Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 20
Filtrar
Mais filtros










Intervalo de ano de publicação
1.
Indian J Exp Biol ; 52(12): 1186-94, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25651612

RESUMO

Mikania scandens, a twining herb that grows as a weed in India and Bangladesh is used as vegetables and is a good source of vitamin A, C, B complex, mikanin, sesquiterpenes, betasitosterin, stigmasterol and friedelin. The present communication reports CNS depressant activities with special emphasis to brain biogenic amines in mice. Ethanol extract of leaves of M. scandens (EEMS) was prepared by Soxhalation and analyzed chemically. EEMS potentiated sleeping time induced by pentobarbitone, diazepam and meprobamate and showed significant reduction in the number of writhes and stretches. EEMS caused significant protection against pentylene tetrazole-induced convulsion and increased catecholamines and brain amino acids level significantly. Results showed that EEMS produced good CNS depressant effects in mice.


Assuntos
Aminas Biogênicas/metabolismo , Encéfalo/efeitos dos fármacos , Depressores do Sistema Nervoso Central/farmacologia , Mikania/química , Extratos Vegetais/farmacologia , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Anticonvulsivantes/isolamento & purificação , Anticonvulsivantes/farmacologia , Encéfalo/metabolismo , Depressores do Sistema Nervoso Central/isolamento & purificação , Relação Dose-Resposta a Droga , Etanol/química , Feminino , Masculino , Camundongos , Atividade Motora/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Reflexo/efeitos dos fármacos , Convulsões/induzido quimicamente , Convulsões/prevenção & controle , Tetrazóis , Testes de Toxicidade Aguda
2.
J Diet Suppl ; 9(3): 166-77, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22891989

RESUMO

CONTEXT: Mimusops elengi (M. elengi) Linn. (Sapotaceae) has been used as a folk medicine in wound healing, and the treatment of pain, and inflammation in many parts of India. OBJECTIVE: The purpose of this investigation was to explore the antitumor activity of methanol extract of M. elengi (MEME) in Swiss albino mice against Ehrlich ascites carcinoma (EAC) cell line. MATERIALS AND METHODS: Twenty-four hours after intraperitoneal (i.p.) inoculation of tumor (EAC) cells in mice (n = 12), MEME was administered at 200 and 300 mg/kg body weight daily for 9 consecutive days. On day 10, half of the mice were dissected and the rest were kept alive for assessment of increase in life span. The antitumor effect of MEME was assessed by evaluating tumor volume, viable and nonviable tumor cell count, tumor weight, hematological parameter, and biochemical estimations. In vivo antioxidant parameters were assayed by estimating liver tissue enzyme. In vitro cytotoxicity assay of MEME was measured by using trypan blue exclusion method. RESULTS AND DISCUSSION: MEME showed significant (p < .001) decrease in tumor volume, packed cell volume, and viable cell count, and increased the life span of EAC bearing mice. Hematological, biochemical profile, and in vivo antioxidant parameters were significantly restored toward normal levels in MEME-treated mice as compared to EAC control. MEME also showed direct cytotoxicity on EAC cell line in a dose-dependent manner. CONCLUSIONS: The present study demonstrates that M. elengi leaves exhibited antitumor activity in Swiss mice, which may be due to its cytotoxic effect and antioxidant properties.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Mimusops , Fitoterapia , Extratos Vegetais/uso terapêutico , Animais , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Ascite , Masculino , Camundongos , Camundongos Endogâmicos , Extratos Vegetais/farmacologia , Folhas de Planta
3.
J Diet Suppl ; 9(1): 9-18, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22432799

RESUMO

Tephrosia purpurea (Fabaceae) is a well-known traditional plant with diuretic effect but no scientific work published till date to support the claimed ethnomedical use. Therefore, the present study appraised the diuretic potential of methanol extract of Tephrosia purpurea (METP) in male wistar rats. The powdered plant material was extracted with methanol by hot extraction. The animals were divided into five groups for diuretic activity. The first group served as saline control (0.9%% saline solution, 25 ml/kg, body weight (b.w)), the second group received osmotic diuretic, urea (1 g/kg b.w), the third group received high-ceiling diuretic, furosemide (5 mg/kg b.w), and the other two groups were administered various concentrations of METP (200 mg/kg and 400 mg/kg b.w) orally to hydrated rats and their urine volume was measured at 5th and 24th hr after drug administration, while animals were deprived of food and water. After collection of urine, the parameters such as urine output, diuretic activity, electrolyte excretion of Na(++), K(++), Ca(2++), and Cl(-), and pH were analyzed. METP at various dose levels exhibited significant diuretic activity as evidenced by increased urine volume, electrolyte concentration, and alkaline pH in comparison to control group of animals. The present study provides a quantitative basis for explaining the folkloric use of Tephrosia purpurea as a diuretic agent in Indian traditional system of medicine.


Assuntos
Diurese/efeitos dos fármacos , Diuréticos/farmacologia , Eletrólitos/urina , Preparações de Plantas/farmacologia , Tephrosia , Micção/efeitos dos fármacos , Animais , Furosemida/farmacologia , Concentração de Íons de Hidrogênio , Masculino , Ayurveda , Ratos , Ratos Wistar , Ureia/farmacologia
4.
Pharm Biol ; 50(3): 304-9, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22321031

RESUMO

CONTEXT: Clerodendrum infortunatum Linn. is a widely used plant in the Indian indigenous system of medicine for the treatment of tumors. OBJECTIVE: The present study evaluated the anticancer activity of methanol extract of C. infortunatum (MECI) against Ehrlich's ascites carcinoma (EAC) bearing Swiss albino mice and isolation of bioactive terpenoids from it. METHODS: HPLC analysis of the methanol extract showed the presence of three major components. Out of those, two compounds were isolated and characterized as oleanolic acid and clerodinin A. The anticancer activity of MECI was assessed by measuring the tumor growth response, percentage increase of life span, study of hematological parameters, lipid peroxidation, antioxidant enzyme activity like glutathion and CAT. In vitro cytotoxicity assay was also performed using EAC cell lines. RESULT AND CONCLUSION: Treatment with MECI causes significant decrease in the tumor cell volume and increase in the life span. The median survival time (MST) of EAC control group was found as 19.42 ± 0.91 d, whereas the MST was increased to 23.44 ± 2.69 d and 27.57 ± 2.57 d for the groups treated with MECI at 100 and 200 mg/kg, respectively. All the hematological parameters, malonaldehyde content and antioxidant enzymes' activity were restored towards the normal level. IC(50) value of MECI was found as 498.33 µg/mL in cytotoxicity study. The experimental results suggested that MECI has significant anticancer activity, which can be attributed to the presence of oleanolic acid and clerodinin A.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Carcinoma de Ehrlich/tratamento farmacológico , Clerodendrum/química , Terpenos/farmacologia , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antioxidantes/metabolismo , Carcinoma de Ehrlich/patologia , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão/métodos , Relação Dose-Resposta a Droga , Índia , Concentração Inibidora 50 , Peroxidação de Lipídeos/efeitos dos fármacos , Medicina Tradicional , Camundongos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Taxa de Sobrevida , Terpenos/administração & dosagem , Terpenos/isolamento & purificação
5.
Pharm Biol ; 50(6): 747-53, 2012 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22092072

RESUMO

CONTEXT: Celsia coromandelina Vahl (Scrophulariaceae) is a shrub found throughout Bangladesh and India, and it is distributed widely in the plains of West Bengal. It is used by the tribal people to treat diarrhea, dysentery, insomnia, skin eruption, fever, syphilis, helminthes infection, and to control fertility. OBJECTIVE: The objective of this study was to fractionate stigmasterol derivative and to investigate the effects of petroleum ether extract of C. coromandelina (PECC) aerial parts on the onset of reproductive maturity and the ovarian steroidogenesis in immature female mice. MATERIALS AND METHODS: PECC was prepared by hot extraction process and one compound was isolated by preparative TLC from it. PECC was completely freed from solvent and administered in immature female mice intraperitoneally once on every alternate day for nine doses. The sexual maturity was observed by means of vaginal opening, first estrus (days), rate of body growth, changes in weight of ovary, uterus and pituitary. The content of ascorbic acid, cholesterol, Δ5-3ß-hydroxy steroid dehydrogenase (Δ5-3ß-HSD) and glucose 6-phosphate dehydrogenase (G 6-PDH) activities in ovaries and carbonic anhydrase activity in uterus were measured by means of biochemical technique in control and treated mice. The activity of PECC was compared with standard marker compound ethinyl estradiol. RESULTS: The isolated compound was characterized as stigmasterol derivative. PECC treatment caused a remarkable delay (30.27 and 18.56%, respectively, by low dose) in sexual maturity compared to vehicle control as evidenced by the age of vaginal opening and appearance of first estrus (cornified smear). PECC treatment also caused a significant fall (58.6 and 50.0%, respectively, by low dose) in Δ5-3ß-HSD and G 6-PDH activities involved in ovarian steroidogenesis compared to vehicle control. Total cholesterol and ascorbic acid content in ovaries and carbonic anhydrase activity in uterus were increased significantly (low dose by 49.3, 424.6 and 82.4%, respectively) along with a reduction in the weight of ovary, uterus and pituitary in comparison to that of control. DISCUSSION AND CONCLUSION: Overall, these results demonstrate that PECC has a good antifertility effect and is responsible for the delayed development of sexual maturity, suppression of ovarian steroidogenesis and elevation of carbonic anhydrase activity in uterus of immature mice. This supports the claim by tribal people as a potential remedy for birth control.


Assuntos
Anticoncepcionais Femininos/farmacologia , Ovário/efeitos dos fármacos , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Scrophulariaceae/química , Maturidade Sexual/efeitos dos fármacos , Estigmasterol/análogos & derivados , 3-Hidroxiesteroide Desidrogenases/metabolismo , Alcanos/química , Animais , Anidrases Carbônicas/metabolismo , Anticoncepcionais Femininos/administração & dosagem , Anticoncepcionais Femininos/química , Anticoncepcionais Femininos/isolamento & purificação , Relação Dose-Resposta a Droga , Etnofarmacologia , Feminino , Glucosefosfato Desidrogenase/metabolismo , Índia , Camundongos , Tamanho do Órgão/efeitos dos fármacos , Ovário/crescimento & desenvolvimento , Ovário/metabolismo , Hipófise/efeitos dos fármacos , Hipófise/crescimento & desenvolvimento , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Solventes/química , Estigmasterol/isolamento & purificação , Estigmasterol/farmacologia , Útero/efeitos dos fármacos , Útero/crescimento & desenvolvimento , Útero/metabolismo
6.
Immunopharmacol Immunotoxicol ; 34(1): 157-62, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-21721906

RESUMO

CONTEXT: Carbon tetrachloride (CCl4) is frequently used as a chemical inducer of tissue damage. Their effects on mouse peritoneal macrophages and also in peripheral blood lymphocytes are still unknown. OBJECTIVE: Therefore we tried to focus on intracellular oxidative stress produced by CCl4 in mouse macrophage and lymphocyte cells. METHODS: Intraperitoneal administration of CCl4 induces intracellular superoxide anions production in mouse macrophages and peripheral blood lymphocytes and leads a subsequent lipid peroxidation and protein oxidation. N-acetyl cystein (NAC) and vitamin C were administered intraperitoneally at a dose of 150 mg/kg and their effect on demodulating the oxidative stress is also checked. RESULT AND DISCUSSION: Several in vitro approaches have already been established as a free radical scavenging models, but this free radical screening models is not always correlated with the in vivo screening models. NAC and vitamin C were administered intraperitoneally and significant reduction of the oxidative stress in term of scavenging of toxic superoxide anion observed in both the macrophages and lymphocytes. CONCLUSION: Therefore we are hopeful that our work will light a new insight into the screening of in vivo free radical scavenging model for evaluating anti-inflammatory compounds.


Assuntos
Intoxicação por Tetracloreto de Carbono/metabolismo , Tetracloreto de Carbono/toxicidade , Linfócitos/metabolismo , Macrófagos Peritoneais/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Acetilcisteína/farmacologia , Animais , Ácido Ascórbico/farmacologia , Intoxicação por Tetracloreto de Carbono/patologia , Sequestradores de Radicais Livres/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Linfócitos/patologia , Macrófagos Peritoneais/patologia , Camundongos , Superóxidos/metabolismo
7.
Pak J Pharm Sci ; 24(3): 369-75, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21715271

RESUMO

Enhydra fluctuans (Compositae), an edible semi aquatic herbaceous vegetable plant, widely used in traditional system of Indian medicine. Total flavonoids of E. fluctuans (TFEF) were screened for analgesic and anti-inflammatory activity. Analgesic activity was studied in acetic acid induced writhing response and by hot plate method in Swiss albino mice. Anti-inflammatory activity was estimated by carrageenan and histamine induced acute inflammation and Freund's complete adjuvant (FCA) induced chronic inflammation in rats. Two flavonoids, baicalein 7-O-glucoside and baicalein 7-O-diglucoside, were isolated from the ethyl acetate fraction. Oral administration of TFEF at the doses of 200 and 400 mg/kg provide 27.05 and 55.49% protection respectively in acetic acid induced writhing method. It also increased the pain threshold in mice evidenced by hot plate method. TFEF showed more potent anti-inflammatory activity. The results of this study may be attributed to high free radical scavenging and antioxidant potential of the flavonoids present in ethyl acetate fraction of Enhydra fluctuans.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Asteraceae/química , Inflamação/tratamento farmacológico , Medição da Dor/efeitos dos fármacos , Fitoterapia/métodos , Acetatos/química , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Dissacarídeos/química , Dissacarídeos/isolamento & purificação , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos/métodos , Flavonas/química , Flavonas/isolamento & purificação , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Glucosídeos/química , Glucosídeos/isolamento & purificação , Inflamação/induzido quimicamente , Masculino , Camundongos , Medição da Dor/métodos , Limiar da Dor/efeitos dos fármacos , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar
8.
Environ Toxicol Pharmacol ; 31(1): 10-7, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21787664

RESUMO

Present study reports the chemopreventive effect of methanol extract of Wedelia calendulaceae (MEWC) against 20-methylcholanthrene (20-MC) induced carcinogenesis in Swiss albino mice. MEWC was administered orally at 250 and 500 mg/kg body weight for 90 consecutive days after 24h of single subcutaneous administration of 20-MC (200 µg) in mice and observed for 15 weeks to record tumor incidence (fibrosarcoma) and survival. After 15 weeks the mice were sacrificed for the estimation of hematological profiles and liver biochemical parameters viz. lipid peroxidation, reduced glutathione (GSH), glutathione-S-transferase (GST), superoxide dismutase (SOD) and catalase (CAT). MEWC treatment markedly reduced tumor incidence and prolonged life span of sarcoma bearing mice as compared to 20-MC control. Hematological profiles were significantly (p<0.001) restored to normal levels in MEWC treated mice. MEWC treatment significantly (p<0.001) modulated the aforesaid liver biochemical parameters as compared to 20-MC control. Therefore, W. calendulaceae possess remarkable chemopreventive efficacy in Swiss mice.


Assuntos
Anticarcinógenos/farmacologia , Carcinógenos/antagonistas & inibidores , Carcinógenos/toxicidade , Metilcolantreno/toxicidade , Wedelia/química , Animais , Contagem de Células Sanguíneas , Análise Química do Sangue , Catalase/metabolismo , Glutationa/metabolismo , Glutationa Transferase/metabolismo , Testes de Função Hepática , Masculino , Camundongos , Neoplasias Experimentais/induzido quimicamente , Neoplasias Experimentais/epidemiologia , Neoplasias Experimentais/prevenção & controle , Extratos Vegetais/farmacologia , Superóxido Dismutase/metabolismo , Sobrevida , Substâncias Reativas com Ácido Tiobarbitúrico/metabolismo
9.
Pharm Biol ; 48(12): 1337-43, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-21091122

RESUMO

CONTEXT: Sansevieria roxburghiana Schult. & Schult. f. (Agavaceae) is a herbaceous perennial plant traditionally used for coughs, rheumatism; as an expectorant, febrifuge, purgative, and tonic. OBJECTIVE: To evaluate the hydroalcoholic extract of S. roxburghiana rhizome (HASR) for antitumor activity against Ehrlich ascites carcinoma (EAC) in Swiss albino mice. METHODS: Twenty-Four hours after intraperitoneal inoculation of tumor (EAC) cells in mice, HASR was administered at 50 and 100 mg/kg body weight for nine consecutive days. On day 10 half of the mice were sacrificed and rest were kept alive for assessment of increase in life-span. The antitumor effect of HASR was assessed by evaluating tumor volume, packed cell count, viable and non-viable tumor cell count, median survival time and increase in life-span of EAC bearing hosts. Hematological profiles and serum biochemical parameters were estimated. Further, antioxidant properties were assessed by estimating lipid peroxidation, reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT). RESULTS AND DISCUSSION: HASR showed a significant (p < 0.001) decrease in tumor volume, packed cell volume and viable cell count and increased the life span of EAC bearing mice. Hematological and serum biochemical profiles were restored to normal levels in HASR treated mice as compared to EAC control. HASR treatment significantly (p <0.001) decreased lipid peroxidation and recovered GSH, SOD and CAT towards normal as compared to EAC control. CONCLUSION: The present study demonstrates that S. roxburghiana rhizome exhibited remarkable antitumor activity in Swiss mice that is plausibly attributable to its augmenting endogenous antioxidant mechanisms.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Carcinoma de Ehrlich/tratamento farmacológico , Extratos Vegetais/farmacologia , Sansevieria/química , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Carcinoma de Ehrlich/patologia , Catalase/metabolismo , Relação Dose-Resposta a Droga , Glutationa/efeitos dos fármacos , Glutationa/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Extratos Vegetais/administração & dosagem , Rizoma , Superóxido Dismutase/efeitos dos fármacos , Superóxido Dismutase/metabolismo
10.
Nat Prod Commun ; 5(8): 1239-42, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20839626

RESUMO

Flavonoids obtained from Enhydra fluctuans (FEF) were screened for anticancer activity against Ehrlich's ascites carcinoma (EAC) bearing Swiss albino mice. The anticancer activity was assessed by measuring the tumor growth response, percentage increase of life span, hematological parameters, lipid peroxidation, and antioxidant enzyme activity, like GSH and CAT. Two flavonoids, baicalein 7-O-glucoside and baicalein 7-O-diglucoside, were isolated from the ethyl acetate fraction. Treatment with FEF caused a significant decrease in the tumor cell volume and increase of life span. All the hematological parameters, malonaldehyde content and antioxidant enzyme activity were restored towards the normal level. FEF was found to be cytotoxic in the in-vitro model.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Asteraceae/química , Carcinoma de Ehrlich/tratamento farmacológico , Flavonoides/farmacologia , Animais , Antioxidantes/metabolismo , Carcinoma de Ehrlich/patologia , Linhagem Celular Tumoral , Peroxidação de Lipídeos/efeitos dos fármacos , Camundongos
11.
Indian J Exp Biol ; 47(9): 743-7, 2009 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19957887

RESUMO

Saponin (SN1) isolated from C. infortunatum leaves in doses of 30, 50, 75 and 100 mg/kg, ip provided 36.28, 60.47, 90.71, 100% protection respectively from writhing induced by 1.2% v/v acetic acid. In hot plate method, SN1 not only produced analgesia in mice but also potentiated the analgesic action of pentazocine and aspirin. The anticonvulsant activity was tested by leptazol-induced seizures. SN1 decreased the duration of seizures and gave protection in a dose dependent manner against leptazol-induced convulsions. The results suggest that saponin has significant analgesic and anticonvulsant effects.


Assuntos
Analgésicos/uso terapêutico , Anticonvulsivantes/uso terapêutico , Clerodendrum , Fitoterapia , Extratos Vegetais/uso terapêutico , Folhas de Planta/química , Saponinas/uso terapêutico , Convulsões/prevenção & controle , Animais , Camundongos , Convulsões/induzido quimicamente
12.
Indian J Pharmacol ; 41(4): 176-81, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20523869

RESUMO

UNLABELLED: In drug discovery research, the compounds should not only to be potent and selective but also must possess acceptable pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) to increase success rate in clinical studies. OBJECTIVE: Exploration of drug-like properties of 2-(2-methylquinolin-4-ylamino)-N-phenyl acetamide, a potent antileishmanial compound by performing some in vitro ADME experiments along with validation of such studies. MATERIALS AND METHODS: Experimental protocols were established and validated for stability (in PBS pH7.4, simulated gastric and intestinal fluid), solubility, permeability, distribution coefficient (Log D), plasma protein binding and metabolism by rat liver microsomes by using spectrophotometer or HPLC. Methods were considered valid if the results of the standard compounds matched with reported results or within acceptable range or with proper ranking (high-medium-low). RESULTS: The compound was found to be stable (>95% remaining) in all stability studies and aqueous solubility was 299.7 +/- 6.42 muM. The parallel artificial membrane permeability assay (PAMPA) indicated its medium permeability (Log Pe = -5.53 +/- 0.01). The distribution coefficients (Log D) in octanol/PBS and cyclohexane/PBS systems were found to be 0.54 and -1.33, respectively. The plasma protein binding study by the equilibrium dialysis method was observed to be 78.82 +/- 0.13% while metabolism by Phase-I enzymes for 1 hour at 37 degrees C revealed that 36.07 +/- 4.15% of the compound remained after metabolism. CONCLUSION: The methods were found to be very useful for day-to-day ADME studies. All the studies with the antileishmanial compound ascertained that the compound bears optimum pharmacokinetic properties to be used orally as a potential drug for the treatment of leishmaniasis.

13.
Electron. j. biotechnol ; 11(3): 1-10, July 2008. ilus, graf
Artigo em Inglês | LILACS | ID: lil-531898

RESUMO

Shilajit is a panacea in Ayurveda, the Indian traditional system of medicine. The major bioactives of shilajit have been identified as dibenzo-alpha-pyrones (DBPs), its oligomers and aminoacyl conjugated derivatives. These bioactive compounds play a crucial role in energy metabolism in all animal cells including those of man. 3-hydroxydibenzo-alpha-pyrone (3-OH-DBP), a key DBP component of shilajit is converted, among other products, to another active DBP derivative, viz. 3,8-hydroxydibenzo-alpha-pyrone, 3,8(OH)2-DBP, in vivo, when its precursor is ingested. 3,8(OH)2-DBP is then involved in energy synthesis in the mitochondria in the reduction and stabilization of coenzyme Q10 in the electron transport chain. As the chemical synthesis of 3,8(OH)2-DBP is a complex, multi-step process and economically not readily viable, we envisioned the development of a process using microorganisms for bioconversion of 3-OH-DBP to 3,8(OH)2-DBP. In this study, the biotransformation of 3-OH-DBP is achieved using Aspergillus niger, which was involved in the humification process on sedimentary rocks leading to shilajit formation. A 60 percent bioconversion of 3-OH-DBP to 3,8(OH)2-DBP and to its aminoacyl derivatives was achieved. The products were characterized and estimated by high performance liquid chromatography (HPLC), high performance flash chromatography (HPFC) and gas chromatography-mass spectrometry (GC-MS) analyses. Among the Aspergillus species isolated and identified from native shilajit, A. niger was found to be the most efficient for this bioconversion.


Assuntos
Aspergillus niger , Compostos Orgânicos/metabolismo , Plantas Medicinais , Biotransformação , Cromatografia Líquida de Alta Pressão
14.
J Enzyme Inhib Med Chem ; 21(5): 501-7, 2006 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-17194018

RESUMO

Bis(1,10-phenanthroline/2,2'-bipyridine) ruthenium(II)complexes containing TCP, TTZ OPBI, and BTSC ligands (where, TCP = 1-thiocarbamoyl-3,5-diphenyl-2-pyrazoline, TTZ = 2-(3,5-diphenyl-4,5-dihydropyrazol-1-yl)-4-phenylthiazole, OPBI = 2-hydroxyphenyl benzimidazole and BTSC = benzoin thiosemicarbazone) have been prepared and characterized. The spectral data suggested that the ligands were coordinated with the metal through nitrogen, sulfur and oxygen atoms. The target complexes were tested in vivo for anticancer activity against transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC). All these complexes increased the life span of the EAC-bearing mice, decreased their tumor volume and viable ascitic cell count as well as improved Hb, RBC and WBC counts. These results suggest that the Ru(II) complexes exhibit significant antitumor activity in EAC-bearing mice. It was also observed that the ruthenium complexes protected red blood cells from 2,2'-azo-bis(2-methylpropionamidine) dihydrochloride (AAPH)- induced hemolysis. The inhibitory effect was dose-dependent at a concentration of 20-120 microg/ml.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/uso terapêutico , Compostos de Rutênio/síntese química , Compostos de Rutênio/uso terapêutico , Animais , Antineoplásicos/química , Carcinoma de Ehrlich/tratamento farmacológico , Carcinoma de Ehrlich/patologia , Linhagem Celular Tumoral , Masculino , Camundongos , Estrutura Molecular , Compostos de Rutênio/química , Relação Estrutura-Atividade
15.
J Enzyme Inhib Med Chem ; 19(2): 185-92, 2004 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15449735

RESUMO

These ligands (L) show a bidentate behavior, forming octahedral ruthenium complexes. The title complexes were subjected to in-vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC) and in-vitro antibacterial activity against several Gram positive and Gram negative bacterial strains. [Ru(bpy)2(ihqs)]Cl2 and [Ru(bpy)2 (hc)]Cl2 (where bpy = 2,2'-bipyridine, ihqs = 7-iodo-8hydroxy quinoline-5-sulphonic acid and hc = 3-hydroxy coumarin) showed promising antitumor activity. Treatment with these complexes prolonged the life span of EAC bearing mice as well as decreased their tumor volume and viable ascitic cell count. All the tested complexes exhibited mild to moderate antibacterial activity.


Assuntos
Antibacterianos/síntese química , Antibacterianos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Compostos de Rutênio/síntese química , Compostos de Rutênio/farmacologia , Animais , Carcinoma de Ehrlich , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Bactérias Gram-Negativas , Bactérias Gram-Positivas/efeitos dos fármacos , Camundongos
16.
Acta Pharmacol Sin ; 25(8): 1070-6, 2004 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-15301742

RESUMO

AIM: To study the antitumor effect and antioxidant role of Bauhinia racemosa. METHODS: Antitumor activity and antioxidant status of methanol extract (50, 100, and 200 mg/kg) of Bauhinia racemosa stem bark was evaluated against Ehrlich ascites carcinoma (EAC) tumor in mice. Acute and short-term toxicity studies were performed initially in order to ascertain the safety of methanol extract of Bauhinia racemosa (MEBR). After 24 h of tumor inoculation, the extract was administered daily for 14 d. After administration of the last dose followed by 18 h fasting, mice were then sacrificed for observation of antitumor activity. The effect of MEBR on the growth of transplantable murine tumor, life span of EAC bearing hosts and simultaneous alterations in the hematological profile and liver biochemical parameters (lipid peroxidation, antioxidant enzymes) were estimated. RESULTS: The MEBR showed decrease in tumor volume, packed cell volume and viable cell count, and increased the nonviable cell count and mean survival time thereby increasing life span of EAC tumor bearing mice. Hematological profile reverted to more or less normal levels in extract treated mice. Treatment with MEBR decreased the levels of lipid peroxidation and increased the levels of glutathione, superoxide dismutase and catalase. CONCLUSION: The methanol extract of Bauhinia racemosa stem bark exhibited antitumor effect by modulating lipid peroxidation and augmenting antioxidant defense system in EAC bearing mice.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/uso terapêutico , Bauhinia/química , Carcinoma de Ehrlich/tratamento farmacológico , Plantas Medicinais/química , Animais , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Carcinoma de Ehrlich/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Transplante de Neoplasias , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
17.
Chem Pharm Bull (Tokyo) ; 52(2): 178-85, 2004 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-14758001

RESUMO

In search of potential anticancer drug candidates in ruthenium complexes, a series of mononuclear ruthenium complexes of the type [Ru(phen)(2)(nmit)]Cl(2) (Ru1), [Ru(bpy)(2)(nmit)]Cl(2) (Ru2), [Ru(phen)(2)(icpl)]Cl(2) (Ru3), Ru(bpy)(2)(icpl)]Cl(2) (Ru4) (phen=1,10-phenanthroline; bpy=2,2'-bipyridine; nmit=N-methyl-isatin-3-thiosemicarbazone, icpl=isatin-3-(4-Cl-phenyl)thiosemicarbazone) and [Ru(phen)(2)(aze)]Cl(2) (Ru5), [Ru(bpy)(2)(aze)]Cl(2) (Ru6) (aze=acetazolamide) and [Ru(phen)(2)(R-tsc)](ClO(4))(2) (R=methyl (Ru7), ethyl (Ru8), cyclohexyl (Ru9), 4-Cl-phenyl (10), 4-Br-phenyl (Ru11), and 4-EtO-phenyl (Ru12), tsc=thiosemicarbazone) were prepared and characterized by elemental analysis, FTIR, (1)H-NMR and FAB-MS. Effect of these complexes on the growth of a transplantable murine tumor cell line (Ehrlich Ascites Carcinoma) and their antibacterial activity were studied. In cancer study the effect of hematological profile of the tumor hosts have also been studied. In the cancer study, the complexes Ru1-Ru4, Ru10 and Ru11 have remarkably decreased the tumor volume and viable ascitic cell count as indicated by trypan blue dye exclusion test (p<0.05). Treatment with the ruthenium complexes prolonged the lifespan of Ehrlich Ascites Carcinoma (EAC) bearing mice. Tumor inhibition by the ruthenium chelates was followed by improvements in hemoglobin, RBC and WBC values. All the complexes showed antibacterial activity, except Ru5 and Ru6. Thus, the results suggest that these ruthenium complexes have significant antitumor property and antibacterial activity. The results also reflect that the drug does not adversely affect the hematological profiles as compared to that of cisplatin on the host.


Assuntos
Antibacterianos , Antineoplásicos , Compostos Organometálicos , Rutênio , Animais , Antibacterianos/síntese química , Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Sobrevivência Celular/efeitos dos fármacos , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Compostos Organometálicos/síntese química , Compostos Organometálicos/química , Compostos Organometálicos/uso terapêutico , Rutênio/química , Rutênio/farmacologia , Rutênio/uso terapêutico , Relação Estrutura-Atividade , Células Tumorais Cultivadas
18.
J Pharmacol Sci ; 94(2): 177-84, 2004 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-14978356

RESUMO

The methanol extract of Caesalpinia bonducella FLEMING (Caesalpiniaceae) leaves (MECB) were evaluated for antitumor activity against Ehrlich ascites carcinoma (EAC)-bearing Swiss albino mice. The extract was administered at the doses of 50, 100, and 200 mg/kg body weight per day for 14 days after 24 h of tumor inoculation. After the last dose and 18 h fasting, the mice were sacrificed. The present study deals with the effect of MECB on the growth of transplantable murine tumor, life span of EAC-bearing hosts, hematological profile, and biochemical parameters such as lipid peroxidation (LPO), glutathione content (GSH), superoxide dismutase (SOD), and catalase (CAT) activities. MECB caused significant (P<0.01) decrease in tumor volume, packed cell volume, and viable cell count; and it prolonged the life span of EAC-tumor bearing mice. Hematological profile converted to more or less normal levels in extract-treated mice. MECB significantly (P<0.05) decreased the levels of lipid peroxidation and significantly (P<0.05) increased the levels of GSH, SOD, and CAT. The MECB was found to be devoid of conspicuous short-term toxicity in the mice when administered daily (i.p.) for 14 days at the doses of 50, 100, 200, and 300 mg/kg. The treated mice showed conspicuous toxic symptoms only at 300 mg/kg. The results indicate that MECB exhibited significant antitumor and antioxidant activity in EAC-bearing mice.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Antioxidantes/uso terapêutico , Caesalpinia , Carcinoma de Ehrlich/tratamento farmacológico , Animais , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Carcinoma de Ehrlich/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Peroxidação de Lipídeos/fisiologia , Masculino , Camundongos , Extratos Vegetais/uso terapêutico , Folhas de Planta
19.
Acta Pol Pharm ; 60(3): 207-10, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-14556490

RESUMO

The methanolic extract of both Cuscuta reflexa stem and Corchorus olitorius seed showed marked protection against convulsion induced by chemoconvulsive agents in mice. The catecholamines contained were significantly increased in the processed extract treated mice. The amount of GABA, which is most likely to be involved in seizure activity, was increased significantly in mice brain after a six week treatment. Results of the present study revealed that both the processed extracts showed a significant anticonvulsive property by altering the level of catecholamines and brain amino acids in mice.


Assuntos
Aminas Biogênicas/metabolismo , Química Encefálica/efeitos dos fármacos , Corchorus/química , Cuscuta/química , Animais , Anticonvulsivantes/farmacologia , Catecolaminas/metabolismo , Convulsivantes , Masculino , Camundongos , Neurotransmissores/metabolismo , Extratos Vegetais/farmacologia , Sementes/química , Convulsões/induzido quimicamente , Convulsões/prevenção & controle , Serotonina/metabolismo , Estricnina
20.
Acta Pol Pharm ; 60(4): 317-23, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-14714862

RESUMO

Methanol extract of Cuscuta reflexa Roxb. stem (MECR) contain flavonoids (0.2%) and Corchorus olitorius Linn. seed (MECO) was found to contain steroids and cardenolide glycosides. Effects of multiple weekly dose of MECR (25, 50, 75 mg/kg, i.p.) and MECO (15, 20, 25 mg/kg, i.p.) on liver and kidney functions and hematological parameters in mice were studied. No significant alteration of RBC count and hemoglobin content was observed in all dose level of treatment in MECR and MECO treated mice whereas significant increase of clotting time was seen in moderate and high doses in both case. MECR and MECO both caused significant increase in WBC count only in high dose level of treatment. Both the extracts in medium and high dose level increased SGOT, SGPT, NPN and plasma cholesterol significantly. Serum alkaline phosphatase and total bilirubin were also increased by both moderate and high dose level of treatments in MECR and MECO treated mice respectively. Low dose of both the extract did not exhibit any significant change of creatinine and serum protein level. But high dose level of MECR and MECO significantly increased creatinine level. Increase in plasma cholesterol may be due to decrease in cholesterol catabolism owing to liver dysfunction of due to the intake of MECO itself as it was found to be steroid in nature. Elevated level of SGOT, SGPT and serum alkaline phosphatase activity in moderate and high dose level of weekly treated mice may be due to improper liver function following the treatment. Increased urea, non protein nitrogen and creatinine content in blood have been observed with impaired renal function. The slightly higher toxicity in case of MECO treated mice may be due to the presence of cardenolide glycosides in the ME of C. olitorius seed. However, low doses of MECR and MECO (25 and 15 mg/kg, i.p. respectively) did not exhibit any remarkable change on liver and kidney functions and hematological parameters.


Assuntos
Corchorus/química , Cuscuta/química , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Animais , Células Sanguíneas/efeitos dos fármacos , Análise Química do Sangue , Corchorus/toxicidade , Cuscuta/toxicidade , Testes de Função Renal , Contagem de Leucócitos , Testes de Função Hepática , Masculino , Camundongos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Sementes/química
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...