Inhibition mechanism of compound ethanol extracts from Wuweizi (Fructus Schisandrae Chinensis) on renal interstitial fibrosis in diabetic nephropathy model mice

Objective

To evaluate inhibition effect and mechanism of compound ethanol extracts from Wuweizi (Fructus Schisandrae Chinensis), Chuanxiong (Rhizoma Chuanxiong) and Muli (Cocha Ostreae) (FRC) on glomerular and tubular interstitial fibrosis in streptozocin (STZ)-induced diabetic nephropathy (ND) model mice.

Methods

Twenty-seven male C57BL/6 mice were divided randomly into 3 groups: nondibetic (ND), STZ-induced diabetic (D), and STZ-induced diabetic that were treated with 5 g · kg⁻¹ · day⁻¹of FRC by oral gavage (D_FRC), with 9 in each group. The protein expressions of E-cadherin, α-smooth muscle actin (α-SMA), Plasminogen Activator Inhibitor-1 (PAI-1) in renal tissues were investigated by Western blotting. The expressions of fibronectin (FN) and α-SMA were detected by immunohistochemical method. The morphological changes of renal tissues were observed under a microscope.

Results

Renal tissues in the D_FRC group showed a lessened degree of fibrosis. Meanwhile, the expressions of FN, α-SMA and PAI-1 were significantly lower in the D_FRC group than those in the D group (all P<0.05).

Conclusion

FRC can ameliorate the DN in the C57BL/6 mice, and its mechanism may relate to inhibition on the epithelial to mesenchymal transdifferentiation, endothelial-myofibroblast transition and PAI-1 expression.     

Antihyperglycemic and antihyperlipidemic action of cinnamaldehyde in C57blks/j Db/db mice

Objective

To investigate the effects of cinnamaldehyde (CA), an active and major compound in cinnamon, on glucose metabolism and insulin resistance in C57BLKS/J db/db mice.

Methods

Sixteen male C57BLKS db/db mice were randomly divided into control and CA treatment groups. CA was given (20 mg · kg⁻¹ · day⁻¹, p. o.) for 4 weeks. Pure water was given to control and db/+ mice. Subsequently, the levels of fasting blood glucose (FBG), fasting serum insulin, triglyeride, cholesterol, low-density lipoprotein -cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C), and free fatty acids (FFA), as well as the mRNA content of adiponectin and tumor necrosis factor (TNF)-α in adipose tissue, glucose transporter type 4 (GLUT-4) in skeletal muscle, and protein expressions of Akt, phospho-Akt (Thr308), AMPKα, phospho-AMPKα (Thr172) in skeletal muscle were measured.

Results

1) CA decreased serum levels of FBG and insulin as well as body weight in db/db mice; 2) CA increased serum HDL-C levels; 3) CA significantly decreased the mRNA expression of TNF-α in adipose tissue and upregulated mRNA expression of GLUT-4 in skeletal muscle; 4) protein expression of p-Akt was increased in CA-treated mice, but Akt, AMPKα and p-AMPKα showed no change.

Conclusion

CA has antihyperglycemic and antihyperlipidemic actions in db/db mice and could be useful in the treatment of type-2 diabetes.     

Pharmacological and toxicological effects of Paronychia argentea in experimental calcium oxalate nephrolithiasis in rats

Aim of the study

Renal protection and antiurolithiasic effects of two extracts of Paronychia argentea (PA), a traditional Algerian plant commonly known as Algerian tea, were evaluated. This study was carried out to determine whether the aqueous extract (APA) or the butanolic extract (BPA) of aerial parts could prevent or reduce calculi aggregation in experimental calcium oxalate (Ox) nephrolithiasis in Wistar rats.

Materials and methods

The two extracts (APA and BPA) were administrated orally and daily, during 28 days to nephrolithiasic treated rats at the dose of 250, 500 mg/kg b.w. and 10, 20 mg/kg b.w. respectively.Body weight, renal index, liver index, serum level of creatinine, uric acid, urea, K⁺, Ca²⁺, Mg²⁺, Na⁺ and transaminase (alanine aminotransferase, ALT; aspartate aminotransferase, AST), phosphatase alkaline activity (PAL) were evaluated following the 28 days treatment in rats. In addition histopathological changes in kidney and liver were stained in hematoxylin eosin (HE).

Results

The effect of the extracts could be advantageous in preventing urinary stone retention by reducing renal necrosis and thus inhibit crystal retention. In contradiction with APA, the two doses of BPA attenuated elevation in the serum creatinine (p < 0.01) and blood urea levels (p < 0.01) (nephroprotective effect). However, the increase in ALT (27%) and PAL (31–51%) serum levels and in the relative liver weights (p < 0.01) in the groups treated with doses of APA may indicate that this extract has not a hepatoprotective effect against oxalate toxicity.

Conclusions

The presented data indicate that administration of the butanolic extract of aerial parts to rats with NaOx induced lithiasis, and reduced and prevented the growth of urinary stones in experimental calcium oxalate nephrolithiasis in Wistar rats.     

Bioactivity-directed isolation, identification of diuretic compounds from Polyporus umbellatus

Aim of the study

Polyporus umbellatus is a fungus used as a diuretic medicine. The objective of this study was to isolate and elucidate the diuretic constituents of n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus and to evaluate their diuretic activity.

Materials and methods

The n-hexane, ethyl acetate, n-butanol and water extracts of Polyporus umbellatus were tested by diuretic experiment of normal rats in metabolic cage. The n-hexane extract and n-butanol extract were prepared separately by the bioassay-guided approach. Three isolated compounds doses (5, 10 and 20 mg/kg BW) were orally administered to normal rats. Water excretion rate, pH and content of Na⁺, K⁺ and Cl⁻ were measured in the urine of saline-loaded rats.

Results

n-Hexane extract (P < 0.05), n-butanol extract (P < 0.05) and three isolated compounds (ergosta-4,6,8(14),22-tetraen-3-one, ergosterol and d-mannitol) displayed diuretic activity.

Conclusions

The ergosta-4,6,8(14),22-tetraen-3-one was the strongest diuretic constituent in the three compounds. Ergosterol and d-mannitol were found to be also responsible for duiretic effects in Polyporus umbellatus for the first time. Data show that 20 mg/kg dose of the ergosterol for urine out put became significantly higher than in the control rats, but the ratio of Na⁺/K⁺ almost unaltered in the three doses. The highest dose of the d-mannitol was significant and increased the cumulative urine output. Regarding the electrolyte excretion, data show that the doses 10 and 20 mg/kg produce significant increase for excretion of Na⁺ and Cl⁻. The present results provide a quantitative basis explaining application of Polyporus umbellatus as a diuretic medicine. The result proved that its diuretic effects were also due to the contribution of multi-components in clinical application.     

Antidepressant-like effects of Tagetes lucida Cav. in the forced swimming test

Aim of the Study

Tagetes lucida (Asteraceae), has been referred in Mexican traditional medicine for the treatment of different central nervous system (CNS) diseases, mainly depression. Nevertheless, the available scientific information about this species is scarce and there are no reports related to its possible effect on the CNS. In this work, the antidepressant-like effect of extract of Tagetes lucida was evaluated in rats, as well as its potential adverse effects on male sexual behavior (MSB).

Materials and methods

Antidepressant activity was studied using forced swimming test (FST), motor activity in the open-field test and on MSB in sexually experienced male. The aqueous extract of Tagetes lucida in doses of 5, 10, 50, 100 and 200 mg/(kg day)⁻¹ were administered orally for 14 consecutive days and evaluated on day 14, 2 h after the last dose treatment. Fluoxetine (10 mg/(kg day)⁻¹, p.o.) was used as the control positive.

Results

The aqueous extract (10, 50, 100 mg/(kg day)⁻¹) significantly reduced immobility and increased swimming without affecting climbing behavior in the FST. These same doses were not able to modify neither the motor activity nor the MSB.

Conclusion

These data indicate that the extract of Tagetes lucida possesses antidepressant-like properties in rats.     

Effect of Cydonia oblonga Mill. leaf extract on serum lipids and liver function in a rat model of hyperlipidaemia

Ethnopharmacological relevance

Cydonia oblonga Mill. leaves are traditionally used in Uyghur medicine to treat or prevent cardiovascular disease. Beyond a demonstrated effect on thrombosis, we tested it for an effect on dyslipidemia, in a rat model of hyperlipidemia.

Methods

Seventy healthy Sprague Dawley rats were randomly divided into 6 groups: normal controls, model controls, simvastatin, and low-, medium- and high-dose Cydonia oblonga Mill. leaf extracts (COM), orally for 56 days. The normal controls were fed a normal diet, all other groups a high fat diet. Rat weights were recorded over time. Total cholesterol (TC), triglycerides (TG), low and high-density lipoproteins (LDL, HDL), as well as AST, ALT and total protein (TP) were measured in serum at the end of the study. The antioxidant capacity of glutathione peroxidase (GSH-PX), superoxide dismutase (SOD), malondialdehyde (MDA) was measured in liver samples, along with lipoprotein lipase (LPL), and hepatic lipase (HL). Liver pathology was described.

Results

COM dose-dependently reduced TC, TG, LDL-C and MDA, inhibited the activity of ALT, AST and LPS, increased HDL-C content, increased the activity of SOD, GSH-PX, LPL and HL, and reduced liver steatosis in hyperlipidaemia rats, which was significant at medium and high doses. The effect of COM was similar to that of simvastatin except for increased LPL and HL which were reduced by COM but not by simvastatin.

Conclusion

Cydonia oblonga Mill. leaf extracts have hypolipidaemic and hepatoprotective effects, probably related to increasing antioxidant capacity and lipoprotein metabolism in the liver, and inhibition of lipogenesis.     

Evaluation of diuretic activity of Amaranthus spinosus Linn. aqueous extract in Wistar rats

Ethnopharmacological relevance

Traditional Siddha medicine literature claims that the Amaranthus spinosus Linn. (family: Amaranthaceae) whole plant possesses diuretic property.

Aim of the study

To evaluate the diuretic potential of Amaranthus spinosus aqueous extract (ASAE) in rats.

Material and methods

Different concentrations of ASAE (200, 500, 1000, 1500 mg/kg), thiazide (10 mg/kg) and vehicle were orally administered to rats (n = 6 animals per group) and their urine output was collected after 24 h. Volume, pH, Na⁺, K⁺ and Cl⁻ concentrations of urine were estimated.

Results

ASAE produced increase in Na⁺, K⁺, Cl⁻ excretion, caused alkalinization of urine, showed strong saluretic activity and carbonic anhydrase inhibition activity. These effects were observed predominantly at 500 mg/kg dose and there was no dose–response relationship.

Conclusion

Our study strongly suggests that the Amaranthus spinosus is acting as a thiazide like diuretic with carbonic anhydrase inhibitory activity which restates the claim as diuretic herb in Siddha medicine.     

Effects of Wei Chang An pill on enzyme activity and levels of vasoactive peptide and substance P in the small intestine of rats with compound diarrhea

Objective

To investigate the regulatory effects of Wei Chang An Pill (WCAP) on enzyme activity and gastrointestinal hormones in the small intestine of rats with compound diarrhea.

Methods

Forty Wistar rats were randomly divided into a control, diarrhea model, and WCAP high, medium, and low dose groups. The control group was not treated, and the model group was administered intragastric distilled water. The WCAP groups were given WCAP suspension, 80, 60 or 40 mg · kg⁻¹ · d⁻¹, for 4 days. Stool properties were observed. After the experiment, thymus and spleen indices were measured, and the activities of lactate dehydrogenase (LDH), malate dehydrogenase (MDH), and disaccharidase (lactase) in the small intestinal mucous membrane, and levels of substance P (SP) and vasoactive peptide (VIP) in the colon were determined.

Results

Compared with the control group, thymus and spleen indices were significantly decreased, LDH, MDH, and disaccharidase activity in the small intestine was decreased, and SP and VIP levels in the colon were significantly increased in the diarrhea model group. Compared with the model group, thymus and spleen indices were significantly increased, and LDH, MDH, and disaccharidase activity in the small intestine and SP and VIP levels in the colon were significantly decreased in the WCAP medium dose group.

Conclusion

The diarrhea model rats exhibited pathological changes including atrophy of the thymus and spleen, decreased enzyme activity in the small intestine, and gastrointestinal hormone disturbance. WCAP can increase the activity of intestinal digestive enzymes and regulate gastrointestinal hormones, thereby relieving diarrhea.     

Hepatoprotective and antioxidant activity of Phaseolus trilobus,Ait on bile duct ligation induced liver fibrosis in rats

Ethnopharmacological relevance

Phaseolus trilobus Ait (Fabaceae) is extensively used by tribal people of Nandurbar district (Maharashtra, India) in the treatment of Jaundice and other liver disorders.

Aim

of the present study was to assess the medicinal claim of Phaseolus trilobus as hepatoprotective and antioxidant.

Material and methods

The hepatoprotective activity of methanol and aqueous extract of Phaseolus trilobus was evaluated by bile duct ligation induced liver fibrosis and antioxidant activity was evaluated using in vitro and in vivo antioxidant models viz anti-lipid peroxidation assay, super oxide radical scavenging assay and glutathione estimation in liver. Liver function tests were carried out to detect hepatoprotective activity, which was further supported by histopathological examination.

Results

Methanol and aqueous extracts of Phaseolus trilobus reduced elevated level of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), lactate dehydrogenase (LDH), bilirubin and hydroxyproline significantly (p < 0.01) in bile duct ligated Wistar rats, proving hepatoprotective activity comparable with Silymarin. Both the extracts were found to reduce the elevated levels of serum thiobarbituric acid reactive substance (TBARS) and elevate superoxide scavenging radical activity proving antioxidant activity comparable with ascorbic acid. The reduced level of glutathione was found to be elevated in liver proving antioxidant activity comparable with Silymarin.

Conclusion

Phaseolus trilobus posses hepatoprotective property and is effective in oxidative stress induced cholestatic hepatic injury.     

Sedative, antiepileptic and antipsychotic effects of Viscum album L. (Loranthaceae) in mice and rats

Ethnopharmacological relevance

Viscum album L. is claimed in traditional medical practice, to be useful in the treatment of epilepsy and insomnia in Himachal Pradesh, India.

Materials and methods

The effect of Viscum album L. on epilepsy, psychosis and sedative activity was evaluated in mice and rats using standard procedure.

Results

The aqueous leaf extract of Viscum album L. prolonged the pentobarbital induced sleeping time and reduced the locomotor activity in actophotometer. This suggests that reduced locomotor activity facilitate GABAergic transmission. In addition the extract reduced MES, INH and PTZ-induced convulsions which suggest that there may be possibility of blocking Na⁺ channels, opening of Cl⁻channels or enhancing the GABAergic system. The extract decreased the apomorphine-induced stereotyped behavior and potentiates the HAL-induced cataleptic score which suggests the extract possess antidopaminergic activity.

Conclusion

The results obtained in present study suggested that title plant exhibited sedative, antiepileptic and antipsychotic activity in mice and rats.     

Antitumoral and antioxidant effects of a hydroalcoholic extract of cat's claw (Uncaria tomentosa) (Willd. Ex Roem. & Schult) in an in vivo carcinosarcoma model

Aim of the study

The present work intended to study the antitumoral and antioxidant effects of Uncaria tomentosa (UT) hydroalcoholic extract in the Walker-256 cancer model.

Methods and materials

Walker-256 cells were subcutaneously inoculated in the pelvic limb of male Wistar rats. Daily gavage with UT extract (10, 50 or 100 mg kg⁻¹, Groups UT) or saline solution (Control, Group C) was subsequently initiated, until 14 days afterwards. For some parameters, a group of healthy rats (Baseline, Group B) was added. At the end of treatment the following parameters were evaluated: (a) tumor volume and mass; (b) plasmatic concentration of urea, alanine aminotransferase (ALT), aspartate aminotransferase (AST), gamma-glutamyltransferase (GGT) and lactate dehydrogenase (LDH); (c) hepatic and tumoral activity of catalase (CAT) and superoxide dismutase (SOD), as well as the rate of lipid peroxidation (LPO) and gluthatione (GSH); and (d) hepatic glutathione-S-transferase (GST) activity. The reactivity of UT extract with the stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) was assessed in parallel.

Results

UT hydroalcoholic extract successfully reduced the tumor growth. In addition, treatment with UT reduced the activity of AST, which had been increased as a result of tumor inoculation, thus attempting to return it to normal levels. UT did not reverse the increase of LDH and GGT plasma levels, although all doses were remarkably effective in reducing urea plasma levels. An important in vitro free radical-scavenging activity was detected at various concentrations of UT extract (1–300 μg mL⁻¹). Treatment also resulted in increased CAT activity in liver, while decreasing it in tumor tissue. SOD activity was reduced in liver as well as in tumor, compared to Group C. No statistical significance concerning ALT, GST, LPO or GSH were observed.

Conclusions

This data represent an in vivo demonstration of both antitumoral and antioxidant effects of UT hydroalcoholic extract. The antineoplastic activity may result, partially at least, from the ability of UT to regulate redox and metabolism homeostasis.     

Analysis of immunological enhancement of immunosuppressed chickens by Chinese herbal extracts

Ethnopharmacological relevance

Radix astragali, Radix codonopis, Herba epimedii and Radix glycyrrizae are 4 plants commonly used in Chinese traditional medicine or veterinary medicine to improve immune functions against chronic diseases in humans and animals.

Aim of the study

We compared immunological enhancement by 4 herbal extracts in clinical healthy chickens or immunosuppressed chickens singly and in combination.

Materials and methods

Water extracts of 4 herbs individually and in different combinations were supplemented in drinking water. Hemagglutination inhibition (HI) antibody titers against Newcastle disease virus (NDV) and H5 avian influenza virus (H5-AIV) after vaccination were measured as indicators to evaluate immunological stimulation across groups supplemented with different herbal extracts. The experiments were conducted in both clinically healthy chickens and chickens with immunosuppression induced by reticuloendotheliosis virus (REV) infection.

Results

In clinically healthy chickens HI antibody titers against NDV and H5-AIV after vaccination were not influenced by supplementation with the herbal extracts of Radix astragali, Radix codonopis, Herba epimedii and Radix glycyrrizae in drinking water. In chicks with REV-induced immunosuppression, however, supplementation of some herbal extracts significantly increased HI antibody titers to NDV and H5-AIV when compared to the immunosuppressed control group (P < 0.01), but the titers were still lower than those in chicks not infected by REV. The 4 herbal mixtures produced the best enhancement among various combinations. The components of the herbal extract were water soluble and treatment by ether had no influence on immunological enhancement. The molecular weights of the active components of the herbal extracts were in the range of 10,000–100,000 Da.

Conclusion

Our results show that the herbal extract supplementation in drinking water can induce an immune stimulation response in immunosuppressed chickens.It suggests that chickens with REV infection-induced immunosuppression could be used as an experiment model for determination of immunological enhancement effects of some herbal components.     

Antidiabetic activity of Paspalum scrobiculatum Linn. in alloxan induced diabetic rats

Ethnopharmacological relevance

Paspalum scrobiculatum Linn. (Poaceae) is traditionally used to treat diabetes mellitus. The grains of Paspalum scrobiculatum are having potential in the development of drug for diabetes due to their antidiabetic activity.

Aim of the study

To evaluate the antidiabetic activity of aqueous and ethanolic extracts of grains of Paspalum scrobiculatum Linn. (Poaceae) in alloxan induced diabetic rats.

Materials and methods

Aqueous and ethanolic extracts (250 and 500 mg/kg body weight), were administered orally to male Wistar albino rats. Alloxan monohydrate was used to induce diabetes mellitus. Total phenolic content was estimated in the extracts. The parameters studied included oral glucose tolerance test, fasting blood glucose, serum insulin and glycated haemoglobin levels, liver glycogen content, serum lipid profile, and changes in body weights.

Results

In oral glucose tolerance test, reduction of fasting blood glucose levels took place from 60 min of extract administration. The extracts produced a dose-dependent fall in fasting blood glucose (FBG). After 15 days of treatment with extracts the maximum reduction in FBG (35.14%) was observed in diabetic rats treated with ethanolic extract 500 mg/kg dose. A significant increase in serum insulin level was observed in the treated rats. Serum lipid levels were reversed towards near normal and a control in the loss of body weight was observed in treated rats as compared to diabetic control. The extract treatment also showed a significant increase in the liver glycogen and a significant decrease in glycated haemoglobin levels. The results demonstrate that Paspalum scrobiculatum possesses significant antidiabetic activity in diabetic rats.

Conclusion

The results suggest that Paspalum scrobiculatum has antidiabetic activity, thereby justifying its traditional claim and augmenting it into the present day systems of medicine.     

A combination extract of Renshen (Panax Ginseng), Yinyanghuo (Herba Epimedii Brevicornus), Yuanzhi (Radix Palygalae) and Jianghuang (Rhizoma Curcumae Longae) decreases glycogen synthase kinase 3β expression in brain cortex of APPV717I transgenic mice

Objective

To investigate the neuroprotective mechanism of combination extract of Renshen (Panax Ginseng), Yinyanghuo (Herba Epimedii Brevicornus), Yuanzhi (Radix Palygalae) and Jianghuang (Rhizoma Curcumae Longae) (GEPT) in treating Alzheimer's disease on the target of glycogen synthase kinase 3β (GSK-3β).

Methods

Three-month-old APPV717I transgenic mice were randomly divided into ten groups (n=12 per group) and intragastrically administrated vehicle or medicines: APP group was given 0.5% CMC, donepezil group was given donepezil (APP + D group) (0.92 mg/kg⁻¹ · day⁻¹), and GEPT groups were given small dose of GEPT (APP+Gs group) (0.075 g/kg⁻¹ · day⁻¹), medium dose (APP+Gm group) (0.15 g/kg⁻¹ ·day⁻¹), and large dose (APP+Gl group) (0.30 g/kg⁻¹ · day⁻¹) for 4 or 8 months, respectively. Three-month-old C57BL/6J mice as vehicle controls (n=12) were given 0.5% CMC for 4 or 8 months as well. The GSK-3β expression in the cortex of 7- and 11-month-old APPV717I transgenic mice with and without GEPT or donepezil treatment and normal C57BL/6J mice were measured via Western blotting and Immunohistochemistry.

Results

Immunohistochemistry analysis showed significant increase of GSK-3β in the cerebral cortex of 7-month-old APP group (compare to control group P=0.003), while the GSK-3β expression of donepezil or GEPT group were all significantly decreased (Donepezil vs APP: P=0.041; Gl vs APP: P= 0.049; Gm vs APP: P=0.029; Gh vs APP: P=0.036). Western blot analysis showed similar results. The densitometric measures of GSK-3β in APP mice increased significantly as compared with the control group (P=0.008). And the GSK-3β expression in donepezil and GEPT groups were all decreased. There was significant difference between Gh group or donepezil group and the control group (P=0.05). Similar findings were shown in the 11-month-old mice in each group, except for greater decrease of GSK-3β in the GEPT group.

Conclusion

GEPT can effectively decrease the level of GSK-3β expression in the brain cortex of AP-PV717I transgenic mice, and such effect is more significant in 11-month-old mice. This partially explains the neuroprotecting mechanism of GEPT in preventing and treating of AD.     

蒙古扁桃药材不同提取物对高脂血症大鼠血脂、脂质过氧化和肝功能的影响

目的:探究蒙古扁桃药材不同提取物对高脂血症大鼠血脂、脂质过氧化和肝功能的影响。方法:依次以乙酸乙酯、正丁醇和水提取蒙古扁桃种仁,得各部提取物。Wistar雄性大鼠60只按体重均衡随机分组,分别为正常组(10只)和模型组(50只),正常组给予普通饲料饲养,模型组采用高脂饲料喂养法建立高脂模型。建模成功后,持续按前述方法饲养,同时模型组分组为模型组、阳性药组(血脂康,0.061 7 g·kg-1)、给药组(乙酸乙酯组、正丁醇组和水提物组,2.0 g·kg-1),每组10只,其中正常组与模型组ig给予生理盐水,实验组分别以蒙古扁桃乙酸乙酯提取物、正丁醇提取物和水提取物ig给药。给药7周后测定大鼠血清总胆固醇(total cholesterol,TC),甘油三酯(triglyceride,TG),高密度脂蛋白胆固醇(high-density lipoprotein cholesterol,HDL-C),低密度脂蛋白胆固醇(low-density lipoprotein cholesterol,LDL-C),丙氨酸氨基转氨酶(alanine aminotransferase,ALT),天门冬氨酸氨基转氨酶(aspartate transaminase,AST),丙二醛(malondialdehyde,MDA),超氧化物歧化酶(superoxide dismutase,SOD),过氧化物酶(peroxidase,POD),过氧化氢酶(catalase,CAT),谷胱甘肽(glutathione,GSH)和谷胱甘肽过氧化物酶(glutathione peroxidase,GSH-Px),并计算动脉粥样硬化指数(AI),低密度脂蛋白与高密度脂蛋白的比值(LDLC/HDL-C)。结果:与正常组比较,模型组大鼠TC,LDL-C,AST,AI,LDL-C/HDL-C,MDA水平明显升高(P0.01);与高脂模型组比较,正丁醇组能显著降低TC,LDL-C,AST,AI,LDL-C/HDL-C,MDA水平(P0.05),显著升高SOD,POD,GSH-Px水平(P0.05);水提物组能显著升高POD(P0.05)。结论:蒙古扁桃药材的正丁醇提取物能显著降低高脂血症大鼠的血脂水平和抵抗脂质过氧化,并且能降低发生心血管疾病的危险性和对肝脏起到一定的保护作用。改善过氧化脂质在大鼠肝脏内的蓄积,减少氧化应激,这可能是正丁醇提取物降血脂的有效机制之一。     

Toxicity assessment of Leonuri Herba aqueous extract orally administered to rats for 13 consecutive weeks

Ethnopharmacological relevance

The Leonuri Herba has been traditionally used for women's disease in Asian countries.

Aim of the study

The objective of the present study was to evaluate the subchronic toxicity of Leonuri Herba aqueous extract in male and female F344 rats.

Material and methods

Leonuri Herba aqueous extract was administered orally once daily at dose levels of 0, 125, 250, 500, 1000 and 2000 mg/kg/day for 13 weeks. Toxicological assessment was performed including mortality, clinical signs, body and organ weights, food consumption, ophthalmology, urinalysis, hematology, serum chemistry, gross findings and histopathologic examination.

Results

There were no treatment related differences in clinical signs, urinalysis, hematology and serum chemistry, except for a histopathologic examination. The squamous cell hyperplasia in the forestomach was observed in both sexes of rats given 2000 mg/kg/day of Leonuri Herba aqueous extract.

Conclusion

In conclusion, the NOAEL (No Observed Adverse Effect Level) for Leonuri Herba aqueous extract was determined as 1000 mg/kg/day in both sexes of rats under the present experimental conditions. And the acceptable daily intake value for Leonuri Herba aqueous extract was calculated to be 10 mg/kg body weight per day using a safety factor of 100 to the NOAEL.     

Hepatoprotective effect of Trichosanthes cucumerina Var cucumerina L. on carbon tetrachloride induced liver damage in rats

Ethnopharmacological relevance

Different parts of the plant Trichosanthes cucumerina Var cucumerina L. (cucurbitaceae) are used to treat liver disorders, traditionally. It is one among the constituents in various Ayurvedic formulations used for the treatment of liver disorders and other diseases.

Aims of study

The aim of the present study is to evaluate the protective effect of Trichosanthes cucumerina against experimentally induced liver injury.

Materials and methods

The methanolic extract of whole plant of Trichosanthes cucumerina (TCME) was evaluated for the hepatoprotective activity against carbon tetrachloride (CCl₄) induced hepatotoxicity in rats. Various biochemical parameters like alanine amino transferase (ALT), aspartate amino transferase (AST), alkaline phosphatase (ALP), total bilirubin (TB), total protein (TP) and albumin (ALB) levels were estimated in serum as well as the glutathione (GSH) and malondialdehyde (MDA) levels in the liver were determined. Histopathological changes in the liver of different groups were also studied.

Results

The pre-treatment of TCME at dose levels of 250 and 500 mg/kg b.w.p.o. had controlled the raise of AST, ALT, ALP, TB and MDA levels and the effects were comparable with standard drug (silymarin 100 mg/kg b.w.p.o.). The GSH, TP and ALB levels were significantly increased in the animals received pre-treatment of the extract. The animals received pre-treatment of the extract shown decreased necrotic zones and hepatocellular degeneration when compared to the liver exposed to CCl₄ intoxication alone. Thus the histopathalogical studies also supported the protective effect of the extract.

Conclusion

This study demonstrates the hepatoprotective activity of Trichosanthes cucumerina and thus scientifically supports the usage of this plant in various Ayurvedic preparations and traditional medicine for treatment of liver disorders.     

Diuretic activity of some Smilax canariensis fractions

Ethnopharmacological relevance

Smilax canariensis is an endemic species of the Canary Islands, popularly known as “Zarzaparrilla sin espinas”. The rhizome, leaves and stem of this species has wide use in folk medicine practice on the islands, where they are habitually employed as diuretic.

Aim of the study

In this paper we report on the diuretic activity in experimental animals of several fractions of the methanol extract of this species.

Materials and methods

Four fractions of the methanol extract of the rhizomes, leaves and stem of Smilax canariensis (50 and 100 mg/kg), Furosemide and Hydrochlorotiazide (10 mg/kg), were orally administered to laboratory animals to evaluate their diuretic activity. Water excretion rate, pH, conductivity, and content of Na⁺, K⁺ and Cl⁻ were measured in the urine of saline-loaded mice.

Results

All the studied extracts showed an interesting increase of the diuresis, although the n-buthanol (27%; p < 0.05) and ethyl acetate extract (35%; p < 0.01), at 100 mg/kg p.o., showed the most interesting diuretic activity, which suggested that this diuretic effect is associated with the compounds contained in the fractions of intermediate polarity (ethyl acetate and n-butanol), decreasing in the most extreme apolar and polar sub-extracts (dichloromethane and methanol: water respectively). The increase in diuresis produced by these two extracts was very close to the values of Hydrochlorothiazide (32%) or Furosemide (39%), used as reference diuretics.

Conclusions

These data, together with previous results on the aqueous and methanol extracts, reaffirm assertions made regarding the effectiveness of the extracts of this plant against urinary pathologies in the Canary Islands folk medicine.     

In vitro and in vivo hepatoprotective and antioxidant activity of ethanolic extract from Meconopsis integrifolia (Maxim.) Franch

Ethnopharmacological relevance

Meconopsis integrifolia (Maxim.) Franch is a high mountain endemic species used as a traditional Tibetan and Mongolian herb to treat hepatitis, pneumonia, and edema. This study aims to investigate the hepatoprotective and antioxidant effects of Meconopsis integrifolia ethanolic extract (MIE) in vitro and in vivo.

Materials and methods

The in vitro antioxidant property of MIE was investigated by employing various established systems. Rats with carbon tetrachloride (CCl₄)-induced liver injury were used to assess the hepatoprotective and antioxidant effect of MIE in vivo. The level or activity of alkaline phosphatase (ALP), glutamate pyruvate transaminase (ALT), aspartate aminotransferase (AST), and total bilirubin (TB) in the blood serum and thiobarbituric acid reactive substances (TBARS), superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) in the liver and kidney of the rats were assayed using standard procedures.

Results

MIE exhibited strong antioxidant ability in vitro. In the rats with CCl₄-induced liver injury, the groups treated with MIE and silymarin showed significantly lower levels of ALT, AST, ALP, and TB. MIE demonstrated good antioxidant activities in both the liver and kidney of the rats in vivo.

Conclusions

MIE exhibits excellent hepatoprotective effects and antioxidant activities in vitro and in vivo, supporting the traditional use of Meconopsis integrifolia in the treatment of hepatitis.