Non-​mutagenic and in vitro toxicity evaluation of embelin on human peripheral blood lymphocytes and mouse macrophages

The development of novel drugs that have chemotherapeutic activity against cancer is a great challenge. The discoveries of these drugs are very difficult, because they must be able to destroy the tumor cells without causing adverse side effects. Significant innovations come forth when human cell lines are used for vetting drugs and other chems. Embelin, a benzoquinone is reported to possess anticancer activity on various cancer cell lines. The present investigation was undertaken to det. the toxicity profile of embelin on human peripheral blood lymphocytes and murine macrophages. The effect of embelin on growth and viability of cells was detd. by MTT assay. Further embelin was tested for mutagenicity by the Ames test, in Salmonella typhimurium strains with and without metabolic activation. Results implicate that embelin was non mutagenic in the tester strains used in the study and did not adversely influence the proliferation of lymphocytes and macrophages and the IC50 was found to be 78.7μg​/mL and 128.54μg​/mL resp

Preventive Effects of Resveratrol against Beta Adrenergic Catecholamine-Induced Acute Myocardial Stress during Experimental Hyperglycemia in in Vivo and in Vitro Models

Aim: To evaluate the cardioprotective effects of resveratrol during hyperglycemic conditions in in vitro and in vivo models. Study Design: H9c2 cardiomyocyte cells were used as in vitro models and adult male Wistar strain albino rats were used as in vivo models. Activities of LDH and levels of lipid peroxides, total reduced glutathione were the end point indicators for the in vitro studies.For the in vivo studies the activities of membrane bound ATPases, levels of lipid peroxides, enzymic and non enzymic antioxidants were the end point indicators. Place and Duration of Study: The study was conducted at the Department of Microbiology and Biotechnology, Bangalore University, Bangalore, between January 2014 and June 2014. Methodology: To mimic myocardial injury during diabetic conditions (in vitro), the H9c2 cells were maintained in high glucose environment followed by isoproterenol challenge. For in vivo studies the animals were segregated as follows: Untreated control; Myocardial stress induced animals (Isoproterenol 150 mg/kg body wt i.p); Diabetic rats (Streptozotocin, 50 mg/kg body wt,i.p);Myocardial stress induced diabetic rats; resveratrol per se (5 mg/kg.body wt. orally for 21 days), and resveratrol pretreated prior to induction of diabetes and myocardial stress. Results: H9c2 cells given glucose insult and challenged with isoproterenol showed severe cytotoxicity and stress as elicited by increased LDH release, increased lipid peroxides and depleted GSH levels. These changes were prevented in the cells pretreated with resveratrol prior to isoproterenol/glucose challenge. The diabetic rats induced with myocardial stress showed significant alterations in the activity of membrane bound phosphatases, levels of lipid peroxides, enzymic and non enzymic antioxidants. Pre-treatment with resveratrol prevented these alterations thereby implicating cardioprotective effects during hyperglycemic conditions Conclusion: Resveratrol could combat myocardial stress during experimental hyperglycemia in in vitro and in vivo model

Effect of Small Molecule Inhibitor Fisetin over Proliferation of Human Non-Small Cell Pulmonary Carcinoma

The percentage of cancer-related deaths attributable to diet and tobacco globally is reported to be as high as 60-70%. A large number of dietary compounds have gained research interest and tested to determine their chemopreventive / antiproliferative effects on in-vivo/in-vitro models. The present study effect of flavonoid fisetin on proliferation of human lung carcinoma cells A549 and NCI-H460 was investigated. The effect of fisetin on cell growth was investigated by MTT, Crystal violet, XTT, LDH release, and colony forming assays. Cell proliferation was assessed by BrdU incorporation test. Further, cell morphology and cytopathology was analyzed by crystal violet test and hematoxylin and eosin staining. Results of study revealed that fisetin treatment exerted a dose dependent decrease in the growth of A549 and NCI-H460 cells with IC50 values of 190µM and 210µM respectively. It also inhibited cell proliferation and colony formation in both A549 and NCI-H460 cells. Cytopathology studies exhibited features such as nuclear fragmentation, cytoplasmic vacuolation, karyorrhexis, chromatin condensation, which were suggestive of apoptotic cell death. Results of the study indicate growth inhibitory, anti-proliferative and pro-apoptotic effects of fisetin on lung carcinoma cells

Pro-Stimulatory Effects of Tinospora Cordifolia (Menispermaceae) on SAOS-2 Osteoblast Cells-Implications on Bone Remodeling and Therapy of Osteoporosis

Osteoblasts, the bone forming cells are currently the most studied target for developing therapeutics to treat bone loss associated with various skeletal disorders including osteoporosis. Tinospora cordifolia (TC) is used in Ayurveda and other traditional medicinal systems to treat bone fractures. The aim of the present investigation is to evaluate the effects of aqueous and alcoholic extracts of TC on osteogenesis using a widely employed in vitro model system for human osteoblasts (human osteoblast like cells SAOS-2), thereby to explore the possibility of its usefulness to stimulate bone formation in osteoporotic conditions. Tests for cell viability and proliferation (crystal violet test, trypan blue dye exclusion test, MTT assay and NBT reduction test) were performed to study the effect of TC on the growth of osteoblasts. It was observed that ethanolic extract of TC stimulated proliferation of osteoblasts at a dosage of 25ìg/ml (P<0.001) but, the aqueous extract of TC showed no influence on cell proliferation. The effect of alcoholic extract of TC on bone resorption was also studied on functional osteoclasts derived from RANKL activated murine macrophage like cells RAW 264.7. Results of the study implicated that ethanolic extract of TC extract elicits pro-stimulatory effects on osteoblasts, but is devoid of any such effects on osteoclast cells thereby indicating that it has no effect on bone resorptio

Growth inhibitory and proapoptotic effects of l-asparaginase from Fusarium culmorum ASP-87 on human leukemia cells (Jurkat)

The objective of this study was to evaluate the anticancer properties of l-asparaginase purified from fungal isolate Fusarium culmorum ASP-87 against human T-cell leukemia cell line (Jurkat). The growth inhibitory and proapoptotic effects of purified l-asparaginase on Jurkat cell lines were investigated by determining its influence on cell viability, colony formation, DNA fragmentation, and cell cycle progression. The results revealed that purified l-asparaginase showed significant decrease in cell survival with IC50 value of 90 μg/mL (9 IU/mL). The enzyme inhibited colony formation and showed characteristic laddering pattern on agarose gel thereby confirming the induction of apoptosis. Further, cell cycle analysis revealed that the enzyme induced apoptotic cell death by arresting the growth of cells at G2-M phase. However, the enzyme did not elicit any toxic effects on human erythrocytes. l-asparaginase purified from F. culmorum ASP-87 showed significant and selective cytotoxic and apoptotic effects on human T-cell leukemic cells in dose-dependent manner. Results of the study give leads for the anticancer effects of fungal l-asparaginase and its potential usefulness in the chemotherapy of leukemia. © 2016 Société Française de Pharmacologie et de Thérapeutiqu

Protective Effects of Embelin and Curcumin Against Diethylnitrosamine / Phenobarbital Induced Experimental Hepatocarcinogenesis in Rats

The effects of administration of Curcumin and Embelin on the levels of certain trace elements and other elements of clinical significance, during experimental hepatocarcinogenesis induced by Diethylnitrosamine/ Phenobarbital (DENA/PB) was studied in Wistar strain male albino rats. The levels of calcium, potassium and sodium were determined in the serum of control and experimental groups of rats. Additionally, the levels of chromium, copper, magnesium, molybdenum and zinc were also determined in the serum, liver and kidney of these rats. Furthermore, lactate dehydrogenase (LDH) activity was also assayed in the serum of these rats. Results revealed both significant and non-significant alterations in the levels of few elements during DENA/PB-induced experimental hepatocarcinogenesis. A statistically significant increase in LDH activity was found in the serum during the cancerous condition. Pre- and co-treatment with Curcumin and Embelin was found to protect the liver against the carcinogenic effects of DENA/PB. This protection was i) due to their ability to prevent changes in the levels of elements studied and ii) by the statistically significant decrease in the activity of LDH that increased in DENA/PBtreated rats and LDH activity in the rats given only Embelin and Curcumin indicating their nontoxic effect. Our present results demonstrate the ability of Embelin and Curcumin to protect against DENA/PB-induced hepatocarcinogenesis in rats

Biochemical studies on the effect of curcumin and embelin during N-nitrosodiethylamine/phenobarbital induced-hepatocarcinogenesis in wistar rats

The biochemical effects of administration of embelin a benzoquinone derivative from Embelia ribes and curcumin (diferuloyl methane) isolated from Curcuma longa against a 2 step hepatocarcinogenic regimen comprising of N-nitrosodiethylamine (DENA)/phenobarbital (PB) was studied in wistar strain male albino rats with respect to lipid profile, renal function tests and levels of blood glucose. Rats administered DENA/PB showed hyper cholesterolaemia, hyper triglyceridaemia, elevated low-density lipoproteins (LDL), free fatty acids (FFA), very-low-density lipoproteins (VLDL) levels and decreased urea levels. Pre- and co-treatment with embelin and curcumin for 14 weeks significantly prevented the biochemical alterations induced by DENA/PB. Results of our study suggest the protective and hypolipidemic effects of embelin and curcumin during chemically- induced hepatocarcinogenesis in wistar rats. © 2009 Academic Journals

Biochemical studies on the effect of curcumin and embelin during N-nitrosodiethylamine/phenobarbital induced-hepatocarcinogenesis in wistar rats

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Purification of Lovastatin from Aspergillus terreus (KM017963) and evaluation of its anticancer and antioxidant properties

Cervical cancer is the second most common malignancy in women worldwide and thus one of the leading causes of mortality in women. Lovastatin, a non polar, anticholesterol drug has previously been reported to exert antitumour activity in vitro. In the present study, lovastatin from Aspergillus terreus (KM017963) was purified by adsoprtion chromatography and evaluated for its anticancer and anti-oxidant properties with a human cervical cancer cell line (HeLa). Growth inhibitory and proapoptotic effects of purified lovastatin on HeLa cells were investigated by determining its influence on cell numbers, mitochondrial membrane potential (MMP), DNA fragmentation and antioxidant properties in terms of hydroxy radical scavenging effects as well as levels of total reduced glutathione. Cell cycle analysis by flow cytometry (propidium iodide staining) confirmed induction of apoptotic cell death and revealed cell cycle arrest in the G0/G1 phase. Results of the study give leads for the anticancer effects of lovastatin and its potential usefulness in the chemotherapy of cervical cance

Different methods for standardization of fishing efforts

Surplus production models are widely employed to evaluate the condition of fish stocks, encompassing the entire stock, overall fishing effort, and the total yield derived from the stock. These models operate under the assumption that variations in population biomass result from hikes due to growth and reproduction, as well as drops due to natural and fishing mortality. Utilizing Catch-Per-Unit-Effort (CPUE) as input, these models rely on the presumption that CPUE is directly proportional to the biomass of fish stock in the sea. An inherent challenge in fitting such a production model lies in determining CPUE, whether in terms of units operated or in hours of operation/actual fishing hours (AFH) or in any measure of fishing efforts. Given the heterogeneous nature of fishing fleets in tropical regions, they are often categorized into boat-gear categories, where fishing units within each category share similar characteristics and performance. When assessing the collective impact of the fishing operations of the entire fleet on the exploitation of fish stock, nominal addition of the efforts of different boat-gear categories may lack meaningfulness without prior effort adjustment to enhance comparability. In tropical regions, due to the varying capacities of gears and the potential presence of multiple species in each gear, the effort expended to catch a resource cannot be simply considered as the sum of the duration/units of operation of all gears. This paper aims to underscore various effort standardization methodologies found in the literature for different situations, offering insights into the challenges faced in tropical fisheries and proposing a way forward