STUDY OF ANTIOBESITY ACTIVITY OF POLYHERBAL FORMULATION IN CORRELATION WITH ANTIDIABETIC ACTIVITY

Objective: The objective of this research was to develop a polyherbal formulation using four different herbs using obese diabetic rat's model. Methods: Rats received high-fat diet and alloxan was injected intraperitoneal to rats for induction of diabetes. In the preventive experiment, diabetic rats received Momordica charantia Linn. (200 and 400 mg/kg/day p.o), Eugenia jambolana Linn. (200 and 400 mg/kg/day p.o), Ziziphus mauritiana (200 and 400 mg/kg/day p.o), Acacia catechu (AC) (200 and 400 mg/kg/day p.o), and aqueous extract of all extracts (100 and 200 mg/kg/day p.o). Diabetic rats were also treated with glibenclamide (5 mg/kg p.o.) and orlistat (60 mg/kg/day p.o.) as reference standards. Results: The results showed that the extract of M. charantia Linn., E. jambolana Linn., Z. mauritiana, and AC significantly (p<0.05) inhibited body weight gain, blood glucose, triglyceride, total cholesterol, low-density lipoprotein (LDL), very LDL, high-density lipoprotein cholesterol, serum glutamic pyruvic transaminase, serum glutamic oxaloacetic transaminase, and fasting blood glucose in a dose-dependent manner. Extracts treated rats at doses of 200 and 400 mg/kg improved dyslipidemia in high-fat diet (HFD)-induced obese rats by enhancing their lipid metabolism when compared to the HFD control. Conclusion: The results obtained in this research work clearly showed that taken together the extract of M. charantia Linn., E. jambolana Linn., Z. mauritiana Lam. AC Willd., and aqueous extract of all extracts has potential as a preventive agent for type 2 diabetes mellitus (and possibly obesity) and deserves clinical trial in the near future

DEVELOPMENT OF POLYHERBAL WITH ANTIOXIDANT ACTIVITY

Objective: The objective of this research was to develop a polyherbal formulation (PHF) using four different herbs and to evaluate their phytochemicals, physical constants, and determination of their antioxidant activity by DPPH method.Methods: The PHF authenticated herbs were characterized by studying its morphological and pharmacognostic characters. Phytochemical screening showed the presence of alkaloids, glycosides, carbohydrates, amino acid, tannin, steroids, and flavonoids in the combination extract. Physical parameters such as loss on drying (LOD), pH, ash values, LOD, and extractive value have been studied. The antioxidant activity of the combination of extract (100 mg each) was determined using DPPH free radical scavenging method.Results: The results showed that the combination extract has best antioxidant effect at a dose of 400 μg/ml when it was compared with ascorbic acid as the reference standard.Conclusion: The results obtained in this research work clearly showed that the combination extract has best antioxidant effect at a dose of 400 μg/ ml when it was compared with ascorbic acid as the reference standard.Â

In Vitro and In Vivo Study of Poly(ethylene glycol) Conjugated Ibuprofen to Extend the Duration of Action

Ibuprofen–polyethylene glycol (PEG) conjugates (PEG-Ibu) were prepared and their potential as a prolonged release system was investigated. Two PEG-Ibu conjugates were synthesized from Ibuprofen and PEG with two different molecular weights by esterification in the presence of DCC and DMAP. The PEG-Ibu conjugates were characterized by FT-IR, 1H NMR, Mass spectroscopy and DSC analysis. The solubility study in aqueous system showed an increase in solubility of conjugates. The dissolution / hydrolysis studies showed a specific acid–base catalysis pattern dependent on the pH of the medium. This indicated a good chemical stability in aqueous buffer solution of acidic medium and the extended release behavior was found in both prodrugs after 9 hour. The results demonstrate that, in the same condition, the rate of hydrolysis for PEG4000-Ibu is slower than other. The Writhing induced by acetic acid experiment and paw edema test after oral administration showed that both conjugates had extended analgesic and anti-inflammatory effects compared with Ibuprofen. These results suggest that PEG-Ibu could be a promising NSAID prodrug with an extended pharmacological effect owing to delayed-release of parent drug

IN VITRO-IN VIVO CORRELATIONSHIP APPROACH OF THE PREPARED MAGNETIC MICROSPHERES OF CYTARABINE

Objective: The objective of this study was to study the in vitro-in vivo correlationship between the magnetic microspheres prepared by continuous solvent evaporation (CSE) method by 32 factorial designs. Methods: CSE technique was used in the preparation of magnetic microspheres. Drug used was cytarabine and mice were the animal model used to check the correlationship. Results: The profiles are nearly identical and reveal that drug absorption is rapid. The in vivo drug absorbed was found to be in concordance with the in vitro release as seen in the superimposable curves. Conclusion: Cytarabine effectively reduces the amount of drug released and consequently absorbed in vivo in the initial phase

ANTIDIABETIC AND ANTIHYPERLIPIDEMIC EFFECTS OF METHANOLIC EXTRACT OF CITRULLUS LANATUS SEEDS IN RATS

Objective: Aim of the present study is to evaluate the antidiabetic and antihyperlipidemic effect of methanolic extract of Citrullus lanatus seeds (MECL) in streptozotocin (STZ) induced diabetic rats.Methods: Diabetes was induced by a single dose of STZ (65 mg/kg) in citrate buffer, while the normal control group was given the vehicle only. After three days of induction of diabetes, the diabetic animals were treated further four weeks with MECL (200, 400 and 600 mg/kg) and glibenclamide (4 mg/kg). Blood glucose level was estimated every week of the study starting from d 1. At the end of study period, biochemical estimations of blood i.e. lipid profile was performed and animals were sacrificed to carry out liver glycogen estimations.Results: At the end of study period, i.e. 28 d, STZ-induced rats showed marked hyperglycemia, hypertriglyceridemia and hypercholesterolemia. Body weight was reduced and the blood sugar level was significantly elevated in diabetic rats. The four-week treatment with MECL in a concentration of 200, 400 and 600 mg/kg significantly reversed the elevated levels of fasting blood glucose, serum cholesterol, serum triglyceride, liver glycogen, glycosylated haemoglobin with increase in body weight of diabetic rats.Conclusion: Thus the present study suggested the useful potential of Citrullus lanatus seed in diabetes due to its antidiabetic, hypoglycemic and antihyperlipidemic properties.Â

METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF ASCORBIC ACID AND FOLIC ACID VITAMINS BY REVERSE-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD IN CYANOBACTERIAL METABOLITES AND NUTRACEUTICAL FORMULATION

Objective: It was aimed to estimate ascorbic acid (ASC) and folic acid (FLC) in cyanobacterial metabolite by the reverse-phase high-performanceliquid chromatography (RP-HPLC) method, and the work was also extended to nutraceutical formulation.Methods: RP-HPLC method were developed for simultaneous estimation of two vitamins ASC and FLC in cyanobacterial metabolite and nutraceuticalusing isosbestic point at wavelength 280 nm. Method was selected after calculating system suitability and validated as per ICH guidelines.Results: The developed analytical method parameters found within limits prescribed by ICH and USP guidelines. The retention time was found to be2.334 and 3.892, respectively, for ASC and FLC. Limit of detection and limit of quantification for ASC and FLC were found to be 0.087 and 0.263 µg/ml,0.052 and 0.159 µg/ml, respectively. Recovery studies show that method is capable of recovering analytes from its formulation. The method is meetingthe criteria for validation as per the guidelines.Conclusion: The method is simple, precise, specific, and accurate. The newly developed method can be used in pharmaceutical industry for routineanalysis of ASC and FLC in tablet dosage form.Keywords: Cyanobacteria, Nutraceutical, Reverse-phase high-performance liquid chromatography, Ascorbic acid, Folic acid, Vitamins, Metabolites

Designing and Synthesis of Flavonoids Derivatives and Screening of their Antioxidant Activity

The flavonoids present in red wine were responsible this low cardiovascular mortality rate. Epidemiologic studies further suggest that dietary flavonoids are useful to control and protect the CHD. The flavonoids are yellow color substance (pigments) and the name given on the basis of Latin term Flavus which means yellow color. Flavonoids are derivatives of benzo-pyrone. Banzopyrone is a group of heterocyclic aromatic oxygen containing compounds. Finely powdered zinc chloride (8.25) was dissolved in glacial acetic acid (18ml)  by heating on sand bath then dry resorcinol (appx.5.5 gm) was added with  continuous  stirring to the mixture at  1400C. Antioxidant Screening by hydrogen peroxide scavenging assays. Hydrogen peroxide solution (40 mini moles) was prepared with standard phosphate buffer of pH 7.4. Different concentration of the compound stock solution and 4ml distilled water was added to 0.6 ml of hydrogen peroxide solution. UV absorbance was determined at the wavelength of 230 nm after 10 min with a blank solution containing phosphate buffer without H2O2. Take 4 ml different concentration of sample solution and 1ml sodium nitroprusside solution, added and incubated for 2.5 hrs at 370C. After incubation baseline was taken with methanol and 1ml sodium nitroprusside solution as blank solution. Griess reagent and methanol was added immediately before recording of readings. The readings were recorded at 546nm wavelenth. In the series of synthesized and evaluated compounds of Flavanoid electron withdrawing group at position four shows good activity. 2,3-dihydroflavan-3-ol derivatives showed lower activity than that of 3- hydroxyflavone derivatives. The 4-oxo (keto double bond at position 4 of the C ring), especially in association with the J2-J3 double bond, increases scavenger activity by delocalizing electrons, 3-hydroxy group on the C ring generates an extremely active scavenger; the combination of J2-J3 double bond,3-hydroxy group and 4-oxo group appears to be the best combination for potent antioxidant activity. Keywords: Flavonoids, Antioxidant activity, Hydrogen peroxide scavenging, free radical

Synthesis and Evaluation of Phenol Derivatives of Sulfonyl Chloride Quinoxaline

The objective of the present study was to synthesize some new 7-sulfonate of 2, 3- Diphenyl quinoxaline which are more potential as antibacterial than parent quinoxalines. The present study was synthesis of derivatives of sulfonyl chloride quinoxaline and physicochemical and spectral characterization, in vitro antimicrobial screening against gram positive and gram negative bacteria.The concentration of derivatives used as 200 and 400 microgram initially. When 200 µg concentrations was used R6 shows sensitivity towards S. aureus and R6 shows sensitivity towards gram negative E. coli organism. When 400 µg used then R3, R5, and R6 shows sensitivity in case of gram positive organism. And in case of gram negative organism R5, R6 shows sensitivity.Azithromycin is used as Reference drug and a comparative study was done. As compare to reference drug all derivatives shows less sensitivity than S- Standard and R- quinoxaline derivatives. Keywords: Diphenyl quinoxaline, QSAR, Quinoxaline, Phenol derivative

EVALUATION OF PHYSICOCHEMICAL STANDARDIZATION PARAMETERS OF SOLENA AMPLEXICAULIS LEAF

Solena amplexicaulis, commonly called as the creeping cucumber, belongs to the family Cucurbitaceae. Traditional it is used as astringent, appetizer, carminative, cardiotonic, digestive, diuretic, expectorant, invigorating, purgative and stimulant. Plant also having antioxidant antidiabetic and antibacterial action. The leaves showed potent anti-inflammatory activity.The present study was carried out to establish physico-chemical parameters along with preliminary phytochemical screening of petroleum ether, chloroform, methanolic and aqueous extracts of Solena amplexicaulis leaf. Preliminary phytochemical screening of various extracts revealed the presence of carbohydrate, alkaloids, flavonoids, sterols, phenolic & tannins compounds. The physico-chemical parameters such as total, water soluble, acid insoluble and sulphated ash (2.2, 1.9, 1.17 and 1.3%w/w respectively) and loss on drying (10.0 %w/w), extractive values foaming and swelling index were studied.   These studies will be helpful in developing standards for quality, purity and sample identification of this plant. Keyword: Standardization, Solena amplexicaulis, physicochemical and phytochemical

Designing and Synthesis of Flavonoids Derivatives and Screening of their Antimicrobial Activity

Antimicrobial drugs either kill microbes (microbicidal) or prevent the growth of microbes (microbistatic). The streptococcus mutans is a bacteria that found in the human mouth cavity. This bacterial strain produces plaque and acids that break down tooth enamel and cause dental caries. Gram positive cocci, facultatively anaerobic bacteria that forms rod-like chains. the chemical reaction of 2- hydroxyacetophenones with aromatic acylchloride occurs to form 1,3-diketones. This rearrangement reaction proceeds via enolate formation followed by acyl transfer. Then it cyclises into flavone.13 As the same of above scheme can be worked out as 2- Methoxybenzoyl Chloride is prepared by reaction of 2- methoxybenzoic acid  with  Thionyl chloride and DMF. 2-Methoxybenzoyl Chloride then added to mixture of 2- hydroxyacetophenone and pyridine, 2-[(2-Methoxybenzoyl)oxy]acetophenone thus obtained is treated with pyridine and KOH which gives1-(2-Hydroxyphenyl)-3-(2- methoxyphenyl)-propan1,3-dione. The result of study indicated that C5 [1-(2- hydroxyphenyl)-5-phenylpenta-2,4-dien-1-one]; is only inactive against Streptococcus mutans. All 3-hydroxyflavone derivatives exhibited their MIC to be in range of 250-125 µg/ml., 2,3-dihydroflavan-3-ol derivatives exhibited their MIC to be in  range of  1000- 500 µg/ml. The chalcone derivatives exhibited their MIC to be at 250 µg/ml. Keywords: Streptococcus mutans, flavonoids derivatives, MIC, 2,3-dihydroflavan-3-ol