RESUMO
AIM: To explore the potential of Rosellinia sanctae-cruciana an endophytic fungus associated with Albizia lebbeck for pharmaceutically important cytotoxic compounds. METHODS AND RESULTS: One novel cytochalasin, named jammosporin A (1) and four known analogues (2-5) were isolated from the culture of the endophytic fungus R. sanctae-cruciana, harboured from the leaves of the medicinal plant A. lebbeck. Their structures were elucidated by extensive spectroscopic analyses including one-dimensional and two-dimensional nuclear magnetic resonance data along with MS data and by comparison with literature reports. In preliminary screening the ethyl acetate extract of the fungal culture was tested for cytotoxic activity against a panel of four cancer cell lines (MOLT-4, A549, MIA PaCa-2 and MDA-MB-231), and found to be active against MOLT-4 with an IC50 value of 10 µg ml-1 . Owing to the remarkable cytotoxic activity of the extract the isolated compounds (1-5) were evaluated for their cytototoxicity against the MOLT-4 cell line by MTT assay. Interestingly, compounds 1-2, 4 and 5 showed considerable cytotoxic potential against the human leukaemia cancer cell line (MOLT-4) with IC50 values of 20·0, 10·0, 8·0 and 6·0 µmol l-1 , respectively, while compound 3 showed an IC50 value of 25 µmol l-1 . This is the first report of the existence of this class of secondary metabolites in R. sanctae-cruciana fungus. CONCLUSION: This study discovered a novel compound, named jammosporin A, isolated for the first time from R. sanctae-cruciana, an endophytic fungus of A. lebbeck with anticancer activity against the MOLT-4 cell line. SIGNIFICANCE AND IMPACT OF THE STUDY: Rosellinia sanctae-cruciana represents an interesting source of a new compound with bioactive potential as a therapeutic agent against a human leukaemia cancer cell line (MOLT-4).
Assuntos
Albizzia/microbiologia , Ascomicetos/química , Sobrevivência Celular/efeitos dos fármacos , Citocalasinas/isolamento & purificação , Citocalasinas/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/toxicidade , Linhagem Celular Tumoral , Citocalasinas/química , Citocalasinas/toxicidade , Humanos , Concentração Inibidora 50 , Folhas de Planta/microbiologia , Plantas Medicinais/microbiologiaRESUMO
The family Apocynaceae is one of the largest and important families in angiosperm. Several members of this family have medicinal properties and have been in the treatment of various ailments. Most of them are consumed as food by tribal people whereas a few plants are used as source of poison. Members of family Apocynaceae are rich in alkaloids, terpenoids, steroids, flavonoids, glycosides, simple phenols, lactones, and hydrocarbons. Other compounds such as sterols, lignans, sugars, lignans, and lactones have been isolated and systematically studied. Few studies have reported antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities of crude extracts as well as single compound(s) isolated from various members of the family Apocynaceae. Holarrhena antidysenterica, Rauvolfia serpentina, Carissa carandas, and Tabernaemontana divaricata are the extensively studied plants in this family. The present review provides a detailed outlook on ethnopharmacology, phytochemistry, and biological activities of selected members of this family. Moreover, it also covers the biotechnological advances used for large-scale production of bioactive compounds of therapeutic interest along with plant tissue culture-based approaches for conservation of this medicinally valuable family.
Assuntos
Apocynaceae/química , Etnofarmacologia , Fitoterapia , Extratos Vegetais , Animais , Anti-Infecciosos/farmacologia , Anti-Infecciosos/uso terapêutico , Antioxidantes/química , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Apocynaceae/classificação , Etnofarmacologia/métodos , Etnofarmacologia/tendências , Humanos , Fitoterapia/métodos , Fitoterapia/tendências , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
Industrial apple pomace, a biowaste generated during apple processing, is rich in cell wall polysaccharides and phenolics. These biologically active compounds are reported to be highly beneficial from the nutritional and health point of view. In the present study, the total phenolic content in the apple pomace aqueous extract (APE) was estimated and evaluated for its possible antioxidant and hepatoprotective efficacy in carbon tetrachloride (CCl4)-induced liver injury mice model. The aqueous extract exhibited 2,2-diphenyl-2-picrylhydrazyl free radical scavenging activity in vitro. Under in vivo study, mice were treated with APE (200 mg and 400 mg/kg body weight) for 2 weeks prior to the administration of CCl4 (30% v/v). The serum liver injury markers alanine transaminase, aspartate transaminase, and alkaline phosphatase were significantly lowered by APE in a dose-dependent manner. The levels of antioxidant parameters superoxide dismutase (SOD), reduced glutathione (redGSH), and lipid peroxidation were also improved by APE in liver homogenate. Histopathological studies revealed that APE treatment significantly lowered the CCl4-induced necrotic changes in the liver. Furthermore, terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end-labeling assay showed that CCl4-induced apoptosis in the liver was significantly inhibited by APE in a dose-dependent manner. Immunohistochemistry results showed higher expression of nuclear erythroid 2-related factor 2 (Nrf2) in the liver of the APE-treated mice, a key regulator of antioxidative response. In conclusion, the results of the present study revealed the hepatoprotective efficacy of APE by inhibiting CCl4-induced apoptosis, which is due to its antioxidant activity and the ability to induce Nrf2 protein expression.
Assuntos
Antioxidantes/uso terapêutico , Apoptose/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Frutas/química , Malus/química , Fator 2 Relacionado a NF-E2/metabolismo , Extratos Vegetais/uso terapêutico , Animais , Antioxidantes/administração & dosagem , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Relação Dose-Resposta a Droga , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Testes de Função Hepática , Masculino , Camundongos , Extratos Vegetais/administração & dosagemRESUMO
A five-week experiment was conducted to delineate stress-mitigating effects of three different methyl donors in Labeo rohita fingerlings subjected to endosulfan toxicity. Four iso-nitrogenous and iso-caloric feed were prepared with and without supplementation of methyl donors. The feed were basal or control diet (i.e., without methyl donor supplementation), feed supplemented with choline, feed supplemented with betaine and feed supplemented with lecithin. Two hundred and twenty-five fishes were distributed randomly in five treatment groups each with three replicates. The experimental setup were normal water (without endosulfan) and fed with control diet (control group), endosulfan-treated water and fed with control diet (T1), endosulfan-treated water and fed with choline supplemented feed (T2), endosulfan-treated water and fed with betaine supplemented feed (T3) and endosulfan-treated water and fed with lecithin-supplemented feed (T4). The level of endosulfan in endosulfan treated water was maintained at the level of 1/10 of LC50, that is, 0.2 ppb. During the experiment, growth performances, metabolic enzyme activity and histological examination were done to assess the effect of treatments. The growth performance (percentage weight gain, feed conversion ratio, specific growth rate and protein efficiency ratio) and nutrient digestibility were significantly different (P<0.01) in lecithin, betaine and choline fed group when compared to endosulfan-exposed group fed with basal diet. The liver LDH and MDH activity were significantly (P<0.01) improved in the groups fed with methyl donor supplemented diet. The liver AST and ALT, brain AChE and muscle ALT did not change with supplementation in the diet, but muscle ALT and G6PDH significantly (P<0.01) changed with supplementation. The gill and liver ATPase and intestinal ALP were significantly (P<0.01) noticeably changed in supplemented group. After endosulfan exposure, histopathology alter like slight large vacuolation in hepatocyte and lipoid vacuole were observed and with supplementation normal appearance of liver were observed. The chromosome aberration (karyotype) was observed in endosulfan-exposed group. The result obtained in present study concluded that inclusion of methyl donors, particularly lecithin and betaine, in feed as nutritional supplements has a potential stress-mitigating effect in L. rohita fingerlings.
Assuntos
Aquicultura , Cipriniformes/fisiologia , Suplementos Nutricionais , Endossulfano/toxicidade , Inseticidas/toxicidade , Estresse Fisiológico , Acetilcolinesterase/metabolismo , Adenosina Trifosfatases/metabolismo , Alanina Transaminase/metabolismo , Fosfatase Alcalina/metabolismo , Animais , Aspartato Aminotransferases/metabolismo , Betaína/administração & dosagem , Colina/administração & dosagem , Glucosefosfato Desidrogenase/metabolismo , Cariotipagem , L-Lactato Desidrogenase/metabolismo , Lecitinas/administração & dosagem , Lipotrópicos , Fígado/patologia , Malato Desidrogenase/metabolismo , TensoativosRESUMO
The effect of raw garlic on normal blood cholesterol level in males of the age group of 18-35 years was studied. The subjects, who never ingested garlic before, were given 10 g of garlic daily with their diet for two months. Fasting blood samples were investigated in respect of cholesterol before and after two months of garlic intake. Initially the blood cholesterol level ranged between 160-250 mg% which decreased significantly in all the subjects of experimental group after two months of ingestion of garlic. The slight decrease or increase in the blood cholesterol level of control group was not significant. The raw garlic can be advocated for daily ingestion in order to lower one's blood cholesterol level even if it is within normal limits.