Effect of ethanol extract of Sphaeranthus indicus on cisplatin-induced nephrotoxicity in rats

Cisplatin is an anticancer drug extensively used against a variety of cancers. Cisplatin chemotherapy is found to manifest dose-dependent nephrotoxicity. Depletion of the renal antioxidant defence system has been suggested to be the main cause of cisplatin-induced nephrotoxicity. The purpose of this study is to investigate whether the ethanol extract of entire plant of Sphaeranthus indicus could reduce the intensity of toxicity in albino rats. Nephrotoxicity was assessed by determining the serum creatinine and urea levels and renal antioxidant status in rats after cisplatin administration (12?mg?kg(-1)?body weight, i.p.). The ethanol extract of S. indicus (150 and 300?mg?kg(-1)?body weight) was administered orally from the sixth day onwards for 10 days after cisplatin administration. The extract significantly reduced the elevated serum creatinine and urea levels. Renal antioxidant defence systems, such as superoxide dismutase, catalase, glutathione peroxidase activities and reduced glutathione level that are depleted by cisplatin therapy were restored to normal by treatment with the extract. Cisplatin-induced lipid peroxidation was also found to be markedly reduced by treatment with the extract. These results suggest that S. indicus has protective effect against cisplatin-induced nephrotoxicity, which may be attributed to its antioxidant potential.     

Effects of Pithecellobium jiringa ethanol extract against ethanol-induced gastric mucosal injuries in Sprague-Dawley rats

Current anti-gastric ulcer agents have side effects, despite the progression and expansion of advances in treatment. This study aimed to investigate the gastroprotective mechanisms of Pithecellobium jiringa ethanol extract against ethanol-induced gastric mucosal ulcers in rats. For this purpose, Sprague Dawley rats were randomly divided into five groups: Group 1 (normal control) rats were orally administered with vehicle (carboxymethyl cellulose), Group 2 (ulcer control) rats were also orally administered with vehicle. Group 3 (positive control) rats were orally administered with 20 mg/kg omeprazole, Groups 4 and 5 (experimental groups) received ethanol extract of Pithecellobium jiringa ethanol extract at a concentration of 250 and 500 mg/kg, respectively. Sixty minutes later, vehicle was given orally to the normal control group, and absolute ethanol was given orally to the ulcer control, positive control and experimental groups to generate gastric mucosal injury. The rats were sacrificed an hour later. The effect of oral administration of plant extract on ethanol-induced gastric mucosal injury was studied grossly and histology. The level of lipid peroxidation (malondialdehyde-MDA), superoxide dismutase (SOD) and gastric wall mucus were measured from gastric mucosal homogenate. The ulcer control group exhibited severe gastric mucosal injury, and this finding was also confirmed by histology of gastric mucosa which showed severe damage to the gastric mucosa with edema and leucocyte infiltration of the submucosal layer. Pre-treatment with plant extract significantly reduced the formation of ethanol-induced gastric lesions, and gastric wall mucus was significantly preserved. The study also indicated a significant increase in SOD activity in gastric mucosal homogenate, whereas a significant decrease in MDA was observed. Acute toxicity tests did not show any signs of toxicity and mortality up to 5 g/kg. The ulcer protective effect of this plant may possibly be due to its preservation of gastric wall mucus along with increased SOD activity and reduction of oxidative stress (MDA). The extract is non-toxic, even at relatively high concentrations.     

Hypoglycaemic effects of tea extracts and ent-kaurenoic acid from Smallanthus sonchifolius

Hypoglycaemic activity was observed in normoglycaemic mice orally administered with the aqueous Smallanthus sonchifolius leaf tea extract, alloxan-induced diabetic mice orally administered with ent-kaurenoic acid (1), and normoglycaemic mice intraperitoneally administered with 1 from S. sonchifolius leaves. A single dose administration of 50 mg kg(-1) BW yacon leaf tea extract demonstrated immediate but relatively short hypoglycaemic activity, with significant effects observed during 1-2 h. Similarly, administration with 100 mg kg(-1) BW yacon leaf tea extract obtained by heavy stirring in hot water demonstrated a more potent activity compared to the positive control at 1.5-2.0 h. Oral administration of 1 did not affect the blood glucose level of the alloxan-induced diabetic mice, but a single intraperitonial injection of 10 mg kg(-1) BW in normoglycaemic mice had consistent percent blood glucose reduction persisting from 1 to 2 h observation periods.     

Six New Triterpene Saponins with a 21,23‐Lactone Skeleton from Gynostemma pentaphyllum

The six new triterpene saponins 1 – 6 with a 21,23‐lactone skeleton were isolated from the MeOH extract of the aerial parts of Gynostemma pentaphyllum. Their structures were elucidated by 1D‐ and 2D‐NMR‐spectra interpretation as well as by chemical degradation.     

低交换量混胺树脂的合成及其对绞股蓝皂甙的吸附性能

高交联聚苯乙烯型树脂S-008(Ⅰ)氯甲基化后,以不同比例的三甲胺/二甲胺混合胺或三甲按/二乙醇胺混合胺胺化,合成了同时含有季铵和叔氨基的混胺树脂Ⅱ-Ⅺ,研究了它们对绞股蓝皂甙的吸附性能,发现树脂的比表面和极性基团对其吸附量均有明显影响,此外,这些树脂对绞股蓝皂甙呈现出一定的吸附选择性和良好的解吸选择性。     

Novel dammarane-type glycosides from Gynostemma pentaphyllum

Three new dammarane glycosides (1-3), together with five known compounds, gypenoside LXIX (4), gylongiposide I (5), gypenoside XLVIII (6), allantion (7) and vitexin (8) were isolated from the MeOH extract of the aerial parts of Gynostemma pentaphyllum. Compounds 5, 7, and 8 were isolated from this plant for the first time. Their structures were elucidated by 1D and 2D NMR spectra interpretation as well as by chemical degradation.     

Toxicity and anticancer effects of an extract from Selaginella tamariscina on a mice model

The toxicity and antitumour effect of the ethanol extract of Selaginella tamariscina (STE), a plant widely used in folk medicine, were examined in a mice model. In the single-dose acute toxicity test, an oral administration of 10,000?mg?kg(-1) STE did not cause any lethality. The sub-acute toxicity study showed that the treatment by 250,?1000 and 3000?mg?kg(-1?)day(-1) for 30 continuous days did neither alter the body weights nor the haematological parameters in BALB/c mice. The anticancer effect of STE was evaluated in BALB/c mice inoculated with Lewis lung carcinoma cells. Oral administration of STE could not prevent the tumour formation but provided strong inhibition of tumour growth.     

Biological fate of 3H-labeled penfluridol. (3) Correlation between concentration of 3H-penfluridol in the brain and its anti-methamphetamine activity]

The Penfluridol (PFL) is a potent and long-acting neuroleptic belonging to the diphenylbutyl piperidine series. The purpose of the present study is to investigate a correlation between the brain concentration of unchanged 3H-PFL and its neuroleptic activity in the methamphetamine-antagonism test. The experimental animal comprised adult male Wistar rats weighing about 200 g. All the rats were administered 3H-PFL orally and killed at appropriate times after administration. After killing blood samples were collected and the brain and liver were excised. The blood was extracted with 4 volumes of ethanol. The brain and the liver were homogenized in 9 volumes of ethanol. The amount of 3H-PFL in the ethanol extract was determined by thin-layer chromatography. The result showed that the drug level in the brain was relatively constant when the dose was the median effective dose (ED50) for the test at those time intervals after administration.     

Effects of 2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide on various ulcer models in rats.

The effects of 2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide (compd. III-1a) on various experimental ulcers were investigated. The oral administration of compd. III-1a at doses ranging from 30 to 300 mg/kg inhibited the acute gastric ulcerations induced by ethanol, HCl.aspirin and indomethacin in rats. Compound III-1a significantly inhibited the water immersion stress-induced gastric ulcer at doses of 3 mg/kg, p.o. The anti-ulcer activity of plaunotol as a reference drug was equivalent on an ethanol-induced ulcer to that of compd. III-1a, but weaker on HCl.aspirin, indomethacin and stress-induced ulcers than that of compd. III-1a. On indomethacin-produced gastric antral ulcer, compd. III-1a showed the same significant inhibitory activity as spizofurone did at a dose of 100 mg/kg, p.o. Compound III-1a also inhibited hemorrhagic shock-, diethyldithiocarbamic acid (DDC)-and platelet activating factor (PAF)-induced ulcers dose-dependently. Plaunotol only showed significant inhibitory activity on PAF-induced ulcer in these three ucler models. The consecutive administration of compd. III-1a (100 mg/kg, p.o.) twice a day significantly accelerated the healing of an acetic acid-induced ulcer and that of plaunotol (200 mg/kg, p.o.) showed the same activity. Moreover, orally administered compd. III-1a at a dose of 100 mg/kg decreased the gastric acid secretion in pylorus-ligated rats. The results in the present study suggest that compd. III-1a has the dual action on ulcer formation.     

Inhibition of experimental pulmonary metastasis of Lewis lung carcinoma by orally administered beta-glucan in mice

The inhibitory effect on experimental pulmonary metastasis of Lewis lung carcinoma (3LL) of SSG, a (1----3)-beta-D-glucan obtained from the fungus Sclerotinia sclerotiorum IFO 9395, administered orally was examined in mice. Oral administration of SSG for 10 consecutive days just after the intravenous implantation of tumor cells significantly inhibited the experimental pulmonary metastasis of 3LL at a dose of 2000 micrograms. However, SSG administered orally involving other timings was less effective. In comparison with oral administration, SSG was effective when administered intraperitoneally for 10 consecutive days at a dose of 200 micrograms. These results suggest that SSG given by both parenteral and nonparenteral routes is effective in the inhibition of experimental pulmonary metastasis of tumors.     

Comparative study on effects of single and multiple oral administration of mungbean (Phaseolus radiatus L.) seed extract on the pharmacokinetics of aconitine by UHPLC‐MS

The study was aimed to investigate the effects of single and multiple oral administration of mungbean (Phaseolus radiatus L.) seed extract (ME) on the pharmacokinetics of aconitine in rats. The Sprague–Dawley rats were randomly divided into three groups (six rats each group). In group 1, rats were orally administered 500 µg/kg aconitine after receiving a single oral dose of 1 g/kg ME. In group 2, rats were orally administered with 500 µg/kg aconitine at day 7 of treatment with 1 g/kg/day ME. In group 3, rats were orally administered with 500 µg/kg aconitine. Blood samples were collected at different time points (0.083, 0.25, 0.5, 1.0, 1.5, 2.0, 4.0, 6.0, 8.0 and 10.0 h). The concentration of aconitine in rats plasma was determined by a fully validated ultra‐high‐performance liquid chromatography coupled with mass spectrometry method. The results showed that single and multiple oral co‐administration of ME significantly altered the pharmacokinetic parameters of aconitine. Copyright © 2014 John Wiley & Sons, Ltd.     

Improvement of Obesity and Dyslipidemic Activity of Amomum tsao-ko in C57BL/6 Mice Fed a High-Carbohydrate Diet

Amomum tsao-ko Crevost et Lemaire (Zingiberaceae) is a medicinal herb found in Southeast Asia that is used for the treatment of malaria, abdominal pain, dyspepsia, etc. The aim of this study was to investigate the effect of an ethanol extract of Amomum tsao-ko (EAT) on obesity and hyperlipidemia in C57BL/6 mice fed a high-carbohydrate diet (HCD). First, the mice were divided into five groups (n = 6/group) as follows: normal diet, HCD, and HCD+EAT (100, 200, and 400 mg/kg/day), which were orally administered with EAT daily for 84 days. Using microcomputed tomography (micro-CT) analysis, we found that EAT inhibited not only body-weight gain, but also visceral fat and subcutaneous fat accumulation. Histological analysis confirmed that EAT decreased the size of fat tissues. EAT consistently improved various indices, including plasma levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein, high-density lipoprotein, atherogenic index, and cardiac risk factors, which are related to dyslipidemia—a major risk factor for heart disease. The contents of TC and TG, as well as the lipid droplets of HCD-induced hepatic accumulation in the liver tissue, were suppressed by EAT. Taken together, these findings suggest the possibility of developing EAT as a therapeutic agent for improving HCD-induced obesity and hyperlipidemia.     

A new lignan from Gynostemma pentaphyllum

A new lignan ligballinone 1 with the know ligballinol 2 were isolated from plant Gynostemma pentaphyllum.Their structures were determined through spectroscopic methods including ESI-MS,1D and 2D NMR (1H,13C,DEPT,1H-1H COSY,HMQC,RMBC) and X-ray diffraction experiment for 2.     

红芪药材防治肝纤维化的谱效关系

研究了红芪药材的高效液相色谱(HPLC)指纹图谱与抗肝纤维化作用之间的谱效关系。采用四氯化碳(CCl₄)-花生油(体积比为4:6)皮下注射(0.1 mL/10 g, 1次/5 d)致小鼠肝纤维化,同时灌胃给予红芪各不同溶剂提取物(10 g原药材/kg, 1次/d), 5周后测定与肝纤维化有关的各血清指标及肝重指数,结果乙醇提取物药效最佳。运用灰色关联度和偏最小二乘法研究了不同产地红芪药材乙醇提取部位的HPLC指纹图谱与抗肝纤维化药效之间的谱效相关性。结果红芪乙醇提取物中多数成分与抗肝纤维化药效均有高度关联性(>0.8),表明该药效是红芪中所有成分共同作用的结果;同时鉴定出腺苷、毛蕊异黄酮及芒柄花苷3种成分,其中腺苷及毛蕊异黄酮对药效有较大贡献。     

Antitumour and antioxidant activity of Scutia myrtina against Ehrlich ascites carcinoma in Swiss albino mice

The aim of this study is to investigate the antitumour and antioxidant activities of the ethanol extract of Scutia myrtina (EESM) against Ehrlich's ascites carcinoma (EAC) in mice. Twenty-four hours after tumour inoculation, EESM was administered at doses 100, 200 and 300?mg?kg?1 bodyweight/mice/day for 21 days. EESM caused a significant (p?相似文献   

Linagliptin,a Selective Dipeptidyl Peptidase-4 Inhibitor,Reduces Physical and Behavioral Effects of Morphine Withdrawal

(1) Background: Recent data indicate that receptors for GLP-1 peptide are involved in the activity of the mesolimbic system. Thus, the purpose of the present study was to examine the effect of the selective dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, on morphine dependence in mice. (2) Methods: Morphine dependence in mice was obtained by administration of increasing doses of morphine for eight consecutive days, twice a day. On the 9th day of the experiment, the naloxone-induced (2 mg/kg, ip) morphine withdrawal signs (jumping) were assessed. Moreover, behavioral effects of short-term (60 h after morphine discontinuation) and long-term (14 days after morphine discontinuation) morphine withdrawal were observed. In terms of behavioral effects, the depressive effect in the forced swim test and anxiety in the elevated plus maze test were investigated. Locomotor activity of mice was also studied. (3) Results: The administration of linagliptin (10 and 20 mg/kg, ip) for 8 consecutive days before morphine injections significantly diminished the number of naloxone-induced morphine withdrawal signs (jumping) in mice. In addition, the cessation of morphine administration induced depressive behavior in mice which were observed during short- and long-term morphine withdrawal. Linagliptin administered during morphine withdrawal significantly reduced the depressive behavior in studied mice. Furthermore, the short-term morphine withdrawal evoked anxiety which also was reduced by linagliptin in mice. (4) Conclusions: The present study reveals that GLP-1 receptors are involved in morphine dependence. What is more, linagliptin might be a valuable drug in attenuating the physical symptoms of morphine dependence. It might be also a useful drug in reducing emotional disturbances which may develop during the morphine withdrawal period.     

Acute toxicity and metabolism of arsenocholine in mice

The acute toxicity of arsenocholine was examined in mice by oral administration and intravenous injection. The LD₅₀ values of arsenocholine were 6.5 g kg^?1 for oral administration and 187 mg kg^?1 for oral administration and 187 mg kg^?1 for intravenous injection. Decreases of respiration and spontaneous motility were observed in the mice dosed orally at 12 g kg^?1. The animals exhibited ataxia and finally showed paralysis of the hind legs within 20 min of administration. When arsenocholine was administered orally to mice at 5 or 50 mg As kg^?1, the greater part of the arsenic administered was recovered in urine within 96 h. The metabolite of arsenocholine in urine was identified as arsenobetaine by high-performance liquid chromatography-inductively coupled plasma emission spectrometry (HPLC ICP) and fast atom bombardment mass spectrometry (FAB MS). These results suggested that the major part of orally administered arsenocholine was absorbed from the gastrointestinal tract in mice and then rapidly excreted in urine with biotransformation.     

Antidepressant-like effect of Casimiroa pubescens root extracts

In this study, we investigated the antidepressant-like effects of the hexane (HCP), ethyl acetate (ECP) and methanol (MCP) extracts of the roots of Casimiroa pubescens Ramírez (Rutaceae) using the forced swim test (FST). In an initial experiment, each extract was orally administered to mice only once 60 min before to the FST. In a second experiment, doses were administered 24, 7 and 1 h before testing. Our results showed that the triple administration of the extracts provided a stronger effect than single administration. However, the combination of HCP at 7.5 mg/kg and imipramine (IMI) at 12.5 mg/kg showed the greatest effect. The coumarins 3-(1′,1′, dimethyl allyl)-herniarin, auraptene, 8-geranyl-oxy psoralen, isopimpinellin and the flavonoid zapotin were isolated from the extracts. The hexane extract of C. pubescens showed an antidepressant-like activity, which may inspire further studies on developing new antidepressant agents.     

地黄提取物改善贫血大鼠记忆及其机制

地黄滋阴补血填髓,广泛用于贫血和脑疾病患者,但其功效机制尚未阐明.本文探讨地黄水提物(Rehmannia glutinosa’s water extracts,RGWE)改善血虚大鼠记忆及其滋阴补血填髓的可能机制.采用断尾放血结合注射环磷酰胺制备贫血大鼠模型,随机分溶媒组和地黄水提物3,6,10g/kg治疗组,灌服等体积自来水或不同剂量地黄水提物10天,采用Morris水迷宫观测大鼠空间记忆能力,采用酶联免疫吸附测定方法(Enzyme linked immunosorbent assay,ELISA)检测血浆红细胞生成素(EPO)水平,免疫组化和免疫蛋白印迹技术(Western blotting)检测分析脑EPO及其受体表达水平.成功制备血虚模型,表现为大鼠红细胞数和血红蛋白显著下降,与造模前比较差异显著(P<0.05),溶媒组空间记忆能力显著下降,地黄治疗组空间记忆能力明显提高,逃避潜伏期明显缩短(P<0.05),一定时间内穿越平台次数显著增多(P<0.05);免疫组化和Western blotting结果显示脑组织EPO及其受体表达、血浆EPO水平均较溶媒组明显升高(P<0.05).地黄水提物显著提高贫血...     

Immunoadjuvant and Humoral Immune Responses of Garlic (Allium sativum L.) Lectins upon Systemic and Mucosal Administration in BALB/c Mice

Dietary food components have the ability to affect immune function; following absorption, specifically orally ingested dietary food containing lectins can systemically modulate the immune cells and affect the response to self- and co-administered food antigens. The mannose-binding lectins from garlic (Allium sativum agglutinins; ASAs) were identified as immunodulatory proteins in vitro. The objective of the present study was to assess the immunogenicity and adjuvanticity of garlic agglutinins and to evaluate whether they have adjuvant properties in vivo for a weak antigen ovalbumin (OVA). Garlic lectins (ASA I and ASA II) were administered by intranasal (50 days duration) and intradermal (14 days duration) routes, and the anti-lectin and anti-OVA immune (IgG) responses in the control and test groups of the BALB/c mice were assessed for humoral immunogenicity. Lectins, co-administered with OVA, were examined for lectin-induced anti-OVA IgG response to assess their adjuvant properties. The splenic and thymic indices were evaluated as a measure of immunomodulatory functions. Intradermal administration of ASA I and ASA II had showed a four-fold and two-fold increase in anti-lectin IgG response, respectively, vs. the control on day 14. In the intranasal route, the increases were 3-fold and 2.4-fold for ASA I and ASA II, respectively, on day 50. No decrease in the body weights of animals was noticed; the increases in the spleen and thymus weights, as well as their indices, were significant in the lectin groups. In the adjuvanticity study by intranasal administration, ASA I co-administered with ovalbumin (OVA) induced a remarkable increase in anti-OVA IgG response (~six-fold; p < 0.001) compared to the control, and ASA II induced a four-fold increase vs. the control on day 50. The results indicated that ASA was a potent immunogen which induced mucosal immunogenicity to the antigens that were administered intranasally in BALB/c mice. The observations made of the in vivo study indicate that ASA I has the potential use as an oral and mucosal adjuvant to deliver candidate weak antigens. Further clinical studies in humans are required to confirm its applicability.