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Momordica charantia L. has been remained a well-known medicinal vegetable used traditionally. However, which part is most effective against which disorder, has been remained undiscovered yet. The objective of this study was to examine the antimicrobial, antihyperlipidemic and antihyperglycemic activities of peel, flesh, and seeds of bitter gourd, through in vitro and in vivo assays. Ethanolic extracts from powders of three fractions of bitter gourd were assessed for antimicrobial potential against bacterial and fungal strains, whereas, powders of these fractions were used to determine antihyperlipidemic and antihyperglycemic activity, in alloxan induced diabetic rats. Our results showed that BSE exhibited better antimicrobial activity against Bacillus cereus, whereas BFE exhibited better against Escherichia coli. Blood glucose was significantly lowered by all three powders in a dose dependent manner, when fed to diabetic rats, with the highest decrease by BSP, which reduced the glucose level from 296.20 ± 2.00 mg/dl to 123.10 ± 0.80 mg/dl, at 15 mg dose, after 28 days trial. Elevated levels of TC (101.18 ± 0.65 mg/dl), TG (83.69 ± 0.61 mg/dl) and LDL–C (25.90 ± 0.09 mg/dl) in positive control rats were lowered down in well manners by BSP at 15 mg dose, to 86.30 ± 0.53, 67.70 ± 0.53 and 19.32 ± 0.06 mg/dl, respectively. As compared to BFP and BPP, BSP showed significant involvement in antibacterial, antihyperglycemic, and antihyperlipidemic actions. Along with the edible flesh, peels and seeds, which are usually discarded as waste, could also be utilized for development of pharma foods capable of promoting health. [ABSTRACT FROM AUTHOR]

Objective: Biopharmaceutics Classification System says that simvastatin (SMV) is a Class II drug with low bioavailability (5%). This is because it dissolves slowly and is broken down a lot in the first pass. Simvastatin transdermal patches were produced as part of this study's aim to treat hyperlipidemia. The Box–Behnken design (three-factor, three-level) was selected for optimization of patches. Methodology: The optimization design involved 15 runs with independent factors hydroxypropyl methylcellulose K100, Eudragit L100, and polyethylene glycol 400 percentage, and dependent factors including folding endurance and in-vitro drug release. Results: The results showed that the concentration of hydroxypropyl methylcellulose K-100 positively impacted the patch's folding endurance. The fact that factor C was the only scenario where the p-value was less than 0.05 and the coefficient value was higher in the in vitro drug release model means that it has a greater influence on the release of medicines. The patches were also evaluated for drug content, swelling, moisture uptake, moisture content, etc. The optimized patch shows an in vitro drug release of 55.3% in up to 24 h. In vivo antihyperlipidemic activity was evaluated in albino Wistar rats. In the standard treatment (simvastatin oral) groups, there is a decrease in cholesterol (132.76 ± 0.35) and triglyceride level (139.80 ± 76) whereas in the test formulation group or test group, there is also a decrease in cholesterol (169.65 ± 0.21 mg/dL) and triglyceride level (151.20 ± 31 mg/dL) level. Conclusion: Based on in-vitro and in-vivo results it can be concluded that simvastatin patches can be an alternative to traditional therapy. [ABSTRACT FROM AUTHOR]

Stevia (Stevia rebaudiana Bertoni) is a natural zero calorie sweetener with significant economic and medicinal values due to its high contents of steviosides (SVGs) in the leaves. The aqueous extract of Stevia leaves (TAqE) was standardized to contain 8.5% w/w of SVGs (HPLC), total phenolics (164.63 ± 1.39 µg Gallic acid/mg extract) and total flavonoids of 100.5 ± 0.79 µg QE/mg extract. Twenty-one compounds were tentatively identified in the leaves via UPLC-Orbitrap HRMS and stevioside, rebaudioside A, and quercetrin were isolated from TAqE by repeated column chromatography. Stevioside showed significant inhibition of pancreatic lipase, α-amylase, and α-glucosidase enzymes. The effect of a standardized TAqE on high fat diet (HFD)-streptozotocin (STZ)-induced diabetic rats was investigated. Thirty-six animals were divided into 6 groups (each of 6). Rats in group I (control) and group II (control/HFD-STZ) received distilled water, and rats in groups III and IV received TAqE for 4 weeks in two doses; 300 mg/kg b.wt., and 500 mg/kg b.wt., respectively. Rats in group V received metformin (200 mg/kg), while those in group VI received statin (1 mg/kg). Body weight, fasting blood glucose, lipid profile (total cholesterol and triglycerides), liver enzymes (alanine transaminase and aspartic transaminase), and serum kidney parameters (urea and creatinine) were decreased in rats treated with TAqE (300 mg/kg b.wt.), while insulin sensitivity was enhanced, when compared to that in group II. These findings could justify the use of Stevia as a complementary medicine for the prevention and treatment of metabolic changes associated with diabetes mellitus type 2. [ABSTRACT FROM AUTHOR]

Background: Dyslipidemia is an aberrant rise in blood lipids due to diet and lifestyle. It has implicated as the major risk factor for developing hypertension among other diseases. This study was designed to evaluate plantain based dough meal nutritional property, antioxidant activity and dyslipidemia ameliorating potential in high-fat induced rats. Methods: The flour blends, i.e., PSC (Plantain 70%, Soycake 30%), PSR (Plantain 65%, Soycake 30%, Rice-bran 5%), PSO (Plantain 65%, Soycake 30%, Oat-bran 5%), PSRO (Plantain 60%, Soycake 30%, Rice-bran 5%, Oat-bran 5%) and controls (100% Plantain flour & Cerolina) were evaluated for chemical, antioxidants and antihyperlipidemia. Results: Protein, fiber and energy composition varied from 2.2–4.97 g/100 g, 16.44–19.59 g/100 g and 369.7–385.5 kcal/100 g, respectively. Essential amino acid index and predicted-biological values of the foods ranged from 68.31–76.31% and 62.19–71.48%, respectively. Phenolic profiles (mg/g) were gallic acid (25.33–31.26), caffeic acid (2.75–4.61), ferulic acid (5.16–12.73), luteolin (16.31–23.60), kaempferol (21.51–30.64), quercetin (24.28–37.13), chlorogenic acid (42.25–59.78), myricetin (28.41–38.41), 3,5-dicaffeoylquinic acid (27.17–41.59) and 4, 5-dicaffeoylquinic acid (39.96–51.28). The antioxidant activity of PSRO on ABTS, DPPH, FRAP, Fe2+ chelation and OH free radicals was higher than other foods. Atherogenic index, coronary risk index and log (TG/HDL-conc.) of rats fed on experimental foods were lower than recommended values. Conclusion: The study established that PSRO had higher antioxidant and anti-hyperlipidemia properties; hence, it may be suitable as a functional food. [ABSTRACT FROM AUTHOR]

Nicotinic acid hydrazide was incorporated into new 4,5-dihydro-5-hydroxy-3,5-diphenylpyrazol-1-yl derivatives. Compounds 6a–h were synthesized, and their antihyperlipidemic activity was evaluated in high cholesterol diet-fed rat model. Compounds 6e, 6f were found to decrease the levels of serum total cholesterol by 14–19% compared to control group. Total triglycerides were also reduced by 24–28% and LDL cholesterol by 16%. As expected from parent niacin, compounds 6e and 6f caused an elevation of HDL cholesterol by 33–41%. Docking study supported the ability of designed compounds to block NPC1L1 active site in a manner similar to that observed with ezetimibe. [ABSTRACT FROM AUTHOR]

Development of fixed dose combinations is growing and many of these drug combinations are being legally marketed. However, the development of these requires careful investigation of possible physicochemical changes during co-processing. This requires investigation of the effect of co-processing of drug combination in absence of excipients to maximize the chance of interaction (if any). Accordingly, the aim was to investigate the effect of co-processing of ezetimibe and atorvastatin on drugs dissolution rate. The objective was extended to in vitro in vivo correlation. Drugs were subjected to wet co-processing in presence of ethanol after being mixed at different ratios. The prepared formulations were characterized using FTIR spectroscopy, X-ray powder diffraction, differential scanning calorimetry, scanning electron microscopy, and in vitro dissolution testing. These investigations proved the possibility of eutectic system formation after drugs co-processing. This was reflected on drugs dissolution rate which was significantly enhanced at dose ratio and 2:1 atorvastatin:ezetimibe molar ratio compared to the corresponding pure drugs. In vivo antihyperlipidemic effects of the co-processed drugs were monitored in albino mice which were subjected to hyperlipidemia induction using poloxamer 407. The results showed significant enhancement in pharmacological activity as revealed from pronounced reduction in cholesterol level in mice administering the co-processed form of both drugs. Besides, histopathological examinations of the liver showed marked decrease in hepatic vacuolation. In conclusion, co-processing of atorvastatin with ezetimibe resulted in beneficial eutexia which hastened the dissolution rate and pharmacological effects of both drugs. Graphical abstract [ABSTRACT FROM AUTHOR]

Hyperlipidemia is one of the main contributing factors in the development of cardiovascular diseases. The hunt for effective antihyperlipidemic drugs is still on with an intention of finding potent agents with meager adverse effects. For the past several decades, medicinal plants have been evaluated for lipid-lowering effects apart from synthetic approaches to develop newer antihyperlipidemic agents. This article highlights the work carried out on potential antihyperlipidemic agents from plant sources from 2006 till 2012 that were archived in Google Scholar and Science Direct database. Seventy-nine articles were included in the review after manual content curation. The review summarizes the investigations on medicinal plants, compounds and herbal formulations using various hyperlipidemic animal models or in humans, the research findings and possibility of chemotaxonomic occurrence of secondary metabolites responsible for the antihyperlipidemic activities within certain plant families. [ABSTRACT FROM AUTHOR]

A series of novel condensed 2-fluoromethylpyrimidines has been synthesized and evaluated for antihyperlipidemic activity in high fat diet fed hyperlipidemic Sprague-Dawley rats. The aim of this study was to investigate the effect of the fluorine atom at the 2-methyl position of these compounds. Most of the synthesized compounds significantly affected the lipid profile of the test animals. Compound IIIb exhibited remarkably best effects in lowering the serum cholesterol and triglyceride levels and elevating the serum HDL levels, of the test animals. Graphical abstract: A series of novel condensed 2-fluoromethylpyrimidines was synthesized and evaluated for antihyperlipidemic activity in hyperlipidemic Spargue-Dawley rats. All compounds, especially IIIb, significantly affected the lipid profile of test animals.[Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

In the present study influence of nature of selected cyclodextrins (CDs) and of methods of preparation of drug-CD complexes on the oral bioavailability, in vitro dissolution studies and pharmacodynamic activity of a sparingly water soluble drug rosuvastatin (RVS) was investigated. Phase solubility studies were conducted to find the interaction of RVS with β-CD and its derivatives, which indicated the formation of 1:1 stoichiometric inclusion complex. The apparent stability constant (K) calculated from phase solubility diagram were in the rank order of β-CD < hydroxypropyl-β-cyclodextrin (HP-β-CD) < randomly methylated-β-cyclodextrin (RM-β-CD). Equimolar drug-CD solid complexes prepared by different methods were characterized by the Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). FTIR study demonstrated the presence of intermolecular hydrogen bonds and ordering of the molecule between RVS and CDs in inclusion complexes. DSC and XRD analysis confirmed formation of inclusion complex by freeze dried method with HP-β-CD and RM-β-CD. Aqueous solubility and dissolution studies indicated improved dissolution rates of prepared complexes in comparison with drug alone. Moreover, CD complexes demonstrated of significant improvement in reducing total cholesterol and triglycerides levels as compared to pure drug. However the in vivo results only partially agreed with those obtained from phase solubility studies. [ABSTRACT FROM AUTHOR]

The aim of present investigation was to study the effects of Mesembryanthemum forsskalei Hochst (Samh) seeds in streptozotocin-induced diabetic rats. Thirty rats were administrated with streptozotocin to induce diabetes and 6 rats were used as untreated diabetic control. Diabetic rats were fed with 5 and 15% Samh seed alone and in combination with fatty diet i.e. 2% Cholesterol for 6 weeks. Effects of Samh seed on blood glucose levels, lipid profiles and enzyme activities of diabetic rats were examined. In addition, total cholesterol (TC), triglyceride (TG) and high density lipoprotein-cholesterol (HDL-C) were determined. Diabetic rats treated with 15% Samh seed diet were significantly decreased the level of TC (40%), TG (46%) and HDL-C (31%) respectively. Whereas, there was no significant effects observed in the glucose level in 15% Samh seeds treated rats for 6 weeks. A decrease in enzymes levels, AST (58.2%), LDH (1.6%), ALT (24.3%) and ALP (5.38%) in 5% Samh seeds diet treated rats were observed and were found near to untreated control. Findings from present study demonstrated that non fatty Samh seeds diet could have hypoglycemic and antihyperlipidemic effects in diabetic rats and could be useful model for the treatment of diabetic patients. [ABSTRACT FROM AUTHOR]

Lagenaria siceraria (Molina) Standl in the Cucurbitaceae family is a large, pubescent, climbing, or trailing herb cultivated throughout India and the tropical regions of the world. Phytochemical investigation of the methanol extract obtained from the fruits of the plant L. siceraria showed a positive Liebermann-Burchard test for sterols. The white sterol crystals or phytosterols from the methanol extract were isolated for the first time and identified as a mixture of four sterols, including fucosterol ( 1), racemosol ( 2), stigmasterol ( 3), and stigmasta-7,22-dien-3β,4β-diol ( 4). These compounds were identified by spectroscopic evidence including FTIR, H-NMR, MS, and GC. The white sterol crystals, which are the mixture of four sterols, were evaluated for antihyperlipidemic activity in Wistar rats. The blood samples were collected from the retro-orbital plexus and serum was separated and analyzed for lipid profiles. These sterol crystals (30 mg/kg) showed significant reductions in lipid profiles which included cholesterol, triglycerides, LDL and VLDL. In addition, a significant increase in HDL cholesterol observed, which is a good cholesterol that protects hearts from coronary artery diseases. These sterol crystals or phytosterols can be used as an antihyperlipidemic agent to treat the hyperlipidemic. [ABSTRACT FROM AUTHOR]

The rising incidence of diabetes mellitus (DM) is alarming and becoming a major health problem worldwide, which is mainly associated with hyperglycemia, abnormal lipid, and antioxidant profiles. Herbal medicines are being used by about 80% of the world population primarily in the developing countries for primary health care, including DM. Based on these facts, in this study, the antihyperglycemic, antihyperlipidemic, and antioxidant properties of Chaenomeles sinensis fruits extract (CSFE) were investigated in streptozotocin (STZ)-induced (55 mg/kg body weight) diabetic rats. CSFE was found to be rich in total phenolics and flavonoid contents. The following assays were performed: fasting blood glucose, hemoglobin (Hb), blood urea nitrogen (BUN), serum total cholesterol (TC), serum triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), serum glutamic pyruvic transaminase/alanine aminotransferase (SGPT/ALT), serum glutamic oxaloacetic transaminase/aspartate aminotransaminase (SGOT/AST), liver glycogen content and superoxide dismutase (SOD), reduced glutathione (GSH), and catalase (CAT) contents in liver and kidney. Oral administration of CSFE (500 mg/kg body weight) significantly decreased fasting blood glucose, BUN, and serum TC, TG, LDL-C, SGPT/ALT, and SGOT/AST, while it increased blood Hb content and HDL-C in diabetic rats. Furthermore, CSFE treatment significantly increased liver glycogen content, SOD, GSH, and CAT levels in diabetic rats. The results showed that CSFE significantly inhibited the progression of diabetes induced by STZ, and the inhibitory effect of CSFE on diabetes might be associated with its hypoglycemic effect, modulation of lipid metabolism, and its ability to scavenge free radicals. [ABSTRACT FROM AUTHOR]

A simple ultraviolet spectrophotometric method for the determination of simvastatin in methanol has been devised and compared with the existing pharmacopoeial RP-HPLC method for the estimation of the drug. Analytical parameters such as stability, selectivity, accuracy, and precision have been established for the method, using SIMS® tablets and human serum samples, and evaluated statistically to assess the application of the method. The method was validated under ICH and USP guidelines and was found to comprise the advantages for simplicity, stability, sensitivity, reproducibility, and accuracy for use as an alternative to existing nonspectrophotometric methods for the routine determination of the drug in pharmaceutical formulations and for pharmaceutical investigations involving simvastatin. [ABSTRACT FROM AUTHOR]