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1.
Appl Biochem Biotechnol ; 194(5): 1955-1980, 2022 May.
Artículo en Inglés | MEDLINE | ID: mdl-35006552

RESUMEN

Contaminated rice is a major source of food poisoning in human communities where our earlier study showed Stenotrophomonas maltophilia, a Gram-negative bacillus, has been a major contaminant of the stored rice. In the present study, mono- and di-unsaturated fatty acids (UFAs) such as 18:1 ω 7 c, 16:1 ω 6 c, 16:1 ω 7 c, and 18:2 ω 6,9 c long-chain fatty acids have been found as the chief constituents of S. maltophilia boiled cell lysate. Throughout the study, both acute and chronic exposure of the cell lysate showed a decrease in the locomotor activity and a time-dependent increase of the depression (p < 0.001-0.0001, two-way ANOVA), supported by bioamine (dopamine, noradrenaline, adrenaline, serotonin, and GABA) depletion in rodents' brain possibly due to UFA-amino acid decarboxylase interaction favoring bioamine depletion as revealed by our study. Furthermore, the UFA-rich cell lysate revealed dose-dependent inhibition of murine brain microglial cell viability in vitro with concomitant increase of reactive oxygen species (ROS) inside the cell. Destruction of neuroprotective and neurotrophin releasing microglial cells, augmentation of brain ROS, and inflaming brain tissue resulting in infiltration of polymorphonuclear leucocytes also suggest to cause neurotoxicity by UFA derived from Stenotrophomonas maltophilia.


Asunto(s)
Infecciones por Bacterias Gramnegativas , Oryza , Stenotrophomonas maltophilia , Animales , Ácidos Grasos Insaturados , Ratones , Especies Reactivas de Oxígeno
2.
Asian Pac J Trop Med ; 5(8): 616-22, 2012 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-22840449

RESUMEN

OBJECTIVE: To evaluate the possible antifertility activity of Enicostemma axillare (E. axillare) leaves and Urena lobata (U. lobata) root in adult male Wistar albino rats. METHODS: Six groups of rats were treated with ethanolic (70%v/v) extracts of E. axillare (375 and 750 mg/kg body weight) and U. lobata root (300 and 600 mg/kg body weight) once daily for 55 days. Control groups received the distilled water and vehicle. All the treated rats had corresponding recovery groups. At the end of each treatment periods, animals were killed and organ weights, sperm characteristics, testicular and epididymal biochemicals as well as testicular enzymes were assessed. RESULTS: The E. axillare and U. lobata at tested doses did not decrease body weight, whereas the weight of testes, epididymides and seminal vesicles were significantly (P<0.01) reduced. Significantly (P<0.01) more reductions in the sperm motility, viability and counts, epididymal and testicular protein contents were noted in the rats treated with higher dose of both the plants. Both the plants at the higher dose caused a marked increase (P<0.01) in sperm morphological abnormalities, testicular cholesterol and ascorbic acid contents were remarkably increased (P<0.01), while, the activities of testicular glucose-6-phosphate dehydrogenase (G-6-PDH) and Δ(5)-3ß-hydroxy steroid dehydrogenase (Δ(5)-3ß-HSD) were significantly reduced (P<0.01). However, reversal of these changes occurred after 55 days of treatment withdrawal. CONCLUSIONS: This study suggests that the E. axillare leaves and U. lobata root reversibly inhibited spermatogenesis and steroidogenesis indicating reversible antifertility activity which could partially support the traditional of these plants as male contraceptives.


Asunto(s)
Anticonceptivos Masculinos/farmacología , Fertilidad/efectos de los fármacos , Gentianaceae , Malvaceae , Medicina Tradicional , Extractos Vegetales/farmacología , Animales , Biomarcadores/metabolismo , Peso Corporal/efectos de los fármacos , Anticonceptivos Masculinos/administración & dosificación , Relación Dosis-Respuesta a Droga , Esquema de Medicación , Genitales Masculinos/efectos de los fármacos , Genitales Masculinos/metabolismo , India , Masculino , Extractos Vegetales/administración & dosificación , Hojas de la Planta , Raíces de Plantas , Ratas , Ratas Wistar , Recuento de Espermatozoides , Motilidad Espermática/efectos de los fármacos , Espermatogénesis/efectos de los fármacos , Espermatozoides/efectos de los fármacos
3.
J Diet Suppl ; 9(1): 9-18, 2012 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-22432799

RESUMEN

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.


Asunto(s)
Diuresis/efectos de los fármacos , Diuréticos/farmacología , Electrólitos/orina , Preparaciones de Plantas/farmacología , Tephrosia , Micción/efectos de los fármacos , Animales , Furosemida/farmacología , Concentración de Iones de Hidrógeno , Masculino , Medicina Ayurvédica , Ratas , Ratas Wistar , Urea/farmacología
4.
Pharm Biol ; 50(6): 747-53, 2012 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-22092072

RESUMEN

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.


Asunto(s)
Anticonceptivos Femeninos/farmacología , Ovario/efectos de los fármacos , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacología , Scrophulariaceae/química , Maduración Sexual/efectos de los fármacos , Estigmasterol/análogos & derivados , 3-Hidroxiesteroide Deshidrogenasas/metabolismo , Alcanos/química , Animales , Anhidrasas Carbónicas/metabolismo , Anticonceptivos Femeninos/administración & dosificación , Anticonceptivos Femeninos/química , Anticonceptivos Femeninos/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Etnofarmacología , Femenino , Glucosafosfato Deshidrogenasa/metabolismo , India , Ratones , Tamaño de los Órganos/efectos de los fármacos , Ovario/crecimiento & desarrollo , Ovario/metabolismo , Hipófisis/efectos de los fármacos , Hipófisis/crecimiento & desarrollo , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Solventes/química , Estigmasterol/aislamiento & purificación , Estigmasterol/farmacología , Útero/efectos de los fármacos , Útero/crecimiento & desarrollo , Útero/metabolismo
5.
Asian Pac J Trop Biomed ; 2(9): 684-90, 2012 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-23569995

RESUMEN

OBJECTIVE: To explore the antispermatogenic and testicular antisteroidogenic activities of Feronia limonia fruit pulp southern India. METHODS: Fourty Wistar male albino rats (Rattus norvegicus) were equally divided into four groups. Experimental groups were administered with the ethanolic extract of Feronia limonia (F. limoni) fruit pulp at doses of 250 and 500 mg/kg body weight once daily for 55 days. All treated rats had corresponding recovery groups. At the end of each treatment periods, various spermatological indices, tissue biochemicals and testicular enzymes levels were analysed. Blood profiles were also estimated. RESULTS: Compared with the control, the F. limonia fruit pulp at both dose levels did not decrease body weight, which were associated with decline in epididymal sperm count, motility, viability and increased percent of abnormal sperm. Further, F. limonia fruit pulp at 500 mg/kg body weight markedly reduced the epididymal and testicular protein content by 24.58% and 29.86%, respectively, as well as the glucose-6-phosphate dehydrogenase and Δ(5)-3ß-hydroxy steroid dehydrogenase) levels by 42.82% and 38.08%, respectively, while a significant elevation was observed in testicular cholesterol and ascorbic acid content. A gradual recovery of all parameters was observed after 55 days of treatment withdrawal. No significant alterations in haematological indices were observed. CONCLUSIONS: The present findings indicate that F. limonia fruit pulp may have reversible antispermatogenic and antisteroidogenic properties, and could partially support the traditional use as male contraceptive.


Asunto(s)
Antiespermatogénicos/farmacología , Frutas/química , Extractos Vegetales/farmacología , Administración Oral , Animales , Antiespermatogénicos/administración & dosificación , Antiespermatogénicos/química , Ácido Ascórbico/química , Supervivencia Celular/efectos de los fármacos , Colesterol/química , Femenino , Dosificación Letal Mediana , Masculino , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Ratas , Recuento de Espermatozoides , Motilidad Espermática/efectos de los fármacos , Espermatozoides/efectos de los fármacos , Testículo/efectos de los fármacos , Testículo/metabolismo , Pruebas de Toxicidad Aguda , Tracheophyta/química
6.
Nat Prod Res ; 26(12): 1141-4, 2012.
Artículo en Inglés | MEDLINE | ID: mdl-22017259

RESUMEN

Terminalia arjuna Roxb. (Combretaceae), commonly known as 'Arjuna', is a large tree occurring throughout the Indian peninsula. This study was undertaken to evaluate the methanol extract of T. arjuna leaf (META) for antitumour activity against Ehrlich ascites carcinoma (EAC) in Swiss albino mice. Twenty-four hours after intraperitonial inoculation of tumour (EAC) cells in mice, META was administered at 100 and 200 mg kg(-1) body weights for 9 consecutive days. On day 10, half of the mice were sacrificed and the rest kept alive for an assessment of the increase in life span. The antitumour effect of META was assessed by evaluating tumour volume, tumour weight, viable and non-viable tumour cell counts, median survival time and increase in life span of EAC-bearing hosts. Haematological profiles were estimated. META showed a significant (p<0.001) decrease in tumour volume, tumour weight and viable cell count, and also increased the life span of EAC-bearing mice. Haematological profiles were significantly (p<0.001) restored to normal levels in META-treated mice compared to the EAC control. Therefore, from this study, it can be concluded that T. arjuna leaf exhibited remarkable antitumour activity against EAC in Swiss mice.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Carcinoma de Ehrlich/patología , Extractos Vegetales/farmacología , Terminalia/química , Animales , Antineoplásicos Fitogénicos/toxicidad , Dosificación Letal Mediana , Ratones , Extractos Vegetales/toxicidad
7.
J Ethnopharmacol ; 138(3): 769-73, 2011 Dec 08.
Artículo en Inglés | MEDLINE | ID: mdl-22041106

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: The plant Cocos nucifera Linn. (Arecaceae) is commonly known as coconut. Traditionally the juice of the young spadix when fresh is used in diarrhea and diabetes. The objective of the present study was to investigate the effect of antidiabetic activity and effect on lipid profile as well as cardioprotective effect of hydro-methanol extract of Cocos nucifera (HECN) on streptozotocin (STZ)-induced diabetic rats. MATERIALS AND METHODS: After 72 h of STZ (50 mg/kg, b.w. i.p.) administration, animals showing plasma sugar level more than 250 mg/dl were considered as diabetic rat. Fasting blood glucose (FBG) levels were measured on 0th (after 72 h of STZ), 5th, 10th, and 15th day. On the 15th day all the animals were sacrificed and the serum biochemical parameters and antioxidant enzyme status were measured. RESULTS: HECN treated animals showed a significant reduction in FBG level as compared with diabetic control group. Serum enzyme level (SGOT, SGPT, SALP), lipid peroxidation and antioxidant enzyme level such as CAT, GSH, SOD and cholesterol and triglycerides in the HECN treated groups were restored towards normal level as compared to diabetic control groups and the values were comparable with the standard groups (glibenclamide). CONCLUSION: Improvement in the FBG and the restoration of all other biomarker as well as enzymes indicates that HECN has very good antidiabetic activity with very low side effects and provides a scientific rationale for the use as an antidiabetic agent.


Asunto(s)
Cocos , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/uso terapéutico , Extractos Vegetales/uso terapéutico , Alanina Transaminasa/sangre , Fosfatasa Alcalina/sangre , Animales , Aspartato Aminotransferasas/sangre , Glucemia/análisis , Catalasa/metabolismo , Diabetes Mellitus Experimental/metabolismo , Femenino , Glutatión/metabolismo , Hipoglucemiantes/toxicidad , Peroxidación de Lípido/efectos de los fármacos , Lípidos/sangre , Masculino , Ratones , Extractos Vegetales/toxicidad , Plantas Medicinales , Ratas , Ratas Wistar , Superóxido Dismutasa/metabolismo
8.
ISRN Pharmacol ; 2011: 138737, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-22084708

RESUMEN

Context. The plant Citrus maxima Merr. (Rutaceae), commonly known as shaddock or pomelo is indigenous to tropical parts of Asia. The objective of present study is to evaluate the methanol extract of Citrus maxima leaves for its antitumor activity against Ehrlich's Ascites Carcinoma cell in Swiss albino mice. Experimental design. The antitumor activity of methanol extract of Citrus maxima leaves (MECM) was evaluated against Ehrlich Ascites Carcinoma (EAC) cell line in Swiss albino mice. 2 × 10(6) cells were inoculated in different groups of animals. MECM (200 and 400 mg/kg BW i.p.) was administered for nine consecutive days. On day 10th half the animals of different groups were sacrificed for determination of tumor and haematological parameters and the rest half were kept with sufficient food and water ad libitum for determination of increase in life span. Result and Discussions. Oral administration of the extract at the doses of 200 and 400 mg/kg significantly decreased tumor parameters such as tumor volume, viable tumor cell count and increased body weight, hematological parameters and life span in respect of the EAC control mice. Conclusion. Experimental design exhibits significant antitumor activity of the extract (MECM) in a dose dependant manner.

9.
Toxicol Mech Methods ; 21(5): 426-33, 2011 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-21417635

RESUMEN

Mycotoxin MT81 was isolated, purified, and identified from a fungal strain of Penicillium nigricans. It is a CNS depressant, hyperglycemic agent and produces massive bone marrow depression, hepatotoxicity, and nephrotoxicity. Its benzolylated analog (benzoylated-MT81) was synthesized in our laboratory having a LD50 value of 87.1 mg/kg body weight in mice. This study was designed to assess the toxicological effects of mycotoxin MT81 and its analog on testicular spermatogenesis and steroidogenesis in mature albino rats. The sperm count and percentage of motile sperm were decreased markedly in MT81- and benzoylated-MT81-treated rats. The body weight and the weight of testis were reduced, whereas weight of adrenal gland was increased in a dose-dependent manner in the toxin-treated rats. MT81 and its derivative caused accumulation of ascorbic acid and total cholesterol in the testis and reduction in the activities of Δ5-3ß-hydroxysteroid dehydrogenase (Δ5-3ß-HSD) and glucose-6-phosphate dehydrogenase (G-6-P-D), whereas the ascorbic acid and cholesterol content of adrenal gland were decreased and enzyme activities were elevated. This experiment suggests that MT81 and benzoylated-MT81 both produce inhibition of testicular spermatogenesis and steroidogenesis but increase adrenal steroidogenesis and ultimately sterility of male rats.


Asunto(s)
Antraquinonas/toxicidad , Micotoxinas/toxicidad , Espermatogénesis/efectos de los fármacos , Testículo/efectos de los fármacos , 3-Hidroxiesteroide Deshidrogenasas/metabolismo , Glándulas Suprarrenales/efectos de los fármacos , Glándulas Suprarrenales/patología , Animales , Antraquinonas/química , Ácido Ascórbico/metabolismo , Peso Corporal/efectos de los fármacos , Colesterol/metabolismo , Glucosafosfato Deshidrogenasa/metabolismo , Dosificación Letal Mediana , Masculino , Ratones , Tamaño de los Órganos/efectos de los fármacos , Ratas , Ratas Wistar , Espermatogénesis/fisiología , Testículo/metabolismo , Testículo/patología , Testosterona/metabolismo , Pruebas de Toxicidad
10.
ISRN Endocrinol ; 2011: 869273, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-22363893

RESUMEN

The present paper aims to evaluate antihyperglycemic activity of methanol extract of Citrus limetta fruit peel (MECL) in streptozotocin-induced (STZ; 65 mg/kg b.w.) diabetic rats. Three days after STZ induction, diabetic rats received MECL orally at 200 and 400 mg kg(-1) body weight daily for 15 days. Glibenclamide (0.5 mg kg(-1) p. o.) was used as reference drug. Blood glucose levels were measured on 0th, 4th, 8th, and 15th days of study. Serum biochemical parameters namely, SGOT, SGPT and ALP were estimated. The TBARS and GSH levels of pancreas, kidney, and liver were determined. MECL significantly (P < 0.001) and dose dependently normalized blood glucose levels and serum biochemical parameters, decreased lipid peroxidation, and recovered GSH as compared to those of STZ control. The present paper infers that in STZ-induced diabetic Wistar rats, C. limetta fruit peel demonstrated a potential antihyperglycemic effect which may be attributed to its antioxidant property.

11.
Oxid Med Cell Longev ; 3(1): 61-70, 2010.
Artículo en Inglés | MEDLINE | ID: mdl-20716929

RESUMEN

Many fungal toxins exhibit in vitro and in vivo antineoplastic effects on various cancer cell types. Luteoskyrin,a hydroxyanthraquinone has been proved to be a potent inhibitor against Ehrlich ascites tumor cells. The comparative antitumor activity and antioxidant status of MT81 and its structural analogue [Acetic acid-MT81 (Aa-MT81)] having polyhydroxyanthraquinone structure were assessed against Ehrlich ascites carcinoma (EAC) tumor in mice. The in vitro cytotoxicity was measured by the viability of EAC cells after direct treatment of the said compounds. In in vivo study, MT81 and its structural analogue were administered (i.p.) at the two different doses (5, 7 mg MT81; 8.93, 11.48 mg Aa-MT81/kg body weight) for 7 days after 24 hrs. of tumor inoculation. The activities were assessed using mean survival time (MST), increased life span (ILS), tumor volume, viable tumor cell count, peritoneal cell count, protein percentage and hematological parameters. Antioxidant status was determined by malondialdehyde (MDA) and reduced glutathione (GSH) content, and by the activity of superoxide dismutase (SOD) and catalase (CAT). MT81 and its structural analogues increased the mean survival time, normal peritoneal cell count. They decreased the tumor volume, viable tumor cell count, hemoglobin percentage and packed cell volume. Differential counts of WBC, total counts of RBC & WBC that altered by EAC inoculation, were restored in a dose-dependent manner. Increased MDA and decreased GSH content and reduced activity of SOD, and catalase in EAC bearing mice were returned towards normal after the treatment of MT81 and its structural analogue. Being less toxic than parent toxin MT81, the structural analogue showed more prominent antineoplastic activities against EAC cells compared to MT81. At the same time, both compounds exhibit to some extent antioxidant potential for the EAC-bearing mice.


Asunto(s)
Antraquinonas/uso terapéutico , Antineoplásicos/uso terapéutico , Carcinoma de Ehrlich/tratamiento farmacológico , Animales , Antraquinonas/farmacología , Antineoplásicos/farmacología , Carcinoma de Ehrlich/metabolismo , Catalasa/metabolismo , Células Cultivadas , Glutatión/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Malondialdehído/metabolismo , Ratones , Superóxido Dismutasa/metabolismo
12.
Am J Chin Med ; 35(1): 103-14, 2007.
Artículo en Inglés | MEDLINE | ID: mdl-17265555

RESUMEN

The aim of this study is to investigate the antioxidant defense system induced by the methanol extract of Bauhinia racemosa L.(MEBR) against N-nitrosodiethylamine (NDEA)-induced hepatocarcinogenesis in Wister albino rats. The effects of MEBR on surface visible macroscopic (Morphometry) liver lesions (neoplastic nodules) and the levels of serum enzymes, lipid peroxidation and antioxidants were evaluated in NDEA-induced hepatocarcinogenesis in rats. In rats treated, with NDEA, significantly elevated levels of serum enzymes (SGOT, SGPT and ALP), bilirubin and decreased levels of protein and uric acid were observed. Significantly elevated amount of malondialdehyde (MDA), the end product of lipidperoxidation, indicated higher levels of lipid peroxidation, which was accompanied by significantly decreased levels of antioxidants like vitamin C, vitamin E, reduced glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT). Administration of MEBR was able to suppress nodule development/hepatocellular lesion formation in rats. The extract treatment increases in antioxidant levels and dramatic decreases in lipid peroxidation levels. MEBR also produced a protective effect by decreasing the level of serum enzymes, bilirubin and increased the protein and uric acid levels. The results suggest that MEBR exert chemopreventive effects by suppressing nodule development and decreasing lipid peroxidation and enhancing the levels of antioxidants in NDEA carcinogenesis by reducing the formation of free radicals.


Asunto(s)
Bauhinia , Carcinoma Hepatocelular/prevención & control , Neoplasias Hepáticas/prevención & control , Fitoterapia/métodos , Corteza de la Planta , Alanina Transaminasa/sangre , Alquilantes , Animales , Antioxidantes/metabolismo , Aspartato Aminotransferasas/sangre , Bilirrubina/sangre , Carcinoma Hepatocelular/inducido químicamente , Quimioprevención , Dietilnitrosamina , Peroxidación de Lípido/efectos de los fármacos , Peroxidación de Lípido/fisiología , Hígado/metabolismo , Hígado/patología , Neoplasias Hepáticas/inducido químicamente , Masculino , Malondialdehído/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Wistar
13.
J Enzyme Inhib Med Chem ; 21(5): 501-7, 2006 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-17194018

RESUMEN

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.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/uso terapéutico , Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/uso terapéutico , Animales , Antineoplásicos/química , Carcinoma de Ehrlich/tratamiento farmacológico , Carcinoma de Ehrlich/patología , Línea Celular Tumoral , Masculino , Ratones , Estructura Molecular , Compuestos de Rutenio/química , Relación Estructura-Actividad
14.
Bioorg Med Chem ; 13(20): 5766-73, 2005 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-15982893

RESUMEN

A series of mononuclear Ru(II) complexes of the type [Ru(M)2(U)]2+, where M = 2,2'-bipyridine/1,10-phenanthroline and U = tpl (Ru1), 4-Cl-tpl (Ru2), 4-CH3-tpl (Ru3), 4-CH3O-tpl (Ru4), and 4-NO2-tpl (Ru5), -pai (Ru6), where tpl = thiopicolinanilide and pai = 2-phenyl-azo-imidazole, have been prepared and characterized by IR, UV-Vis, 1H NMR, 13C-NMR, FAB-Mass spectrophotometer, and elemental analysis. The complexes display metal-ligand charge transfer (MLCT) transitions in the visible region. 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 Gram positive and Gram negative microorganisms. Ru1-Ru6 were found to increase the life span of the tumor hosts by 19-52%, and decreased tumor volume and viable ascitic cell count. The results of the present study clearly demonstrated the tumor inhibitory activity of the ruthenium chelates against transplantable murine tumor cell line. The treatment with ruthenium complexes could be secondary to tumor regression or due to the action of the compounds itself. The significant antibacterial activity was observed for Ru1-Ru4 against microorganisms like Vibrio cholera 865, Staphylococcus aureus 6571, and Shigella flexneri as compared to that of standard drug chloramphenical. Ru5 showed moderate activity against S. aureus 8530. However, all the complexes fail to show significant antibacterial activity against V. cholera 14033 and Shigella sonnai.


Asunto(s)
Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/farmacología , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Ratones , Pruebas de Sensibilidad Microbiana , Análisis Espectral
15.
J Toxicol Sci ; 30(4): 265-74, 2005 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-16404135

RESUMEN

The aim of the present investigation deals with the hematology and hepatorenal function of Caesalpinia bonducella Flem. and Bauhinia racemosa Lam. belonging to the Family: Caesalpiniaceae, and used in the traditional system of medicine. The tribal people of Kolli Hills, Tamil Nadu, India, use the leaves of Caesalpinia bonducella and the stem bark of Bauhinia racemosa in combination with some other herbs for the treatment of various tumors, liver disorders, inflammation and some other diseases. In ancient Ayurveda medicine these plants were mentioned to possess antitumor agents. Since there are no scientific reports regarding the toxicological aspects of these plants, the present investigation deals with the sub-chronic toxicity studies of a methanol extract of Caesalpinia bonducella (MECB) leaves and Bauhinia racemosa (MEBR) stem bark in Swiss albino mice. The MECB and MEBR were administered intraperitoneally (i.p) to Swiss albino mice twice a week for thirteen weeks. No significant alterations in hematological, biochemical and histopathological parameters were observed in the MECB- and MEBR-treated groups at the doses of 100 and 200 mg/kg body weight. Administration of MECB and MEBR at the dose of 400 mg/kg body weight elevated the levels of serum enzymes and altered the hematological parameters. Our results suggested that MECB and MEBR at doses 100 and 200 mg/kg body weight did not induce any toxic effects in the mice. Adverse effect was noted at the dose of 400 mg/kg body weight.


Asunto(s)
Bauhinia , Caesalpinia , Pruebas Hematológicas , Extractos Vegetales/toxicidad , Animales , Recuento de Células Sanguíneas , Peso Corporal/efectos de los fármacos , Evaluación Preclínica de Medicamentos , Ingestión de Alimentos/efectos de los fármacos , Enzimas/sangre , Hematócrito , Riñón/efectos de los fármacos , Riñón/patología , Hígado/efectos de los fármacos , Hígado/enzimología , Hígado/patología , Masculino , Ratones , Tamaño de los Órganos/efectos de los fármacos , Corteza de la Planta/química , Extractos Vegetales/administración & dosificación , Hojas de la Planta/química
16.
J Enzyme Inhib Med Chem ; 19(2): 185-92, 2004 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-15449735

RESUMEN

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.


Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Compuestos de Rutenio/síntesis química , Compuestos de Rutenio/farmacología , Animales , Carcinoma de Ehrlich , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Bacterias Gramnegativas , Bacterias Grampositivas/efectos de los fármacos , Ratones
17.
Acta Pharmacol Sin ; 25(8): 1070-6, 2004 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-15301742

RESUMEN

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.


Asunto(s)
Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/uso terapéutico , Bauhinia/química , Carcinoma de Ehrlich/tratamiento farmacológico , Plantas Medicinales/química , Animales , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Carcinoma de Ehrlich/patología , Peroxidación de Lípido/efectos de los fármacos , Masculino , Ratones , Trasplante de Neoplasias , Corteza de la Planta/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico
18.
Chem Pharm Bull (Tokyo) ; 52(2): 178-85, 2004 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-14758001

RESUMEN

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.


Asunto(s)
Antibacterianos , Antineoplásicos , Compuestos Organometálicos , Rutenio , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antibacterianos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/uso terapéutico , Carcinoma de Ehrlich/tratamiento farmacológico , Supervivencia Celular/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Compuestos Organometálicos/síntesis química , Compuestos Organometálicos/química , Compuestos Organometálicos/uso terapéutico , Rutenio/química , Rutenio/farmacología , Rutenio/uso terapéutico , Relación Estructura-Actividad , Células Tumorales Cultivadas
19.
J Pharmacol Sci ; 94(2): 177-84, 2004 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-14978356

RESUMEN

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.


Asunto(s)
Antineoplásicos Fitogénicos/uso terapéutico , Antioxidantes/uso terapéutico , Caesalpinia , Carcinoma de Ehrlich/tratamiento farmacológico , Animales , Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Carcinoma de Ehrlich/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Peroxidación de Lípido/fisiología , Masculino , Ratones , Extractos Vegetales/uso terapéutico , Hojas de la Planta
20.
Acta Pol Pharm ; 60(3): 207-10, 2003.
Artículo en Inglés | MEDLINE | ID: mdl-14556490

RESUMEN

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.


Asunto(s)
Aminas Biogénicas/metabolismo , Química Encefálica/efectos de los fármacos , Corchorus/química , Cuscuta/química , Animales , Anticonvulsivantes/farmacología , Catecolaminas/metabolismo , Convulsivantes , Masculino , Ratones , Neurotransmisores/metabolismo , Extractos Vegetales/farmacología , Semillas/química , Convulsiones/inducido químicamente , Convulsiones/prevención & control , Serotonina/metabolismo , Estricnina
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