05). CONCLUSIONS: The results suggested that the ethanolic extract of Chinese juniper berries possesses a potential hypoglycaemic effect while the aqueous extract has a potential hypolipidemic effect.     

Hypoglycemic effects of Cecropia pachystachya in normal and alloxan-induced diabetic rats

Ethnopharmacological relevance

Leaves of Cecropia pachystachya are described in the folk medicine as possessing antitusive, expectorant, antiasthmatic and hypoglycemic effects.

Aim of the study

To investigate the hypoglycemic and antioxidant effects of methanolic extract from the leaves of Cecropia pachystachya. The total amount of phenolic and flavonoids compounds was determined and the qualitative composition of the extract was analyzed.

Materials and methods

The hypoglycemic effect of the extract was tested in normal, glucose loading and alloxan-induced diabetic rats. The antioxidant activity was assessed by DPPH free radical scavenging and reduction power assays. The total amount of phenolic and flavonoids compounds was determined by Folin-Denis and AlCl₃ reagent method, respectively. The qualitative composition of the extract was analyzed using a HPLC-DAD system.

Results

The glucose tolerance test showed that in diabetic rats, the extract caused a significant hypoglycemic effect with a blood glucose reduction of 68% after 12 h. The administration of the extract in alloxan-induced diabetic rats also produced a significant reduction in the blood glucose levels at all points being more pronounced at 90 min (reduction of 60%). After 120 min, no significant difference was observed between the blood levels of the rats treated with the extract and those treated with the standard drugs (metformin and glibenclamide). The extract also presented relevant antioxidant activity with IC₅₀ = 3.1 μg/ml (DPPH assay) and EC₅₀ = 10.8 μg/ml (reduction power). Results were compared with the reference antioxidants quercetin, rutin, and ascorbic acid. The content of flavonoids was 83 mg/g plant and that of phenolics was 326 mg/g plant. Chlorogenic acid and the C-glycosylated flavones, orientin and isoorientin, were identified in the extract.

Conclusions

In conclusion, the findings showed that the folk medicinal plant Cecropia pachystachya possesses hypoglycemic and antioxidant effects which confirmed the traditional use of the plant in the treatment of diabetes. Chlorogenic acid and the C-glycosylated flavonoids may explain these activities.     

Antioxidant and anti-inflammatory effects of Urtica pilulifera extracts in type2 diabetic rats

Ethnopharmacological relevance

"Urtica pilulifera has been traditionally used in Egyptian system as an herbal remedy to be a diuretic, antiasthmatic, anti-inflammatory, hypoglycemic, hemostatic, antidandruff and astringent"

Aim of the study

To evaluate the potential effects of ethyl acetate (EA), chloroform (CHLOR) and hexane (HEXA) extracts of Urtica piluliferaas oral anti-diabetic agents as well as to evaluate their possible anti-oxidant and anti-inflammatory effects in type2 diabetic rat model.

Material and methods

Type2 diabetes was induced by a high fat diet and low dose streptozotocin (STZ). Diabetic adult male albino rats were allocated into groups and treated according to the following schedule; Pioglitazone HCL (PIO), EA, CHLOR and HEXA extracts of Urtica pilulifera at two doses of 250 and 500 mg/kg were used. In addition, a normal control group and a diabetic control one were used for comparison. Blood glucose, insulin resistance, antioxidant enzymes, 8-hydroxy-2-deoxyguanosine (8-OHdG) as well as C-reactive protein and tumor necrosis factor-α levels were evaluated.

Results

EA and CHLOR extracts of Urtica pilulifera exhibited a significant hypoglycemia associated with antioxidant and anti-inflammatory effects in diabetic rats; however, HEXA extract showed no beneficial effect. These activities are responsible, at least partly, for improvements that have been seen in hyperglycemia and insulin resistance of diabetic rats.

Conclusion

Our results encourage the traditional use of Urtica pilulifera extract as an antioxidant and anti-inflammatory agent as an additional therapy of diabetes.     

Screening and evaluation of traditional Chinese medicine by microarray expression analysis

Ethnopharmacological relevance

Salvia miltiorrhiza is a Chinese medicinal herb, which is widely used for the treatment of cardiovascular disorders. In this article, we investigated the effects of Salvia miltiorrhiza and its hydrophilic and lipophilic components (HCS and LCS) on human umbilical vein endothelial cells (HUVECs), and the molecular mechanism was explored by microarray gene expression profiling.

Materials and methods

Cell proliferation and migration were used to evaluate the angiogenic effects of HCS, LCS and total extract of Salvia miltiorrhiza (TES). Microarray technology was applied to detect the gene expression of HUVECs treated with TES, HCS and LCS. Besides, quantitative real-time PCR was used to verify the microarray results.

Results

Our results showed that LCS inhibited the proliferation and migration of HUVECs, HCS promoted the proliferation and migration of HUVECs, and TES did not affect the viability of HUVECs at the concentration of 5 µg/mL. From the result of principle component analysis (PCA) of microarray data, the effect of LCS on HUVECs was significantly different from the other components. Moreover, there were more differentially expression genes in LCS group than in the other groups, which meant LCS had a strong influence on HUVECs. Compared with untreated cells, 511 significantly changed genes had been detected in LCS treated cells and 236 (approximately 46%) of them were up-regulated. The mRNA expression of IL-6 was found to be increased significantly in LCS group.

Conclusions

In Salvia miltiorrhiza, HCS and LCS had opposite effects on HUVECs. LCS showed significantly inhibitory action on HUVECs proliferation and migration. It was proposed that LCS could apply in the diseases caused by vascular anomaly hyperplasia. In the mechanism of action of LCS on HUVECs, the pathways of ErbB, MAPK, p53, oxidative phosphorylation and inflammatory response were involved.     

基于指纹图谱和含量测定评价地黄不同入药形式制千金黄连丸质量

目的 综合评价地黄不同入药形式制千金黄连丸（Qianjin Huanglian Pills,QHP）的质量。方法 建立地黄不同入药形式制QHP的HPLC指纹图谱,通过多元统计分析及2种环烯醚萜苷类成分（梓醇、益母草苷）、5种生物碱类成分（黄连碱、表小檗碱、药根碱、小檗碱、巴马丁）、5种糖类成分（果糖、葡萄糖、蔗糖、棉子糖、水苏糖）定量分析对30批地黄不同入药形式制QHP的质量进行评价。结果 30批QHP样品指纹图谱相似度较高,采用SPSS19.0和SIMCA-P14.1软件对黄连丸19个共有峰峰面积进行系统聚类分析和主成分分析,30批样品可按鲜地黄连丸、鲜干黄连丸、生地黄连丸明显分为3类;采用正交偏最小二乘法-判别分析标记了黄连丸中8个差异性成分,分别为峰1、6、15（表小檗碱）、3、4、2（梓醇）、16、9。含量测定结果表明,2种环烯醚萜苷类成分梓醇、益母草苷总含量顺序为鲜干黄连丸>鲜地黄连丸>生地黄连丸,5种生物碱类成分总含量顺序为生地黄连丸>鲜地黄连丸>鲜干黄连丸,5种糖类成分总含量顺序为鲜地黄连丸>鲜干黄连丸>生地黄连丸,棉子糖和水苏糖的含量...     

Preliminary study of antidiabetic activity of the methanolic leaf extract of Axonopus compressus (P. Beauv) in alloxan-induced diabetic rats

Ethnopharmacological relevance

Axonopus Compressus is commonly used by the people of Southern Nigeria to treat different ailment such as common cold and diabetes. This study therefore, evaluated the anti-diabetic effect of the methanolic leaf extract of the plant.

Materials and methods

Diabetes was induced in the rats by intraperitoneal (i.p.) injection of alloxan monohydrate at the dose of 180 mg/kg. Three test doses of the extract (250, 500 and 1000 mg/kg) administered per os through gastric gavage to the rats were used in the study. The activity was compared to a standard reference drug (glibenclamide, 2 mg/kg) and a negative control. Blood from the tail snip was used to measure the effects of the extract and drug at 0, 1, 3 and 6 h using autoanalyzer (AccuCheck Active^®) glucose kit.

Results

Methanolic leaf extract of Axonopus compressus at all the doses (250, 500 and 1000 mg/kg) used caused a respective time dependent and significant (p < 0.0001) reduction (by 31.5%, 19.8% and 24.5%) of the blood glucose levels in the diabetic rats when compared to the negative control group at the 6th hour. However, the reference drug (glibenclamide, 2 mg/kg) decreased the blood glucose levels by 69.9% and the tween 20 solution (negative control) increased the blood glucose level by 15.2% at the 6th hour. Moreso, the extract at the different test doses caused various degrees of reduction of the blood glucose levels of the test rats at 1st, 3rd and 6th hours when compared to the negative control rats.

Conclusion

The findings suggest that Axonopus compressus may possess antidiabetic property.     

Ethnobotany,phytochemistry and pharmacology of the genus Caragana used in traditional Chinese medicine

The genus Caragana is a member of the family Fabaceae, subfamily Faboideae and is native to arid and semi-arid areas of the temperate zones of Asia and Eastern Europe. Many species are cultured for dune-fixation, livestock forage and biological resources for fuel energy and fiber production. More than 10 species in this genus have a long history of use in traditional Chinese, Mongolian and Tibetan medicines and are believed to “nourish yin, invigorate the spleen, temper the blood and promote blood flow”. They have been used for the treatment of a wide range of ailments including fevers, inflammation, wounds and infections, dizziness, headache, hypertension, female disorders, arthritis and cancer. Over 100 phytochemicals have been identified with flavonoids and stilbenoids being the major constituents of this genus. Clinical studies have demonstrated the pharmacological activities of different Caraganum species, e.g. Caragana sinica for the treatment of hypertension, and in vivo and/or in vitro studies have provided some support for other traditional uses, e.g. anti-cancer, anti-inflammatory, phytoestrogenic, immunostimulant and immunosuppressant activities. However, further studies to identify the active components and further verify the pharmacological activities are warranted. This review presents a comprehensive analysis of the ethnobotany, phytochemistry and pharmacology of the genus Caragana.     

In vitro and in vivo antimalarial and cytotoxic activity of five plants used in congolese traditional medicine

Aim of the study

The in vitro antiplasmodial activity and cytotoxicity of methanolic and dichloromethane extracts from five Congolese plants were evaluated. The plants were selected following an ethnobotanical survey conducted in D.R. Congo and focusing on plants used traditionally to treat malaria. The in vivo antimalarial activity of aqueous and methanolic extracts active in vitro was also determined in mice infected by Plasmodium berghei berghei.

Materials and methods

The growth inhibition of Plasmodium falciparum strains was evaluated using the measurement of lactate dehydrogenase activity. The extracts (aqueous, CH₃OH, EtOH and CH₂Cl₂) were prepared by maceration and tested in vitro against the 3D7 (chloroquine sensitive) and W2 (chloroquine resistant) strains of Plasmodium falciparum and against the human normal fetal lung fibroblasts WI-38 to determine the selectivity index. Some extracts were also used at the dose of 300 mg/kg to evaluate their activity in mice infected since 4 days by Plasmodium berghei.

Results

Two plants presented a very high activity (IC₅₀ < 3 μg/ml). These plants were Strychnos icaja roots bark (MeOH and CH₂Cl₂) and Physalis angulata leaves (MeOH and CH₂Cl₂). One plant (Anisopappus chinensis whole plant, MeOH and CH₂Cl₂) presented a high activity (IC50 < 15 μg/ml). The extracts of Anisopappus chinensis and Physalis angulata showed also a good inhibition of parasitemia in vivo. Flavonoids, phenolic acids and terpenes were identified in these plants by a general phytochemical screening method.

Conclusion

Three plants showed a very interesting antiplasmodial activity (Anisopappus chinensis, Physalis angulata and Strychnos icaja) and one of them showed a good selectivity index (>10, Anisopappus chinensis). Anisopappus chinensis and Physalis angulata were also active in vivo.     

An-Gong-Niu-Huang Wan protects against cerebral ischemia induced apoptosis in rats: Up-regulation of Bcl-2 and down-regulation of Bax and caspase-3

Ethnopharmacological relevance

The An-Gong-Niu-Huang Wan (AGNH), a Chinese traditional medicine, has been used for treatment of cerebral diseases for centuries in China and other Asian countries, and is approved by the State Food and Drug Administration of China for the treatment of stroke. The aim of present study is to test the neuroprotective effects of AGNH on cerebral ischemia in rats and to explore the underlying mechanisms.

Materials and methods

75 Male Sprague-Dawley rats were randomly divided into 5 groups: sham, ischemia–reperfusion (I/R), and I/R plus 0.065 g/kg/d AGNH, 0.125 g/kg/d AGNH and 0.25 g/kg/d AGNH. Cerebral ischemia was induced by 1.5 h of middle cerebral artery occlusion (MCAO). Neurological functional deficits were evaluated according to Zea longa?s score, cerebral infarct area was measured by tetrazolium staining. Cell injury and apoptosis were assessed by Nissl staining and DNA fragmentation assay. The expression of Bax, Bcl-2 and caspase-3 were analyzed by Western blot.

Results

Rats subjected to MCAO exhibited worsened neurological score, infarct area, cell damage and apoptosis. These were all attenuated by AGNH (0.125 and 0.25 g/kg/d). Moreover, AGNH reversed cerebral ischemia induced decreases in Bcl-2 expression and increases in Bax and caspase-3 expression.

Conclusions

These results suggest that AGNH exerts neuroprotective effects, and the neuroprotection is likely to relate to depressed Bax/Bcl-2 ratio and caspase-3 level, leading to inhibition of apoptotic cell death.     

Comparison of the chemical profiles and anti-platelet aggregation effects of two "Dragon's Blood" drugs used in traditional Chinese medicine

Ethnopharmacological relevance

“Dragon's Blood” has been used as a medicine since ancient times by many cultures. In traditional Chinese medicine, the resin obtained from Daemonorops draco (RDD) and the resin from Dracaena cochinchinensis (RDC) are equally prescribed as “Dragon's Blood” for facilitating blood circulation.

Aim of the study

To verify the traditional efficacy and elucidate the mechanism, the present study compared the chemical profiles and the pharmacological effects of two species of “Dragon's Blood” mainly used in China.

Materials and methods

A UPLC-MS fingerprinting method was developed to compare the chemical profiles of the two medicines. The anti-platelet aggregation effects of the two medicines induced by arachidonic acid (AA) were investigated.

Results

The chemical profiles of these two species of “Dragon's Blood” were significantly different. The characteristic constituents were found to be: flavanes in RDD and stilbenes in RDC. In the in vivo platelet inhibition test, performed with the dose of 200 mg/kg on rats, the peak inhibitory effects of RDD and RDC were 35.8% and 27.6%, respectively, compared with the control group. With the in vitro concentrations of 0.2, 0.4 and 0.8 mg/ml, RDD exerted significant inhibition of aggregation by 18.7%, 20.0%, and 61.6%, respectively, and RDC exerted significant inhibition of aggregation by 13.3%, 20.2%, and 31.6%, respectively.

Conclusion

The fingerprinting method used here is suitable for distinguishing them. All pharmacological tests indicated that RDD was more potent than RDC against platelet aggregation.     

Investigation of plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts

Aim of the study

To investigate the activities of the 217 plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts.

Materials and methods

Plant extracts were prepared by the method of maceration using solvents of different polarities. The growth inhibition of chloroquine-resistant Plasmodium falciparum strain (FcB1) was determined by measuring the radioactivity of the tritiated hypoxanthine incorporated. Activity against Leishmania (Leishmania) chagasi and Trypanosoma cruzi was measured by the MTT colorimetric assay. The antifungal tests were carried out by using the CLSI method. The active extracts were tested also by cytotoxicity assay using NIH-3T3 cells of mammalian fibroblasts.

Results

Two hundred and seventeen extracts of plants were tested against Plasmodium falciparum. The eleven active extracts, belonging to eight plant species were evaluated against L. (L.) chagasi, Trypanosoma cruzi, yeasts and in NIH-3T3 cells. The results found in these biological models are consistent with the ethnopharmacological data of these plants. The ethyl acetate extract of Diospyros hispida root showed IC₅₀ values of 1 μg/mL against Plasmodium falciparum. This extract demonstrated no toxicity against mammalian cells, resulting in a significant selectivity index (SI) of 435.8. The dichloromethane extract of Calophyllum brasiliense root wood was active against Cryptococcus gattii LMGO 01 with MIC of 1.95 μg/mL; and Candida albicans ATCC 10231 and Candida krusei LMGO 174, both with MIC of 7.81 μg/mL. The same extract was also active against Plasmodium falciparum and L. (L.) chagasi with IC₅₀ of 6.7 and 27.6 μg/mL respectively. The ethyl acetate extract of Spiranthera odoratissima leaves was active against Cryptococcus gattii LMGO 01 with MIC of 31.25 μg/mL, and against Plasmodium falciparum with IC₅₀ of 9.2 μg/mL and Trypanosoma cruzi with IC₅₀ of 56.3 μg/mL.

Conclusion

The active extracts for protozoans and human pathogenic yeasts are considered promising to continue the search for the identification and development of leading compounds.     

Hepatoprotective and antioxidant effects of Cuscuta chinensis against acetaminophen-induced hepatotoxicity in rats

Tu-Si-Zi, the seeds of Cuscuta chinensis Lam. (Convolvulaceae), is a traditional Chinese medicine that is commonly used to nourish and improve the liver and kidney conditions in China and other Asian countries. As oxidative stress promotes the development of acetaminophen (APAP)-induced hepatotoxicity, the aim of the present study was to evaluate and compare the hepatoprotective effect and antioxidant activities of the aqueous and ethanolic extracts of C chinensis on APAP-induced hepatotoxicity in rats. The C chinensis ethanolic extract at an oral dose of both 125 and 250mg/kg showed a significant hepatoprotective effect relatively to the same extent (P<0.05) by reducing levels of glutamate oxaloacetate transaminase (GOT), glutamate pyruvate transaminase (GPT), and alkaline phosphatase (ALP). In addition, the same ethanolic extract prevented the hepatotoxicity induced by APAP-intoxicated treatment as observed when assessing the liver histopathology. Regarding the antioxidant activity, C chinensis ethanolic extract exhibited a significant effect (P<0.05) by increasing levels of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), and by reducing malondialdehyde (MDA) levels. In contrast, the same doses of the aqueous extract of C chinensis did not present any hepatoprotective effect as seen in the ethanolic extract, and resulted in further liver deterioration. In conclusion, these data suggest that the ethanolic extract of Cuscuta chinensis can prevent hepatic injuries from APAP-induced hepatotoxicity in rats and this is likely mediated through its antioxidant activities.     

Hypoglycemic and antihyperglycemic effect of Begonia malabarica Lam. in normal and streptozotocin induced diabetic rats

Aim of the study

The stem of Begonia malabarica was used traditionally by the Malasar tribe to treat diabetes. To validate the hypoglycemic and antihyperglycemic effects of the hexane, ethylacetate and methanol extracts obtained from an ethnomedicinal plant, Begonia malabarica.

Materials and methods

The doses for the study were fixed based on Irwin test. The hypoglycemic effect of hexane, ethylacetate and methanol extracts of Begonia malabarica stems were studied in normal animals. The antihyperglycemic effect of the methanol extract was studied in streptozotocin induced diabetic rats.

Results

In normal rats the treatment with the methanol extract of Begonia malabarica had shown a highly significant reduction (16.54 and 34.47%) in plasma glucose levels from the 0 h values at the dose of 100 and 200 mg/kg respectively. In streptozotocin induced diabetic rats the body weight of the Begonia malabarica methanol extract treated animals had shown a significant increase (13.38% at 200 mg/kg) after 4 weeks treatment. The plasma glucose levels were reduced significantly by 46.57 and 50.20% after 4 weeks treatment at 100 and 200 mg/kg respectively. Likewise the absolute kidney weight was also reduced in a significant manner. After 25 days treatment the Begonia malabarica methanol extract treated animals had shown low fasting plasma glucose levels (54.29, 61.34% in 100 and 200 mg/kg) and reduced postprandial plasma glucose levels (54.23, 65.96% in 100 and 200 mg/kg) when compared with diabetic control values. Serum insulin levels and liver glycogen levels were increased to 40.04 and 42.18% in 200 mg/kg Begonia malabarica methanol extract treated animals respectively. The treatment with Begonia malabarica methanol extract did not change the triglycerides and total cholesterol levels. The urea and creatinine levels were also reduced significantly by this treatment. The reduction in SGPT levels indicated the absence of toxicity of Begonia malabarica extract at this dose level.

Conclusion

This study supports the use of Begonia malabarica by the Malasar tribe for the treatment of diabetes. Fractionation of this extract may yield novel prototypes to manage diabetes mellitus.     

Anti-hyperglycemic effects and mechanism of Bidens pilosa water extract

Aim of study

Bidens pilosa has traditionally been used as an anti-diabetic phytomedicine. However, its alleged benefits and mechanism remain elusive. This study aimed to evaluate the effect and action of Bidens pilosa water extract on type 2 diabetes.

Materials and methods

A daily dose of Bidens pilosa water extract or glimepiride, a positive control, was given orally to C57BL/KsJ-db/db mice once or for 28 days. Levels of blood glucose, serum insulin, and glycosylated hemoglobulin A1C, glucose tolerance, and islet structure were used to evaluate its anti-diabetic effects in db/db mice. Rat pancreatic islets and streptozocin-treated mice were tested for insulin-releasing mechanism of Bidens pilosa water extract.

Results

A daily dose of Bidens pilosa water extract given once or for 28 days significantly decreased blood glucose levels and increased serum insulin levels in db/db mice. Besides, 28-day treatment with Bidens pilosa water extract significantly improved glucose tolerance, decreased HbA1C levels and protected islet structure in db/db mice. Mechanism study showed that Bidens pilosa water extract stimulated insulin secretion via pancreatic islets.

Conclusions

Our results suggest that Bidens pilosa water extract ameliorates type 2 diabetes in db/db mice via regulation of insulin secretion and islet protection.