Asian Journal of Pharmaceutical and Clinical Research

Aqueous extract of leaves of Solanum melongena Linn was investigated for its anti-inflammatory activity. Acute oral toxicity study according to OECD425 guidelines was done to find out the LD50 of test drug. Carrageenan induced paw oedema method in Wistar Albino rats were used in this study. Aspirin in the dose of 300mg/kg was used as the standard drug and three doses of aqueous extract of leaves of Solanum melongena L. (100mg/kg, 200mg/kg, 400mg/kg b.w.) was used as the test drug. The results were measured at 1(st) h, 3(rd) h, and 5(th) h after the carrageenan injection. In acute oral toxicity study none of the animals died at the dose of 2000mg/kg. Aqueous extract of Solanum melongena Linn leaf in the dose of 200mg/kg showed significant anti-inflammatory activity (p <0.05) at 3(rd) hr and highly significant anti-inflammatory activity (p<0.001) at 5(th) hr; in the dose of 400 mg/kg, test drug showed p<0.01 at 3(rd) and p<0.001 at 5(th) hr and in the dose of 100mg/kg it showed significant (p<0.05) anti-inflammatory activity at 5(th) hr. In doses of 200mg/kg and 400 mg/kg of aqueous extract of S. melongena L showed the percentage of inhibition of 42.62% which is less than the standard drug aspirin which showed 64.5% inhibition. Aqueous extract of leaves of Solanum melongena Linn has anti-inflammatory activity.

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p>ABSTRACT Over the last few decades, most of the pharmaceutical companies and research sponsors are facing a lot of challenges in clinical research for their new drug approval. The sponsor research needs a high-quality data report for getting new drug approval from Food and Drug Administration for their medical products. Clinical trial data are important for the drug and medical device development processing pharmaceutical companies to examine and evaluate the efficacy and safety of the new medical product in human volunteers. The results of the clinical trial studies generate the most valuable data and in recent years; there has been massive development in the field of clinical trials. A good clinical data management system reduces the duration of the study and cost of drug development. Further a well-designed case report form (CRF) assists data collection and make facilitates data management and statistical analysis. Nowadays, the electronic data capture (EDC) is very beneficial in data collection. EDC helps to speed up the clinical trial process and reduces the duration, errors and make the work easy in the data management system. This article highlights the importance of data management processes involved in the clinical trial and provides an overview of the clinical trial data management tools. The study concluded that data management tools play a key role in the clinical trial and well-designed CRFs reduces the errors and save the time of the clinical trials and facilitates the drug discovery and development. Keywords: Pharmaceutical, Clinical trial, Clinical data management, Data capture.</p

Objective. Pharmaceutical interaction between cytostatic drugs and its infusion fluids and packaging materials may cause therapy failure and reduce its cytostatic potential. Therefore, several tests on pharmaceutical interaction between several cytostatic drugs which are most commonly used in clinics and its infusion fluids need to be done. Methods. Some cytostatic drugs (such as cyslophosphamide, 5-fluorouracyl, cisplatin, and paclitaxel) are dissolved in certain concentration of NaCl 0.9% or Dextrose 5% infusion solution. Then, the solutions are incubated at room temperature and protected from sunlight. On the 0th hour (initial condition), 2nd, 4th, 8th, 12th, and 24th hour visual observations, pH measurement, and content measurement are performed. Results. Based on visual observations, it is indicated that there is no change in color, clarity, and particles of all solutions. At pH measurement, obtained changes in pH of cytostatic solution, which is still within the tolerable range of injection preparation (pH 4-10) and on active compounds stability range. Meanwhile, based on change of cytostatic concentration in each solution, it is indicated that there is no significant difference after 24-hour observation. Conclusion. Cytostatic drugs dissolved in NaCl 0.9% or Dextrose 5% infusion remained stable in terms of clarity, pH, and concentration level.

Objective: This study was conducted to analyze the effects obtained with different concentrations (0.5 and 0.1%) of propolis flavonoids on in vitro biofilm formation by clinical Streptococcus mutans strains isolated from children’s dental plaque.Materials and Methods: S. mutans isolated from children’s dental plaque was assayed for biofilm formation in 96-microwell plates using crystal violet.Results: The effects on S. mutans biofilm formation were the same for propolis flavonoids administered at concentrations of 0.05 and 0.1% (p>0.01).Conclusion: A 0.05% propolis flavonoids concentration was deemed as effective as a 0.1% concentration at inhibiting S. mutans biofilm formation.

Objective: The aim of this study was to obtain protein isolate from amaranth using alkaline method at extraction pH 8 and extraction pH 12 with different precipitation pHs and to analyze protein isolate with electrophoresis. Methods: Amaranth protein isolates were obtained using isoelectric precipitation method at different pHs. Proteins were analyzed using sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Results: A yield of 20.52% of protein isolate of defatted amaranth at pH 4.0 was obtained. The content of protein isolate was higher than 53% in all pH assays. Globulins and albumins in protein isolate at different pHs were observed. A band with 50 kDa corresponding to 7S globulin was found. The bands 36-38 kDa and 18-20 kDa correspond to 11S globulin. Bands less to 14.4 kDa correspond to albumins. Conclusions: Amaranth protein isolate is possible to obtain in extreme conditions of pH. The treatment with water was optimum to obtain amaranth protein isolate. © 2016, Innovare Academics Sciences Pvt. Ltd. All rights reserved.

Objectives: This study was carried out to compare intermittent bolus and continuous infusion for epidural labor analgesia in terms of total dose requirement of local anesthetic and quality of analgesia as primary objective. Secondary objective was level of sensory block, motor block, hemodynamic variables, mode of delivery, duration of second stage, neonatal outcome, side effects, and postpartum complications. Methods: Eighty women of ASA physical status I or II, with single pregnancy, cephalic presentation and cervical dilatation 3–5 cm, that is, during active labor were included in the study. Patients were randomly divided into two groups. In Group A, a bolus of 8 ml of 0.1% levobupivacaine (plain) with fentanyl 2 mcg/ml was given every hour and in Group B, an infusion of 0.1% levobupivacaine (plain) with fentanyl 2 mcg/ml at 8 ml/h was given. Pain scores using visual analog scale and verbal rating score, additional bolus requirement and total dose of local anesthetic, motor blockade, fetal and neonatal outcome, mode of delivery, and duration of second stage were recorded and compared. Side effects and postpartum complications if any were documented. Results: Additional bolus requirement and total dose of local anesthetic were significantly high in Group B (45.60±6.67 mg) as compared to Group A (34.20±5.58 mg). There was no difference in the quality of analgesia, neonatal outcome, mode of delivery, duration of second stage, side effects, and complications. Conclusion: Intermittent epidural bolus is better in terms of less drug consumption and less number of additional bolus requirement.

Objective: The objective of the current study is to assess the antibacterial efficiency of an herbal mouthwash (clove and neem) against 0.2% chlorhexidine and 2% betadone mouthwash in patients who have undergone Stage-1 implant surgery.Methods: 30 patients undergoing implant surgery (Stage-1) were divided into 3 groups and were given 3 different mouthwashes. The patient was recalled after 15 days. Swab samples from the site of implant were taken after 15 days and cultured. The results were tabulated.Results: 0.2% chlorhexidine and 2% bernadine were found to have better antibacterial efficiency than herbal mouthwash (p>0.05).Conclusion: The herbal mouthwash consisting of neem and clove was not efficient in killing microbes immediately after Stage-1 implant surgery when compared to 0.2% chlorhexidine and 2% bernadine.

Objective: The objective of present study was to compare the efficacy of 0.2% chlorhexidine and 0.25% sodium hypochlorite as a mouthwash in controlling chronic gingivitis.Methods: A total of 80 patients suffering from chronic marginal gingivitis were recruited for the study. Non-surgical periodontal therapy was completed for all the patients to bring the gingival status to healthy levels. The patients were divided into two study groups with 40 patients in each group, Group A patients were asked to use 0.2% chlorhexidine mouthwash, and Group B patients used 0.25% sodium hypochlorite mouthwash as an adjunct to brushing twice daily for 2 weeks. After a period of 2 weeks, the gingival status was recorded using the oral hygiene index simplified (OHIS), plaque index (PI), and modified gingival index (MGI) and compared between the two groups.Results: The mean OHIS score for Group A was 1.38 and for Group B it was 1.05. The mean PI for Group A and B was 3.62 and 2.32, respectively. The mean MGI score for Group A was 1.22 and for Group B was 1.20. Group B showed better results than Group A. Intergroup comparison of OHIS and PI revealed significantly better results in Group B than Group A while MGI did not show any statistical difference on comparison.Conclusion: Nearly 0.25% sodium hypochlorite was more effective than 0.2% chlorhexidine in reducing the gingival inflammation. Thus, 0.25% sodium hypochlorite may represent an efficacious, safe and affordable antimicrobial agent in the prevention and treatment of gingival disease.

Aim: This study is conducted to evaluate the efficacy of pre procedural mouth rinses, in reducing the bacterial count in the oral cavity which in turn could reduce the risk in generating aerosol. Objectives • To compare the effectiveness of herbal mouthwash as a pre procedural mouth rinse over 0.2% chlorhexidine mouthwash in reducing the bacterial count in saliva. • To determine the extent of the spread and to assess the amount of contamination in the clinical environment by collecting the aerosol at 1 foot, 2 feet and 3 feet distance after the pre procedural mouth rinsing with herbal mouthwash and 0.2% chlorhexidine mouthwash. • To know whether the reduction of bacterial count in the saliva has any effect on the expected proportionate reduction of the aerosol production in the two groups of patient with herbal and chlorhexidine mouthwash. Material and methods: A total of 30 patients were selected and randomly divided into three groups. Group I consists of 10 patients who rinsed with normal saline for 60 seconds. Group II consists of 10 patients who rinsed with 0.2% chlorhexidine mouthwash for 60 seconds. Group III consists of 10 patients who rinsed with herbal mouthwash for 60 seconds. Salivary sample were collected in sterile disposable container before the mouth rinse and 5 minutes after the mouth rinsing. The samples were subjected to bacteriological analysis to estimate the total bacterial count. Aerosols produced during the oral prophylaxis procedure were collected on BHI agar plates by exposing the plates at 1 foot, 2 feet and 3 feet distance and the exposed plates were incubated at 37°c aerobically for 24 hours. The number of colony forming units (CFU) in aerosol and CFU in the saliva were counted and statistically analyzed. Care was taken to exclude the bacterial colonies that were of non oral origin. Results: Reduction in the bacterial load using 0.2% of chlorhexidine gluconate mouthwash is found to be significant in both saliva and aerosol produced during scaling. Although the CFU is reduced to 99.91% in saliva, the reduction is not proportionate in the aerosol produced among the same group. Conclusion: Chlorhexidine mouthwash as a pre procedural rinse is more effective than the herbal mouthwash. Preprocedural rinse has a definite benefit in the treatment perspective but as aimed, the reduction in the bacterial load in saliva has not proportionately decrease the bacterial load in the aerosol.

Objective: To evaluate the efficacy and safety of tamsulosin 0.4mg once daily compared with placebo in men with symptomatic benign prostatic hyperplasia. Patients and method: In this randomised, placebo-controlled study 69 patients were enrolled. Of these 51 were receive tamsulosin 0.4 mg and 18 patients were receive placebo once daily for 12 weeks. Study was designed to compare the efficacy safety and of tamsulosin verses placebo group. The primary outcome measures were; mean changes in total and /or individual I-PSS score, prostate volume and life style questionnaire, from baseline to 12 weeks of study. Result: Tamsulosin significantly improved lower urinary tract symptoms compared to placebo, with a mean change in I-PSS scores from baseline to end of the study was 16.7 VS 9.0 for placebo (P ≤0.0002). Improvement in symptoms was 85.74%. Compare to placebo. The life style questionnaire was significantly improved in tamsulosin group. Adverse events were similar to placebo, most common observed adverse event was dizziness (4.34%) similar to placebo ((7.14 %). While sexual disorder ((2.1% delayed ejaculation) was prominent in tamsulosin group. Conclusion: Once daily dosing of tamsulosin at bed time at a fix dose level (0.4mg) offers an efficient improvement in total and individual I-PSS score but have no effect on prostate volume, adverse events other than ejaculatory disorder were similar to placebo. Tamsulosin is safe and well tolerated and most effective for treatment of symptomatic BPH at a short term basis.

Objectives: Pupillary dilatation is an integral part of comprehensive ophthalmic examination. It is also essential for cataract surgery and outpatient laser procedures. Rapid and sustained dilatation is often required. It has been proposed that prior instillation of proparacaine 0.5% can potentiate the effect of the routinely used tropicamide 0.8% phenylephrine 5% combination mydriatic agent. However, certain studies have shown that it is not effective in dark colored iris as compared to light colored iris; hence, this study was done on a predominantly South Indian population with dark iris. Methods: Hundred eyes of 50 patients requiring pupillary dilatation as part of routine ophthalmic evaluation were included in the study. The patients were divided into two groups. The study group was given 0.5% proparacaine before instillation of mydriatic agent and the control group was given only tropicamide 0.8% and phenylephrine 5% eye drops. Pupillary dilatation was measured after 15 min and 30 min in both eyes. The end point was taken as 6 mm pupillary dilatation. Results: There was a statistically significant difference in the rate of pupillary dilatation between the control and the study group at 15 min and 30 min after instillation of eye drops. Conclusion: The study concluded that prior instillation produced faster dilatation even in patients with dark colored iris; hence, we suggest the use of topical anesthetic proparacaine 0.5% in situations where rapid mydriasis is required.

Objective: Intrathecal magnesium as an adjuvant to hyperbaric ropivacaine could extend duration of sensory blockade and improve the quality of post-operative analgesia; thereby reducing opioid requirements and its adverse effects. Hence, we conducted this prospective, randomized, double-blind clinical trial to observe its effects for day care surgeries. Methods: After obtaining institutional ethical committee approval and registration of trial, patients’ informed consent was taken and eighty adult patients of either gender, ASA 1 and 2, posted for infra umbilical surgeries were divided into two groups: Group RM received 3 ml hyperbaric Ropivacaine with 0.75 ml magnesium sulfate (75 mg) and Group R received 3 ml hyperbaric Ropivacaine with 0.75 ml sterile water. Sensory and motor blockade parameters, hemodynamic variables, and adverse effects were monitored, analyzed using appropriate statistical tests. Results: Total duration of sensory blockade was significantly prolonged in Group RM compared to Group R (242.8 ± 9.9 versus 186.6 ± 8.4 min) (***p<0.001). Complete motor regression was observed significantly earlier in Group RM than in Group R (151.3 ± 7.8 versus 184.7 ± 5.6 min) (*p<0.05). Post-operative pain free interval was significantly prolonged in group RM compared to group R (725.2 ± 18.6 vs. 515.2 ± 17.8 min) (***p<0.001). Conclusion: We concluded that intrathecal magnesium as an adjuvant to hyperbaric Ropivacaine significantly prolonged both sensory blockade duration, post-operative pain-free interval without increasing motor blockade duration and the incidence of adverse effects.

Objectives: The objective of the study was to compare the efficacy of adjuvant use of subarachnoid fentanyl with the adjuvant use of subarachnoid magnesium sulfate as adjuvants to bupivacaine in subarachnoid block for infraumbilical surgeries in terms of: (1) Block characteristics, namely, time taken for onset of block and time taken for regression of block, (2) Hemodynamic stability in intra- and post-operative phase. Methods: A total of 70 ASA I/II patients scheduled for infra-umbilical surgery were enrolled in the study and were randomized either to Group F (0.5 mL Fentanyl+3 mL 0.5% Bupivacaine) (n=35) or to Group M (0.5 mL 20% Magnesium sulfate+3 mL 0.5% Bupivacaine). Time to achieve onset of block, duration of block. Data were analyzed using the Chi-square and Independent samples, t’-test. Results: Age of patients ranged from 18 to 55 years. The two groups were matched onset of sensory and motor block was significantly earlier in Magnesium sulfate group as compared to fentanyl group. Regression of motor and sensory block was significantly earlier in group where magnesium sulfate was used as an additive in contrast to fentanyl. No other complication except nausea (8.6%) and bradycardia (8.6%) was reported in any of the patient. Conclusion: Although magnesium sulfate appears to be a relatively safer alternative than fentanyl for adjuvant use with hyperbaric bupivacaine for post-operative pain management and to facilitate better block characteristics; however, it fails to achieve the analgesic effect even comparable to fentanyl. Further studies with inclusion of a control group and with changed drug–dose combinations are recommended to find out a better alternative.

Chronic Myelogenous Leukemia (CML) and Philadelphia chromosome positive (Ph+) Acute Lymphoblastic Leukemia (ALL) are caused by the BCR-ABL oncogene. Imatinib inhibits the tyrosine kinase activity of the BCR-ABL protein and is an effective, frontline therapy for chronic-phase CML. However, accelerated or blast-crisis phase CML patients and Ph+ ALL patients often relapse due to drug resistance resulting from the emergence of imatinib-resistant point mutations within the BCR-ABL tyrosine kinase domain. This has stimulated the development of new kinase inhibitors that are able to over-ride resistance to Imatinib. The novel BCR-ABL inhibitor, AN-024, was designed to fit into the ATP-binding site of the BCR-ABL protein with higher affinity than Imatinib. In addition to being more potent than Imatinib (IC50<1 nM) against wild-type BCR-ABL, AN-024 is also significantly active against Imatinib-resistant BCR-ABL mutants. In preclinical studies, AN-024 demonstrated activity in vitro and in vivo against wild-type and Imatinib-resistant BCR-ABL expressing cells.

Objective: The main aim of this study is to prevent biofilm formation by impregnating an antimicrobial on urinary catheter.Methods: Catheter segments were immersed in the antimicrobial compound for impregnation. After 2 h, the segments were removed, sterilized and dried after which mechanical and antimicrobial properties of the catheter segments were determined. The shelf life of the impregnated segments was also ascertained as well as anti-biofilm assay. Spectral analysis (UV & FTIR) was also performed.Results: Impregnation was achieved by immersing catheter segments in antimicrobial compound ensuring it does not affect the catheter texture. The impregnated antimicrobial catheters were able to prevent colonization by common uropathogens Escherichia coli, Proteus, Pseudomonas aeruginosa, Staphylococcus aureus, Klebsiella, and Candida albicans for up to 12 weeks. Antibiotic impregnation of the catheters did not affect the mechanical properties and did not render it as unfit for insertion. The antimicrobial-impregnated catheter offers a means of reducing biofilm formation and subsequently reducing the infection in long-term urinary catheter users. Spectral analysis was done by UV-Vis and FTIR.Conclusion: Antibiotic impregnation of the catheters did not affect the mechanical properties and did not render it as unfit for insertion. The antimicrobial impregnated catheter offers a means of reducing biofilm formation and subsequently reducing the infection in long-term urinary catheter users.

Objective: Antioxidants are vital substances which possess the ability to protect the body from damage caused by free radical-induced oxidative stress. The purpose of this study is to determine antioxidant activities of alkaloid fractions of Zanthoxylum acanthopodium DC. fruits.Methods: Z. acanthopodium DC. fruit was extracted by maceration. Ethanol extract was fractionated with liquid-liquid extraction using n-hexane and chloroform at pH 3, 7, 9, and 11 to obtained alkaloid fractions. Antioxidant activity for extract and fractions was determined with 1,1-diphenyl-2- picrylhydrazyl.Results: The IC50 of extract and fractions was 101.11±0.11, 273.24±0.12, 116.62±0.04, 61.12±0.01, 23.15±0.01, and 112.39±0.04 μg/mL, respectively.Conclusion: The results reveal that alkaloid fractions of Z. acanthopodium DC. fruit have very strong antioxidant potential. Our further study is to isolate the alkaloid compounds.

Objective: This study was designed to evaluate in vitro antioxidant activity and wound healing activity in Triticum aestivum (wheat grass).Methods: T. aestivum commonly known as Wheatgrass had a wide range of health benefits among the young grass of common wheat plant components includes chlorophyll, flavonoids, and Vitamins A, C, and E. Wheatgrass is used in Folklore medicine for treatment of skin diseases and wound healing. In our present study, petroleum ether, ethanol and aqueous extracts of T. aestivum have been evaluated for in vitro antioxidant activity and wound healing activity by 1,1- diphenyl, 2 Picrylhydrazyl radical scavenging activity, and Chick chorioallantoic method, respectively.Results: The results of both the assay showed that all the extracts of T. aestivum have significant antioxidant and wound healing activity on dose-dependent manner.Conclusion: The wheatgrass has antioxidant and wound healing activity.

Objectives: The aim of the present study is to isolate an antifungal compound from Derris indica (Lam) Bennett seed oil with various solvents and evaluation of its antifungal activity against the clinical species of Candida. Methods: D. indica seed hexane extract was tested against Trichophyton rubrum, Trichophyton tonsurans and Candida albicans. Hexane extract was fractioned using different solvents through column chromatography (CC). Isolated compound D1 was identified and characterized using ultraviolet, Fourier-transform infrared, 1HNMR, and mass spectroscopy. In vitro evaluation of D1 carried out against 12 Candida strains. In vivo evaluation of D1 carried out against T. rubrum, T. tonsurans, and C. albicans using an excision wound healing model on male Wistar rats. Results: Different concentrations of hexane extract showed antimicrobial activity against tested microorganism with varying minimum inhibitory concentration values. On fractionation with hexane-petroleum ether through CC, it yielded a crystalline fraction. Compound D1 characterized as a 3,5-bis (4,4’’-dimethoxy-[1,1’: 2’,1’’-terphenyl]-4’-yl)-4H-pyrazole-4,4-diol. A novel alkaloid compound from D. indica is a new report and proved to be inhibitory against C. albicans MTCC 3017 (14.83±0.28), MTCC 1637 (16.0±0.0), Candida glabrata MTCC 3814 (16.83±0.28) and MTCC 3014 (16.66±0.57), Candida tropicalis MTCC 230 (20.0±0.0), MTCC 1406 (12.33±0.57). C. glabrata MTCC 3981 was found to be resistant to the compound. In vivo studies showed no visual symptoms at the end of treatment indicating the therapeutic property of the compound. Conclusion: The D1 was found to be effective against human fungal pathogens and can be used as a base molecule in designing new antifungal drugs.

Objective: The objective of this work was to synthesize and evaluate antimicrobial properties of 1-(4-methyl-6-nitro-2H-benzo[b][1,4]thiazine- 3(4H)-ylidene)hydrazine-1,1-dioxide derivatives.Methods: These new compounds were synthesized by methylation in 4-N and reacted with hydrazine derivatives and oxidized at the sulfur atom by 30% hydrogen peroxide to obtain sulfones. All the synthesized compounds were evaluated for antimicrobial activity using the disc diffusion method.Results: The Fourier transform infrared, 1H nuclear magnetic resonance (NMR), 13CNMR, and mass studies confirm the synthesis of some new 1-(4-methyl- 6-nitro-2H-benzo[b][1,4]thiazine-3(4H)-ylidene)hydrazine-1,1-dioxide derivatives. Compound 6f showed the potent antimicrobial activity.Conclusion: Result obtained in this research work clearly indicated that the compound 6f having methyl at 2 position and nitro groups at 2′ and 4′ position showed the most potent antimicrobial activity.

Objective: The herbal medicines do not have any side effect and it is cost effective and safest medicine from an ancient periods. Urolithiasis or Lithiasis is a consequence of complex physical processes. The major factors are supersaturation of urine with the offending salt and crystallization. Crystals retained in kidney can become nucleus for stone formation. This process is synonymously known as Urolithiasis or Lithiasis or Nephrolithiasis or Kidney stones or renal calculi. Calcium-containing stones are the most common comprising about 75% of all urinary calculi, which may be in the form of pure calcium oxalate (50%) or calcium phosphate (5%) and a mixture of both (45%). In this study, ethanolic & aqueous extracts of roots and rhizomes of Hedychium coronarium J. Koenig plant were evaluated for their potential to dissolve experimentally prepared kidney stones like calcium oxalate by titrimetic method with an invitro model and Antioxidant activity performed by DPPH scavenging assay method. Phytoconstituents were also isolated by chromatographic techniques of this plant species. Method: For performing invitro antilithiatic activity titrimetic method was adopted and for antioxidant activity 1,1-diphenyl-2-picryl hydrazyl (DPPH) scavenging assay method was adopted. Phytoconstituents were isolated by column and thin layer chromatographic techniques. Results & Conclusion: Ethanolic roots & rhizomes extract of this plant produced highest dissolution of stones when compare to standard drug cystone and at 10 mg. concentration. Also this study showed alcoholic extract of roots & rhizomes of Hedychium coronarium J. Koenig plant in higher concentration possess best antioxidant potential as compare to standard ascorbic acid with IC50 value 9.0 and 18.9 μg/ml. for ascorbic acid and alcoholic extract respectively. Isolated phytoconstituent from alcoholic extract of this plant was 8a, hydroxy hedychilactone and its structure was confirmed by IR, NMR and Mass spectroscopic datas. © 2015, Asian Journal of Pharmaceutical and Clinical Research. All right reserved.

Objective: The present study aims to synthesize a novel derivatives of Imidazo[1,2-a]pyridines and the compounds were evaluated for their antibacterial activity.Methods: A series of newly synthesized compounds were characterized by 1H-nuclear magnetic resonance (NMR), 13C-NMR, Fourier transform infrared, mass spectral analysis, and screened for their antibacterial activity by disc diffusion method. Molecular docking studies were performed with a bacterial beta subunit of DNA gyrase using Auto Dock 4.2.6, and the docked conformations were analyzed using visual molecular dynamics.Results: The structural activity relationship of the synthesized imidazo[1,2-a]pyridine derivatives was studied against Gram-positive and Gram-negative bacteria. Among the synthesized compounds N-benzyl-4-((2-(6-methyl-2-(p-tolyl)imidazo[1,2-a]pyridin-3-yl) acetamido)methyl) benzamide (9a) are possessing high activity against Bacillus subtilis. The zone of inhibition produced by the compound 9a is wider than that of remaining compounds used in this study.Conclusion: The synthesized compounds exhibited good antibacterial activity in comparison with standard drug streptomycin. This suggests that the compound 9a and its analogs are exerting their activity by probably inhibiting bacterial beta subunit of DNA gyrase.

Objective: The aim of this study was to evaluate the colon cancer protective activity of Cycas revoluta (Cycadaceae).Methods: Methanolic extracts of C. revoluta (MECR) were assessed for total polyphenols and total flavonoids content. For the in vivo study, animals were divided into five groups (n=6). Group I serves as control which received 0.25% carboxymethyl cellulose solution. Groups II-V were treated with 1,2-dimethylhydrazine (DMH) which was given at the dose of 20 mg/kg b.w., s.c. once a week for 4 consecutive weeks. Aqueous suspension of MECR at a dose of 200 mg/kg/day and 400 mg/kg was administered orally to the animals in Groups III-IV every day for 16 weeks. Group V received 5-fluorouracil (5-FU) as a standard drug at a dose of 10 mg/kg b.w., per day s.c. for 16 weeks. After that, animals are sacrificed and colons are taken separately to evaluate biochemical parameters and morphological and histopathological changes.Results: MECR contains total polyphenols (6.3±0.09 mg of gallic acid equivalent /g) and total flavonoids (4.6±0.06 mg of rutin equivalent/g). The in vivo study revealed that superoxide dismutase (SOD), catalase, and reduced glutathione (GSH) activity were decreased in DMH Group. All these parameters were restored significantly (p<0.05) toward the near normal value on supplementation with MECR (200 and 400 mg/kg b.w.) to DMH-treated rats (Groups III and IV). In Group V, the synthetic standard drug 5-FU (10 mg/kg b.w.) also increases the activities of SOD, CAT, and GSH significantly (p<0.05) more in DMH-treated rats.Conclusions: It can be concluded that MECR protects rat from DMH-induced colon cancer.

Objectives: The present work planned to investigate the anti-bacterial, anti-fungal, and anti-oxidant activity against 4-amino benzamide derived 1,2,3-triazole linked chalcone and pyrazoline derivatives. Methods: Anti-microbial activity for pyrazoline derivatives was accomplished by serial dilution method. The test organisms of bacterial strains were (Enterococcus faecalis, Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas fluorescence) and the fungal cultures (Aspergillus niger, Aspergillus terreus, and Trichoderma harzanium). The method used in the anti-oxidant activity is 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide scavenging method. Results: All the compounds showed good to moderate anti-bacterial and anti-fungal activities. The results of IC50 values showed lower potent inhibition activity with DPPH and higher potent inhibition activity in nitric oxide scavenging method. Conclusion: All the compounds had exhibited capricious growth inhibitory effect on anti-bacterial, anti-fungal, and anti-oxidant activities.

Objective: The objective of the study was to synthesis of 1,2,3,4-tetrahydro-4-oxo-6-(5-substituted 2-phenyl-1H-indol-3-yl)-2-thioxopyrimidine-5- carbonitrile derivatives (4a-c). Methods: The structures of all these unknown compounds have been confirmed with the help of physical and spectral techniques such as IR, 1H, and 13C NMR and mass spectral data and these newly synthesized compounds were evaluated for in-vitro antimicrobial and antitubercular activities. Results: Screening studies have demonstrated that the newly synthesized compound 4a exhibited promising antimicrobial and antitubercular properties. Conclusion: The final results revealed that compound 4a exhibited promising antimicrobial and antitubercular properties when compared to the standard drugs.