1. Evaluation of pharmacological activities of Rivea hypocrateriformis in experimental animal models S. Godipurge, S. Rahber, J. S. Biradar, N. Mahurkar
The present study aimed to investigate the potential pharmacological activities of the ethanolic extract of aerial parts of Rivea hypocrateriformis (EERH) and also their phenolic and flavonoid contents measured. The use of this plant in traditional medicine prompted us to study the antioxidant activity by using in vitro assay of total antioxidant assay, 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging assay and reducing power assay. In DPPH assay, the IC50 values of EERH, ascorbic acid and Butylated hydroxyanisole (BHA) were 43.23, 46.70 and 46.61µg/mL respectively. Reducing power of the extracts increased by increasing their concentration. The analgesic activity employed by hot plate and tail flick methods and in vitro and in vivo methods of anti-inflammatory activity by human red blood cell membrane stabilization (HRBC) and carrageenan induced paw edema were screened. Percentage protection of inhibited by 250 µg/mL concentration was more and corresponds to standard diclofenac sodium. In EERH in doses of 200 and 400 mg/kg of body weight showed 28.57% and 71.42% inhibition of paw edema, respectively at the end of the 4 hours compared to that of standard diclofenac sodium (85.71%). In hot plate and tail flick methods, the ethanolic extract at high dose 400 mg/kg of body weight increased the pain threshold significantly (P < 0.001) after 4 hours of administration and the effect was retained for 6 hours. The EERH shows the dose dependent effect in all the experimental simulations. The results of this study provide pharmacological application of the Rivea hypocrateriformis in pain and inflammatory disorders.
2. In vitro α-amylase and α-glucosidase enzymes inhibitory effects of the aqueous extract of Combretum molle twigs Miaffo D, Wansi S.L, Kamani Poualeu S.L, Fofié Kueté C, Kamanyi A
The present study is carried out to evaluate the in vitro α-amylase and α-glucosidase enzymes inhibition studies together with in vivo studies to confirm the activity of Combretum molle twigs extract to control postprandial blood glucose level in starch and sucrose loaded normal rats. The inhibitory effect of the extract on α-amylase and α-glucosidase was determined in vitro studies. In in vivo studies, oral tolerance tests were done by inducing hyperglycemic state via administration of starch (4g/kg) and sucrose (3 g/kg). Thereafter, hyperglycemic rats groups received 0, 125, 250 and 500 mg/kg of the extract. The glycemia was evaluated at 0, 30, 60, 90 and 120 minutes after the administration of carbohydrates. In vitro studies had indicated dose-dependent inhibitory activity of the extract against α-amylase and α-glucosidase with the IC50 values of 31.25 ± 5.95 and 50.60 ± 2.81 µg/mL, respectively. In in vivo studies, the extract alone was administered to starch and sucrose loaded normal fasting rats which produced a significant decrease in AUC and in postprandial glycemia at 90 and 120 minutes at 500 mg/kg. However, at 250 mg/kg, the extract induced a significant decrease in AUC and in blood glucose concentration at 60 and 120 minute after carbohydrates loading. The current study demonstrates one of the mechanisms in which C. molle twigs extract effectively inhibits α-amylase and α-glucosidase leading to suppression of postprandial hyperglycemia in rats loaded with starch and sucrose. The extract seems to be promising in the treatment of type-2 diabetes mellitus by reducing postprandial hyperglycaemia.
3. Evaluation of Mutagenic Effect (Antimutagenic) of Dalbergia latifolia on Swiss Albino Mice Nagarathna P K M, Chandrajeet kumar yadav, Saroj kumar yadav
The present study was designed to evaluate the anti-mutagenic potential of Methanolic extract of Dalbergia latifolia, using micronucleus (MN) and chromosomal aberration (CA) assay in mice bone marrow. The anti-mutagenic effect of Dalbergia latifolia was assessed using cyclophosphamide MN formation and CA in mice. The animals were pre-treated with the Methanolic extract of Dalbergia latifolia orally at two doses of 100, 200mg/kg body weight for seven days. In MN and CA test the two doses provided protection when given 24hrs prior to a single i.p administration of cyclophosphamide (100 mg/kg body weight). These results demonstrate that Methanolic extract of Dalbergia latifolia has got anti-mutagenic potential.
4. Impact of Genetic Polymorphisms of MDR1 Gene in the Chemotherapeutic Treatment of Cervical Cancer: A Case Control Study P.Jytothirmaye, Raju lingumpelly
Polymorphisms in genes coding for metabolising enzymes can affect drug efficacy and toxicity. The cervical cancer is the leading cause of death from gynecological malignancy, and the second most commonly diagnosed gynecologic malignancy Aim and objective: The present study will be undertaken with an objective to evaluate the clinical significance of polymorphisms in drug-metabolising enzymes in cervical cancer patients.Materials and methods: Genomic DNA isolation: Genomic DNA isolation will done for control blood samples and homogenised tumor samples by salting out method followed by ethonol extraction. Agarose gel elctrophorosis: presence of DNA well cheked by using 0.8% agarose gel electrophorosis. Polymarase chaine reaction(PCR): PCR amplification will be done by using specific set of primers and PCR condition followed by agarose gel electrophoresis to conform the amplified product, Single strand conformatory polymorphisms: SSCP of the PCR product will done for detecting the presence of polymorhisms in the amplifide exons from cancer samples compared to helthy samples, Sequenceing: Sequence analysis will done for the strands which showing shifts in SSCP Results: Detection of single nucliotide polymorphisms in Cervical cancer patients lead to safer chemotherapetic procedures for their treatment, and play role in Disease prognosis, relative risk individually in developing cervical cancer. Conclusion: Hence this study form the basis of an effort to reduece the trama and suffering of the cervical cancer patient.
5. Dyslipidemia in the Elevated Cadmium Exposure Population Surapon Tangvarasittichai, Sukumarn Niyomtam, Patchanrin Pingmuangkaew, Prapa Nunthawarasilp
Excessive cadmium (Cd) exposure has been reported to cause alter and disorder lipid metabolism and lipid compounds in tissue and circulation. Cd-induced renal toxicity is caused from increased oxidative stress production at the cellular level and induced cell apoptosis. We examined the association of elevated Cd exposure with dyslipidemia, oxidative stress and chronic kidney disease (CKD) in 258 residents of the Cd exposure area. Elevated Cd exposure was significantly correlated with triglycerides/high-density lipoprotein-cholesterol (TG/HDL-C) ratio, malondialdehyde (MDA), N-acetyl-β-D-glucosaminidase (NAG) and negatively correlated with total antioxidants capacity (TAC) and estimated glomerular filtration rate (eGFR). Elevated Cd exposure may cause hypertriglyceridemia, low high-density lipoprotein-cholesterol (HDL-C), high TG to HDL-C ratio, oxidative stress and CKD. Our study demonstrated that excessive Cd exposure associated with hypertriglyceridemia, reduced HDL-C, elevated TG/HDL-C ratio, oxidative stress and CKD in residents of Cd contaminated area.
6. Screening of In-vivo Anti-proliferative Activity of Limonia Acidissima Against MCF-7 Cell Line Tripathy Gitanjali, Pradhan Debasish
The aim of the study is to evaluate the anti-proliferative activity of Limonia acidissima. Anti-proliferative activity of methanolic extracts (200 and 400 mg/kg) of Limonia acidissima roots were evaluated against MCF-7 cell line in rats. Acute and short-term toxicity studies were performed initially in order to ascertain the safety of methanol extract of Limonia acidissima (MELA). After 24 h of tumor inoculation, the extract was administered daily for 14 days. After administration of the last dose followed by 18 h fasting, mice were then sacrificed for observation of anti proliferative activity. The effect of MELA on the growth of transplantable murine tumor, life span of MCF-7 bearing hosts and simultaneous alterations in the hematological profile were estimated. The MELA 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 MCF-7 tumor bearing mice. Hematological profile reverted to more or less normal levels in extract treated mice. The methanolic extract of Limonia acidissima fruit pulp exhibited anti-proliferative activity in MCF-7 tumor bearing rat.
7. Canagliflozin: A First-in-class Medication for the Treatment of Type 2 Diabetes Mellitus Dylan Hosein, Akram Ahmad, Muhammad Umair Khan, Sameer Dhingra
Diabetes mellitus (DM) is a group of metabolic disorders characterized by hyperglycemia and abnormalities in carbohydrate, fat, and protein metabolism. It results from defects in insulin secretion, insulin sensitivity, or both. Chronic microvascular, macrovascular, and neuropathic complications may ensue.Despite the large amount of treatment options available, Diabetes Mellitus is not well managed. Canagliflozin, a recently approved first-in-class anti-diabetic medication, employs a novel mechanism of action which is not dependent upon insulin release or improving insulin sensitivity. It is a sodium glucose co-transporter 2 (SGLT-2) inhibitor, developed to treat hyperglycemia in Type 2 Diabetes Mellitus patients. This causes more glucose to be removed from the urine, thereby lowering blood sugar levels. Canagliflozin was reported to improve glycemic control, reduce body weight and systolic BP, and was generally well tolerated in older subjects with T2DM who were on background therapy with a variety of blood glucose-lowering agents.
8. Cytotoxic Action of Flavonoids in Human Burkitt`s Lymphoma Cell Lines and its Antiandrogenic Modulation Sak K., Lust H., Everaus H.
In the past decades, studies of anticancer agents from natural sources have attracted a great attention whereas flavonoids are considered as interesting lead compounds. Differently from various leukemia cells, the knowledge about the cytotoxic action of these plant secondary metabolites in lymphoma cells is much scarcer. Therefore, the antiproliferative activity of structurally different flavonoids (baicalein, luteolin, chrysin, quercetin, fisetin, hesperetin) was described in two human Burkitt`s lymphoma lines, Daudi and Namalwa, showing baicalein as the most potent agent among the tested compounds (IC50 values of 6.97 μM and 23.71 μM, respectively). Other flavonoids revealed cytotoxic effects in higher concentration range whereas hesperetin displayed no activity even at 100 μM. In Daudi, but not in Namalwa cells, the antiproliferative action of baicalein and luteolin was partially suppressed by coincubation with 1 μM antiandrogen hydroxyflutamide showing that androgen receptor-related signaling pathways might be involved in the cytotoxicity of these flavones. Androgen receptors are indeed expressed in Daudi, but not in Namalwa cells. However, at higher micromolar doses, hydroxyflutamide itself induced the growth inhibitory effects in both cell lines. Therefore, as flavonoids offer novel potential leads for antilymphoma therapy, the possible involvement of gender-specific mechanisms in their cytotoxic action certainly needs further investigation.
9. Acute and Subchronic Toxicity Of Gmelina arborea Roxb, (Verbenaceae) in Wistar Rat Osseni R, Awede B⃰⃰, Adjagba M, Kpadonou C, Fall M, Laleye A, Darboux R
Gmelina arborea is a plant used in the traditional treatment of many diseases. However, only few pharmaco-toxicological studies are available on this plant. The aim of this study is to investigate the acute and subchronic toxicity of the aqueous extract of Gmelina arborea leaves. Materials and Method: acute and subchronic toxicity study has been performed in wistar rats using an aqueous extract of Gmelina arborea leaves. In the acute toxicity test, a single dose of 2000 mg/kg of body weight was administered to rats and they were observed during 14 days. The subchronic toxicity study was carried out using three doses of 31.25 mg/kg, 125 mg/kg and 500 mg/kg of body weight, administrated to rats (5 male and 5 female) for 28-days. Physiological behaviour, diet consumption, and body weight were evaluated. Biochemical, haematological and histological studies were realized at the end of the study. Results: There was neither mortality, nor physiological behaviour changes. The body weight and diet consumption of the rats were not modified. As for blood parameters, a dose dependent increase in Cholesterol and transaminases levels and decrease in blood glucose were observed. There was also an increased level of creatinine in male rats and urea in female rats. Histology of the treated rats’ liver shows in the centrolobular area lipid inclusions in hepatocytes almost at 500 mg/kg. In kidneys, a thickening of the glomerular interstitium was observed. Conclusion: These results show that the aqueous extract of Gmelina arborea is probably hepato- and nephro-toxic.