Conventional solvent fractionation and bioactivity based target assays were used to identify a new anti-cancer molecule from Phyllanthus urinaria, a herbal medicinal plant used in South India. At each step of the purification process the different fractions that were isolated were tested for specific anti-proliferative activity by assays measuring the inhibition of [ 3 H]thymidine incorporation, and trypan blue drug exclusion. The ethyl acetate fraction that contained the bioactivity was further purified and resolved by HPLC on a preparative column. The purity of each of the fractions and their bioactivity were checked. Fraction 3 demonstrated a single spot on TLC and showed maximum anti-proliferative activity. This fraction was further purified and the structure was defined as 7'-hydroxy-3',4',5,9,9'-pentamethoxy-3,4-methylene dioxy lignan using NMR and mass spectrometry analysis. The pure compound and the crude ethyl acetate fraction which showed anti-proliferative activities were examined for ability to target specific markers of apoptosis like bcl2, c-myc and caspases and for effects on telomerase. Four specific cancer cell lines HEp2, EL-1 monocytes, HeLa and MCP7 were used in this study. The results indicate that 7'-hydroxy-3',4',5,9,9'-pentamethoxy-3,4-methylene dioxy lignan was capable of inhibiting telomerase activity and also could inhibit bcl2 and activate caspase 3 and caspase 8 whose significance in the induction of apoptosis is well known. We believe that this compound could serve as a valuable chemotherapeutic drug after further evaluations.
This study aimed to investigate the preventive role of Elateriospermum tapos seed extract against obese Sprague Dawley rats through assessment of bodyweight, caloric intake, organs weight, biological assays and histopathology. Thirty-six male Sprague Dawley rats were assigned into six groups of normal control (G1) group fed with standard chow diet, negative control (G2), positive control (G3) and treatment groups (G4, G5 and G6) were on high-fat and cafeteria diet for 9 weeks. G3 group was given 10 mg kg−1 of Orlistat while treatment groups were supplemented with E. tapos seed extract of 5 mg kg−1, 25 mg kg−1 and 125 mg kg−1 orally daily for another 10 weeks. Bodyweight and food intake were monitored weekly. At the end, liver, retroperitoneal white adipose tissue (rpWAT) and blood were collected for analysis of total cholesterol (TC), triglycerides (TG), low-density (LDL-C) and high density lipoprotein (HDL-C). The E. tapos seed treated groups showed significant (p < 0.05) reduction in bodyweight, caloric intake, liver and rpWAT weight as compared to the G2 group. G6 group showed tremendous improvement of liver histopathology and biological assay. There was a significant decrease (p < 0.05) of TC, TG, and LDL-C level and significant increase (p < 0.05) of HDL-C in the E. tapos seed treated group as compared to G2 group. Based on the findings, E. tapos seed extract exhibited a great potential as an anti-obesity. The extract promoted the fat oxidation by removing the uptake and storage of fat by the adipose cells and also decrease the fatty acid synthesis.
: Maternal obesity is a metabolic disorder described by chronic inflammation and an increase of stress hormones, influencing non-communicable diseases in offspring. Elateriospermum tapos has the potential as an antioxidant and inhibitor of lipids (pancreatic lipase) and carbohydrates (α-amylase and α-glucosidase) which are beneficial to combat obesity and diabetes. This study aimed to investigate the effect of E. tapos supplementation in obese rats prior to pregnancy on the dam and male offspring body weight and the level of stress hormones—adrenocorticotropic hormone (ACTH) and corticosterone (CORT). Thirty female Sprague Dawley rats were used in this study. Six rats were assigned to a normal diet (DND) group fed with a standard chow diet. The remaining rats were fed with a high-fat and cafeteria diet (HFCD) to generate obesity for five weeks. The obese rats were further divided into four groups (n = 6/group); dams negative control group (DNC, normal saline), dams positive control group (DPC, 200 mg/kg body weight of orlistat), dams treatment 1 group (DTX1, 200 mg/kg BW of E. tapos seed) and dams treatment 2 group (DTX2, 200 mg/kg BW of E. tapos shell). The treatment was given for six weeks daily before mating. At weaning, male offspring were designated into six groups according to their dam’s group (n = 6/group) and continued with the cafeteria diet except for the control group. The offspring were culled at 12 weeks of age for blood sample collections. DTX2 and their male adult offspring showed significantly lower body weight compared to DNC and their male offspring. Male offspring from DTX2 also showed significantly low ACTH and CORT levels compared to male offspring from the DNC group and a comparable level with the DND group. E. tapos shell supplementation was effective in reducing the development of obesity and suppressed stress through the regulation of ACTH and CORT release in male adult offspring.
Obesity is one of the risk factors associated with cardiovascular diseases, hypertension, abnormal liver function, diabetes, and cancers. Orlistat is currently available to treat obesity, but it is associated with adverse side effects. Natural resources are widely used for obesity treatment. Hence, this study aimed to investigate the anti-obesity activity of Elateriospermum tapos (E. tapos) shell extract in obesity induced Sprague Dawley rats. The rats’ obesity was induced by a high-fat (HF) diet made up of 50% standard rat pellet, 20% milk powder, 6% corn starch, and 24% ghee and a cafeteria (CAF) diet such as chicken rolls, salty biscuits, cakes, and cheese snacks. A hot aqueous method for the extraction of E. tapos shells was applied by using 500 mL of distilled water for about 24 h. Various dosages of E. tapos shell extract (10 mg/kg, 100 mg/kg, and 200 mg/kg) were used. At the end of the study, body weight, caloric intake, organ weight, lipid profile, lipoprotein lipase (LPL) activity, and histopathology analysis were carried out. E. tapos shell extract treated groups showed a reduction in body weight, positive lipid-lowering effect, decrements in triglyceride accumulation and LPL activity, and positive improvement in histopathology analysis. A dose of 200 mg/kg showed the most effective result compared to 10 mg/kg and 100 mg/kg doses.
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