The effect of a strongly basic alkaloidal fraction of Rhazya stricta,a traditional medicinal plant,on cytochrome P450-mediated metabolism of theophylline in mice

The strongly basic alkaloidal fraction of the traditional medicinal plant Rhazya stricta (RS) was given orally to mice, in a single dose of 10 mg/kg (group 1) or, twice daily for 3 days at the same dose (group 2). A third group (control) received normal saline. Liver homogenates from all animals were used to assess the microsomal activity of cytochrome P450 and its isoforms as well as its catalytic activity (using theophylline as a substrate). RS alkaloidal fraction had no significant effect on the total amount of microsomal cytochrome P450, but it caused a significant increase in the cytochrome P450 isoforms CYPs 1A1 and 1A2. It also significantly increased the concentrations of some metabolites of theophylline. These results suggest that RS has the potential to interact with other drugs that are biotransformed by cytochrome P450, when given concomitantly with it.     

白花蛇舌草核苷体外抗肿瘤作用实验研究

目的 探讨白花蛇舌草中核苷的体外抗肿瘤作用.方法 采用24孔板培养法和MTT法观察白花蛇舌草核苷对人红白血病细胞株K562、人非小细胞肺癌细胞株A549的抑制作用.结果 显微镜下观察24孔板,白花蛇舌草核苷呈现明显的抗肿瘤作用.体外抑瘤实验表明,白花蛇舌草核苷对两种细胞株起效的最低药物浓度分别为100 μg/ml和50μg/ml,半数致死量IC50分别是248.1 μg/ml和147.7 μg/ml.结论 白花蛇舌草核苷具有抗肿瘤活性.     

An evaluation of toxicity of Taxus baccata Linn. (Talispatra) in experimental animals.

A toxicological study was performed in albino mice and rat with methanolic extract and isolated alkaloid of Taxus baccata Linn. (family: Taxaceae). LD(50) study showed the higher toxic activity in stem (TXA-1,2,3) as compared with leaf (TXB-1,2,3) extract. As the extract were further fractionated into crude alkaloids and purified by chromatography the toxicity of these fractions were found to be in increasing order as follows: methanolic extract (1) < crude alkaloidal fraction (2) < purified alkaloidal fraction (3). The effects of leaf and stem extract of T. baccata were studied on certain biochemical and haematological parameters of mice and rat after 10, 20 and 30 days of exposure. Among the parameters examined, the exposed animal exhibited significant decrease in total leukocyte count (TLC), lymphocytes and cholesterol level (mg/dl), whereas increase was observed in serum transminases (SGOT, SGPT) and alkaline phosphatase (AP) of TXA-1 and TXB-1 treated groups indicating toxic conditions associated due to liver involvement.     

Anti-inflammatory,antipyretic and antinociceptive activities of Tabernaemontana pandacaqui Poir

Studies on carrageenin-induced rat paw edema, yeast-induced hyperthermia in rat and writhing response induced by acetic acid in mice showed that the alcoholic extract of stems of Tabernaemontana pandacaqui (T. pandacaqui) has significant anti-inflammatory, antipyretic and antinociceptive activities. These activities are due to alkaloidal components since they were also observed when the crude alkaloidal (CA) fraction separated from alcoholic extract was tested in the same models.     

Neuropharmacological activities of the crude alkaloidal fraction from stems of Tabernaemontana pandacaqui Poir.

The crude alkaloidal (CA) fraction from the stem of Tabernaemontana pandacaqui Poir. was studied for its pharmacological activity on the central nervous system (CNS) of animals. The CA fraction was found to produce symptoms of CNS depression in conscious rats and mice, viz. reduction in spontaneous motility, potentiation of pentobarbital sleeping time, prolongation of latency of convulsions induced by pentylenetetrazole and antinociception. However, the fraction could not antagonize oxotremorine-induced tremor. The observations suggest that the CA fraction possesses a CNS depressant activity.     

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.     

Evaluation of the wound healing effect of some Jordanian traditional medicinal plants formulated in Pluronic F127 using mice (Mus musculus)

The wound healing effect of the aqueous extracts of Inula viscosa, Ajuga chia, Rubia taenifolia and Parieteria diffusa, and the oil of Laurus nobilis, dispersed in water, were examined. The 10% (w/w) Pluronic F127 (PF127) was added to the applied preparations, in order to modify the aqueous extracts viscosity, and to stabilize the oil dispersion. A full thickness wound was made in the dorsal area of the mice. The wounds were treated with the different preparations with 12h intervals for four times in two successive days. For 16 days, the wounds were visually observed, photographically documented and the wound area was measured. After day 16, the animals were sacrificed and the histology of the wound area was examined. The best wound healing activity was observed with the extract of Inula viscosa, followed by Parieteria diffusa, Laurus nobilis, Ajuga chia and the least active extract was that of Rubia taenifolia.     

Anticonvulsant activity of root and stem extracts of Calliandra portoricensis

A comparative study of the anticonvulsant properties of root and stem extracts of Calliandra portoricensis was carried out in mice. The convulsion models were pentylenetetrazole- and electroshock-induced convulsions. The results showed that the aqueous extracts of both root and stem possess anticonvulsant activity when given intraperitoneally. An alkaloidal extract did not show any anticonvulsant action up to 316 mg/kg i.p.     

Effect of alkaloids of Solanum melongena on the central nervous system

Crude alkaloidal fraction isolated from the leaves of Solanum melongena was screened for its effects on the central nervous system. It exhibited significant analgesic effect and some CNS depression but no anticonvulsant action. The analgesic effects were of non-narcotic type. LD50 was estimated to be higher than 1 g/kg i.p. in mice.     

Leishmanicidal activity of two canthin-6-one alkaloids,two major constituents of Zanthoxylum chiloperone var. angustifolium

The crude alkaloidal extract of Zanthoxylum chiloperone stem bark exhibited in vitro activity against various strains of Leishmania ssp. at 100 μg/ml. Two active major constituents were isolated and identified as canthin-6-one and 5-methoxycanthin-6-one. The effect of these compounds was also tested in an in vivo assay using BALB/c mice infected with Leishmania amazonensis. The mice were treated for 5 weeks postinfection with these alkaloids by oral (14 days) or intralesional route (4 days) at 10 mg/kg daily. The reference drug, N-methylglucamine antimonate was administered by subcutaneous injections at 100 mg/kg for 10 days. Intralesional administration of canthin-6-one reduced the parasite burden but not significantly when it was compared with the untreated group, while the reference drug reduced by 91% the parasite loads in the lesion.     

Analgesic studies on total alkaloids and alcohol extracts of Eclipta alba (Linn.) Hassk

A variety of analgesics are used for the treatment of acute and chronic pain in different disease states. A narcotic or a non-narcotic analgesic that does not cause respiratory depression and addiction is needed. In Ayurveda a large number of indigenous drugs have been mentioned possessing analgesic properties (e.g. Guggul, Erand, Rasna, Bhringaraj, Methika, Palandu and Prasikayavani). The present experimental research work was undertaken to determine the analgesic activity of the total ethanol extract of Eclipta alba, and also the isolated alkaloids of Eclipta alba in albino mice by using standard experimental models such as the tail clip method, the tail flick method and the acetic acid induced writhing response. The results from this study show that both the ethanol extract as well as the total alkaloids produce good analgesic activity in all the different models of analgesia used. The total alkaloidal fraction was the most efficacious in all models tested.     

Antiprotozoal activity of quinoline alkaloids isolated from Galipea longiflora,a Bolivian plant used as a treatment for cutaneous leishmaniasis

The stem bark of Galipea longiflora is used by the Chimane Indians in Bolivia for the treatment of cutaneous leishmaniasis produced by Leishmania braziliensis. Petroleum ether and chloroform extracts of stem, root bark and leaves were found active in vitro against Leishmania ssp and Trypanosoma cruzi at 100 μg/mL. The activity guided fractionation of the extracts by chromatography afforded 12 active compounds identified as 2-substituted quinoline alkaloids. BALB/c mice were infected with Leishmania amazonensis (strain PH8 or H-142) and treated 24 h after infection with the major alkaloids from the crude alkaloidal extract; 2-phenylquinoline and 2-n-pentylquinoline. 2-phenylquinoline was as potent as Glucantime (Rhǒne-Poulenc) against the strain H-142, but less active than the reference drug against the virulent strain PH8 of L. amazonensis. 2-n-pentylquinoline did not exhibit any activity. Assays of single local treatments on the rear footpad infection, 2 weeks after the parasitic inoculation, indicated an effect for 2-phenylquinoline by reducing the severity of lesion. However, this activity was found to be slightly lower than that obtained using Glucantime.     

Boerhaavia diffusa: a study of its hepatoprotective activity

An alcoholic extract of whole plant Boerhaavia diffusa given orally exhibited hepatoprotective activity against experimentally induced carbon tetrachloride hepatotoxicity in rats and mice. The extract also produced an increase in normal bile flow in rats suggesting a strong choleretic activity. The extract does not show any signs of toxicity up to an oral dose of 2 g/kg in mice.     

Investigation on the hypoglycaemic effects of extracts of four Mexican medicinal plants in normal and alloxan-diabetic mice

The hypoglycaemic activities of four water ethanol extracts (WEE) prepared from Bidens pilosa L., Salvia officinalis L., Psacalium peltatum H.B.K. (Cass) and Turnera diffusa Willd. were investigated in healthy and alloxan-diabetic mice. The WEE of S. officinalis significantly reduced the blood glucose of fasting normal mice 120 (15.7%) and 240 min (30.2%) after intraperitoneal administration (p < 0.05). The WEE of P. peltatum and B. pilosa also significantly diminished glycaemia in healthy mice at 240 min (19.6% and 13.8%, respectively). In mildly diabetic mice, the WEE of P. peltatum lowered the basal blood glucose level 120 (16%) and 240 min (54%) after intraperitoneal administration (p < 0.05 and p < 0.01, respectively). The WEE of B. pilosa and S. officinalis also significantly diminished the hyperglycaemia in mildly diabetic mice at 240 mins (32.6% and 22.7%, respectively). The administration of these three extracts to animals with severe hyperglycaemia did not cause a significant decrease. The WEE of T. diffusa did not show any hypoglycaemic activity. Thus, three of the WEE studied conserved the hypoglycaemic activity originally detected in the traditional preparations of the studied antidiabetic plants. It appears that these extracts require the presence of insulin to show hypoglycaemic activity.     

白花蛇舌草抑制肝癌H22小鼠淋巴管转移的实验研究

目的:观察白花蛇舌草对小鼠肝癌淋巴管转移的影响。方法:在小鼠右下肢爪垫内侧皮下注射接种腹水型肝癌H22瘤株,复制淋巴管转移模型。将模型小鼠随机分为5组,空白组每天灌生理盐水,大、中、小剂量组每天灌白花蛇舌草水煎液,对照组给予环磷酰胺腹腔注射。观察小鼠体质量、免疫器官、肺部转移率、爪垫移植瘤、淋巴结转移瘤等指标变化。结果:白花蛇舌草作用组的小鼠,体质量和免疫器官胸腺质量明显增长,肺部瘤结节数和肺部转移瘤生长指数均下降,且淋巴结转移数明显减少。结论:白花蛇舌草对H22肝癌淋巴管转移有一定抑制作用。     

Hypoglycemic effect of extracts and fractions from Psacalium decompositum in healthy and alloxan-diabetic mice

The hypoglycemic effect of the hexane, methanol and water extracts obtained from roots of Psacalium decompositum (Asteraceae) was investigated in fasting healthy mice. Only the water extract significantly reduced blood glucose in a dose-dependent manner in normal mice after intraperitoneal administration (P<0.05). This water extract was macerated with methanol obtaining a precipitate (WMP fraction), and it was studied in healthy and alloxan-diabetic mice. The WMP fraction showed significant hypoglycemic activity in healthy and mild diabetic mice, but the administration of this fraction to animals with severe diabetes did not cause any significant decrease in blood glucose levels. Two polysaccharide components isolated from WMP fraction showed hypoglycemic effect when tested in healthy mice.     

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.     

Hepatoprotective activity of indigtone--a bioactive fraction from Indigofera tinctoria Linn.

A bioactive fraction, indigtone (FA), obtained by fractionation of a petroleum ether extract of the aerial parts of Indigofera tinctoria, showed significant dose related hepatoprotective activity against CCl(4) induced liver injury in rats and mice. Hexobarbitone induced 'sleeptime', zoxazolamine induced 'paralysis time', levels of transaminases, bilirubin and total protein in serum were employed as indices of liver injury. Pre and post treatment with FA significantly reversed the majority of the parameters altered by the hepatotoxin. This indicated the preventive and restorative effect of FA in the process of CCl(4) induced liver damage. The fraction possessed a high therapeutic ratio, as no mortality was observed up to a dose of 2 g/kg p.o. in mice.     

具有乙酰胆碱酯酶抑制活性的总生物碱提取物的筛选

目的:从采自甘肃文县和舟曲的22种植物的总生物碱提取物中筛选具有乙酰胆碱酯酶抑制活性的提取物,为进一步寻找天然乙酰胆碱酯酶抑制剂单体成分奠定基础。方法:采用酸提碱沉法提取生物碱,用改良的Ellman比色法测定总生物碱的抗乙酰胆碱酯酶活性。结果:弯柱唐松草(Thalictrumuncinulatum Franch.)、阔叶十大功劳(Mahnia bealei(Fort.)Steam.)、蚬壳花椒(Zanthoxylum dissitumHemsl.)、刺柄南星(Arisaema aspeiatum N.E.Brown)、一把伞南星(Arisaema erunescens(Wall.)Schott)、猫儿屎(Decaisnea insignis(Griff)Hook.f.et thoms)、虎耳草(Saxifraga stolonifera curt.)和西固凤仙花(Impot-iens notolopha Maxim.)的总生物碱提取物具有明显的乙酰胆碱酯酶抑制活性,其IC50值分别为2.3μg.mL-1、2.9μg.mL-1、3.5μg.mL-1、11.0μg.mL-1、16.9μg.mL-1、22.7μg....