Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150501
Binal N Patel, Hitesh J Vekaria
Sofosbuvir is an antiviral drug that is used to treat hepatitis C. A present investigation deals with simple, sensitive, rapid, precise and accurate reverse phase high-performance chromatography (RP-HPLC) method developed and validated for related substances of sofosbuvir in tablet dosage form. The chromatographic separation was achieved on a Kromasil 100 C18 (250 × 4.6 mm, 5 μ) column. A sofosbuvir and its impurities were extracted by composed mixture of Mobile Phase A: buffer solution: acetonitrile (97.5:2.5% v/v) and Mobile Phase B: acetonitrile, isopropyl alcohol, methanol and purified water (60:20:10:10 % v/v/v/v) using with flow rate was 1-mL/min, column temperature was 25°C, injection volume was 10 μL, Vial thermostat temperature was 10°C. The UV detection was carried out at 263 nm. The retention time of sofosbuvir, methyl ester and ethyl ester were 54.28, 36.31 and 43.77, respectively. The method shows linearity with correlation coefficient of sofosbuvir and its impurity was 0.999 over the 0.5–7.5 ppm range. The average recovery was found to be 90.2–113.9%. The LoD and LoQ for sofosbuvir and its impurities were found to be 0.1 and 0.5 μg/mL, respectively. The method was validated as per ICH guidelines. The developed method was precise, accurate, novel and detectable towards sofosbuvir and its impurity. This method is efficient in separating the sofosbuvir and its impurity. Hence, the proposed method can be utilized for the determination of related substances in routine analysis in quality control department of pharmaceutical Industry.
{"title":"A Stability Indicating Reverse Phase High Performance Liquid Chromatography Method for Related Substances of Sofosbuvir in Tablet Dosage Form","authors":"Binal N Patel, Hitesh J Vekaria","doi":"10.25004/ijpsdr.2023.150501","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150501","url":null,"abstract":"Sofosbuvir is an antiviral drug that is used to treat hepatitis C. A present investigation deals with simple, sensitive, rapid, precise and accurate reverse phase high-performance chromatography (RP-HPLC) method developed and validated for related substances of sofosbuvir in tablet dosage form. The chromatographic separation was achieved on a Kromasil 100 C18 (250 × 4.6 mm, 5 μ) column. A sofosbuvir and its impurities were extracted by composed mixture of Mobile Phase A: buffer solution: acetonitrile (97.5:2.5% v/v) and Mobile Phase B: acetonitrile, isopropyl alcohol, methanol and purified water (60:20:10:10 % v/v/v/v) using with flow rate was 1-mL/min, column temperature was 25°C, injection volume was 10 μL, Vial thermostat temperature was 10°C. The UV detection was carried out at 263 nm. The retention time of sofosbuvir, methyl ester and ethyl ester were 54.28, 36.31 and 43.77, respectively. The method shows linearity with correlation coefficient of sofosbuvir and its impurity was 0.999 over the 0.5–7.5 ppm range. The average recovery was found to be 90.2–113.9%. The LoD and LoQ for sofosbuvir and its impurities were found to be 0.1 and 0.5 μg/mL, respectively. The method was validated as per ICH guidelines. The developed method was precise, accurate, novel and detectable towards sofosbuvir and its impurity. This method is efficient in separating the sofosbuvir and its impurity. Hence, the proposed method can be utilized for the determination of related substances in routine analysis in quality control department of pharmaceutical Industry.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139315898","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150503
Sainika H Kanzaria, T. Gandhi, K. Patel
Despite abundant anti-arthritic therapies, there always remains an opportunity to identify novel drugs as well as targets. One such emerging drug Capparis aphylla Roth. acting on inflammatory cascades. This study was planned to investigate the effect of C. aphylla Roth. on inflammatory cascade in rheumatoid arthritis induced in wistar albino rats. The rheumatoid arthritis was induced by injection of 0.2 mL complete Freund’s adjuvant. The animals were randomized into six groups receiving either vehicle (control), injection of 0.2 mL complete Freund’s adjuvant (model) or treatments (indomethacin 100 mg/kg and methanolic extract of C. aphylla Roth. 190, 240, 300 mg/kg) for 21 days. Various hemodynamic parameters, anti-inflammatory parameters, and x-ray and histopathology of synovial joints were carried out. Paw volume, body weight, arthritic index, ESR, RF, CRP, A/G ratio estimated. Treatment with methanolic extract of C. aphylla Roth. Significantly prevented the rise in body weight, serum A/G ratio and increased arthritic index, paw volume, ESR, RF, CRP. The normal architecture of synovial joints was preserved in histopathological analysis by methanolic extract of C. aphylla Roth. treatment. Furthermore, the prevention of damage in joints carried out by methanolic extract of C. aphylla Roth. Altogether, methanolic extract of C. aphylla Roth. prevented architecture and functions of joints by augmenting the inflammation in complete freund’s adjuvant rats. Such promising effects are attributed to inflammation by novel herbal drug C. aphylla Roth.
尽管抗关节炎疗法非常丰富，但仍有机会发现新的药物和靶点。Capparis aphylla Roth.就是这样一种作用于炎症级联的新兴药物。本研究计划调查 C. aphylla Roth.对类风湿关节炎的炎症级联的影响。类风湿性关节炎是通过注射 0.2 mL 完全弗氏佐剂诱发的。动物被随机分为六组，分别接受载体（对照组）、注射 0.2 mL 完全弗氏佐剂（模型组）或治疗（吲哚美辛 100 mg/kg 和 C. aphylla Roth 的甲醇提取物 190、240、300 mg/kg）。190、240、300 毫克/千克），为期 21 天。对滑膜关节进行了各种血液动力学参数、抗炎参数、X光和组织病理学检查。估算了爪体积、体重、关节炎指数、血沉、射频、CRP、A/G 比值。用 C. aphylla Roth.显著防止了体重、血清 A/G 比率的上升，并增加了关节炎指数、爪体积、血沉、射频、CRP。经 C. aphylla Roth.甲醇提取物处理后，滑膜关节的正常结构在组织病理学分析中得以保留。此外，C. aphylla Roth.甲醇提取物还能预防关节损伤。总之，C. aphylla Roth.的甲醇提取物通过增强完全弗伦德佐剂大鼠的炎症，防止了关节的结构和功能。新型草药 C. aphylla Roth.
{"title":"Ameliorating Effect of Capparis aphylla Roth. in Adjuvant-induced Arthritis in rats with Reference to Changes in Reactants RF, CRP, Radiological Erosions","authors":"Sainika H Kanzaria, T. Gandhi, K. Patel","doi":"10.25004/ijpsdr.2023.150503","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150503","url":null,"abstract":"Despite abundant anti-arthritic therapies, there always remains an opportunity to identify novel drugs as well as targets. One such emerging drug Capparis aphylla Roth. acting on inflammatory cascades. This study was planned to investigate the effect of C. aphylla Roth. on inflammatory cascade in rheumatoid arthritis induced in wistar albino rats. The rheumatoid arthritis was induced by injection of 0.2 mL complete Freund’s adjuvant. The animals were randomized into six groups receiving either vehicle (control), injection of 0.2 mL complete Freund’s adjuvant (model) or treatments (indomethacin 100 mg/kg and methanolic extract of C. aphylla Roth. 190, 240, 300 mg/kg) for 21 days. Various hemodynamic parameters, anti-inflammatory parameters, and x-ray and histopathology of synovial joints were carried out. Paw volume, body weight, arthritic index, ESR, RF, CRP, A/G ratio estimated. Treatment with methanolic extract of C. aphylla Roth. Significantly prevented the rise in body weight, serum A/G ratio and increased arthritic index, paw volume, ESR, RF, CRP. The normal architecture of synovial joints was preserved in histopathological analysis by methanolic extract of C. aphylla Roth. treatment. Furthermore, the prevention of damage in joints carried out by methanolic extract of C. aphylla Roth. Altogether, methanolic extract of C. aphylla Roth. prevented architecture and functions of joints by augmenting the inflammation in complete freund’s adjuvant rats. Such promising effects are attributed to inflammation by novel herbal drug C. aphylla Roth.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316303","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150507
Tanvir Y. Shaikh, S. Lodhi
Myricetin is considered a flavonols under the category of flavonoids. According to recent research, myricetin has different curative effects on diabetes, cancer, and the heart. It has been suggested that myricetin is a more potent antioxidant than quercetin. The present study aimed to investigate the wound healing effect of myricetin loaded nanoemulsion (MYCT-NE) gel formulation in diabetic animals. Myricetin-loaded nanoemulsion was converted in nanoemulsion gel using carbopol 934 and evaluated for diabetic wound healing effect against wound contraction measurement, hydroxyproline estimation, protein estimation, antioxidant assay and histopathological study. On day 18th of treatment, the wound contraction of Faster wound healing was observed in the MYCT-NE gel treated groups compared to the control group, as indicated by a shorter epithelialization duration. Increased collagen turnover was shown by increased hydroxyproline levels in MYCT-NE gel-treated tissue, which sped up the healing of treated wounds. MYCT-NE gel possesses effective antioxidant activity by restoration of the superoxide dismutase SOD, GSH and catalase level in the wound tissues after treatment and healing. The observations showed that the original tissue regeneration was found efficiently in the wound treated with MYCT-NE gel and reference group without edema and congestion. The results obtained in the present study were indicated that MYCT-NE gel accelerates cutaneous diabetic wound healing through reducing oxidative status in experimental animals.
{"title":"Evaluation of Myricetin loaded Nanoemulsion Formulation for the Management of Diabetic Wound Healing in Experimental Animals","authors":"Tanvir Y. Shaikh, S. Lodhi","doi":"10.25004/ijpsdr.2023.150507","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150507","url":null,"abstract":"Myricetin is considered a flavonols under the category of flavonoids. According to recent research, myricetin has different curative effects on diabetes, cancer, and the heart. It has been suggested that myricetin is a more potent antioxidant than quercetin. The present study aimed to investigate the wound healing effect of myricetin loaded nanoemulsion (MYCT-NE) gel formulation in diabetic animals. Myricetin-loaded nanoemulsion was converted in nanoemulsion gel using carbopol 934 and evaluated for diabetic wound healing effect against wound contraction measurement, hydroxyproline estimation, protein estimation, antioxidant assay and histopathological study. On day 18th of treatment, the wound contraction of Faster wound healing was observed in the MYCT-NE gel treated groups compared to the control group, as indicated by a shorter epithelialization duration. Increased collagen turnover was shown by increased hydroxyproline levels in MYCT-NE gel-treated tissue, which sped up the healing of treated wounds. MYCT-NE gel possesses effective antioxidant activity by restoration of the superoxide dismutase SOD, GSH and catalase level in the wound tissues after treatment and healing. The observations showed that the original tissue regeneration was found efficiently in the wound treated with MYCT-NE gel and reference group without edema and congestion. The results obtained in the present study were indicated that MYCT-NE gel accelerates cutaneous diabetic wound healing through reducing oxidative status in experimental animals.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150512
S. Roshan, Dharani Gunaseelan, Sherin Benazsir, Nithya Pandian, Swaminathan K. Jayachandran, Mahesh Kandasmy, Anusuyadevi Muthuswamy
Cognitive disorders, including dementia and Alzheimer’s disease, pose substantial global health challenges, demanding effective prevention and treatment strategies. Intermittent hypoxia therapy (IHT), involving brief exposures to reduced oxygen levels, is a novel approach with potential cognitive benefits. This study investigates the effects of IHT on cognitive behavior in wistar albino rats through comprehensive behavioral experiments, including the open field test (OFT) and Morris water maze (MWM). The results reveal that IHT promotes locomotor activity, reduces anxiety-related behaviors, and positively impacts cognitive flexibility. In the OFT, the IH group exhibited increased grid crossings and distance traveled, indicating heightened locomotion, which may be associated with cognitive improvement. Furthermore, IH significantly reduced thigmotaxis behavior and the number of fecal boli, indicating reduced anxiety levels compared to the control group. While IHT did not significantly enhance spatial memory acquisition in the MWM, it improved platform recognition during the probe test. The IH group spent more time in the target quadrant, suggesting enhanced memory retrieval and recognition. Additionally, in the reverse MWM, IH demonstrated moderate improvements in cognitive flexibility, with faster latency on trial 1. These findings suggest that IHT holds promise as a non-invasive intervention for cognitive enhancement, particularly in terms of locomotor activity, anxiety reduction, and certain aspects of memory and cognitive flexibility. Further research is warranted to elucidate the underlying mechanisms and explore the potential therapeutic applications of IHT in cognitive disorders. In summary, this study highlights the cognitive benefits of IHT in rats, paving the way for future investigations and potential clinical applications in the realm of cognitive disorders.
{"title":"Acute Intermittent Hypoxia Therapy alters Cognitive Behavioral Parameters in Wistar Albino Rats","authors":"S. Roshan, Dharani Gunaseelan, Sherin Benazsir, Nithya Pandian, Swaminathan K. Jayachandran, Mahesh Kandasmy, Anusuyadevi Muthuswamy","doi":"10.25004/ijpsdr.2023.150512","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150512","url":null,"abstract":"Cognitive disorders, including dementia and Alzheimer’s disease, pose substantial global health challenges, demanding effective prevention and treatment strategies. Intermittent hypoxia therapy (IHT), involving brief exposures to reduced oxygen levels, is a novel approach with potential cognitive benefits. This study investigates the effects of IHT on cognitive behavior in wistar albino rats through comprehensive behavioral experiments, including the open field test (OFT) and Morris water maze (MWM). The results reveal that IHT promotes locomotor activity, reduces anxiety-related behaviors, and positively impacts cognitive flexibility. In the OFT, the IH group exhibited increased grid crossings and distance traveled, indicating heightened locomotion, which may be associated with cognitive improvement. Furthermore, IH significantly reduced thigmotaxis behavior and the number of fecal boli, indicating reduced anxiety levels compared to the control group. While IHT did not significantly enhance spatial memory acquisition in the MWM, it improved platform recognition during the probe test. The IH group spent more time in the target quadrant, suggesting enhanced memory retrieval and recognition. Additionally, in the reverse MWM, IH demonstrated moderate improvements in cognitive flexibility, with faster latency on trial 1. These findings suggest that IHT holds promise as a non-invasive intervention for cognitive enhancement, particularly in terms of locomotor activity, anxiety reduction, and certain aspects of memory and cognitive flexibility. Further research is warranted to elucidate the underlying mechanisms and explore the potential therapeutic applications of IHT in cognitive disorders. In summary, this study highlights the cognitive benefits of IHT in rats, paving the way for future investigations and potential clinical applications in the realm of cognitive disorders.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316133","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Different disorders and physiological process have been found to be associated with monoacylglycerol lipase enzyme in humans, like pain, inflammation, and neurodegenerative diseases also. The enzyme is a 33 KDa in weight and a type of serine hydrolase enzyme in nature. The presence of enzyme has been reported in both central and peripheral nervous systems and has show its importance as a key signalling factor in endocannabinoid signalling network system. The enzyme has also reported as source of free fatty acid provider for the cancer cell and tumor growth and their proliferation. In proliferative cancer cells, increased the monoacylglycerol lipase activity is observed. The growth, migration and survival of cancer cells have also found to be associated with phosphatidic acid, lysophosphatidic acid, sphingosine phosphate and prostaglandin E2, which are act as signalling molecules and are found to be derived from free fatty acid. These are also found to be related to the growth, transmission and viability of cancer cells, which increases with the enzyme activity. In the present study we performing computation screening studies of newly designed monoacylglycerol inhibitors which contains carbamate features, these molecules are designed based on previously developed monoacylglycerol carbamate inhibitors
{"title":"Design and Computational Evaluation of New Carbamate Derivatives for the Inhibition of Monoacylglycerol Lipase Enzyme by using Docking","authors":"Abhishek Kashyap, Dimpy Rani, Suresh Kumar, Shailendra Bhatt","doi":"10.25004/ijpsdr.2023.150515","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150515","url":null,"abstract":"Different disorders and physiological process have been found to be associated with monoacylglycerol lipase enzyme in humans, like pain, inflammation, and neurodegenerative diseases also. The enzyme is a 33 KDa in weight and a type of serine hydrolase enzyme in nature. The presence of enzyme has been reported in both central and peripheral nervous systems and has show its importance as a key signalling factor in endocannabinoid signalling network system. The enzyme has also reported as source of free fatty acid provider for the cancer cell and tumor growth and their proliferation. In proliferative cancer cells, increased the monoacylglycerol lipase activity is observed. The growth, migration and survival of cancer cells have also found to be associated with phosphatidic acid, lysophosphatidic acid, sphingosine phosphate and prostaglandin E2, which are act as signalling molecules and are found to be derived from free fatty acid. These are also found to be related to the growth, transmission and viability of cancer cells, which increases with the enzyme activity. In the present study we performing computation screening studies of newly designed monoacylglycerol inhibitors which contains carbamate features, these molecules are designed based on previously developed monoacylglycerol carbamate inhibitors","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150508
Manju Tripathi, V. B. Adsul, E. Khatiwora, V.B Jadhav
The present study was designed to investigate the anthelmintic potential of Amaranthus tricolor Linn plant of the Amaranthaceae family using acetone, ethyl acetate and ethanol as solvents. The extracts were screened for phytochemical constituents and evaluated for their vermicidal activity against adult Eisenia fetida earthworms. All the extracts contained phytochemicals, but comparatively. The acetone extract showed the presence of most of the phytochemicals, while ethanol extract contained fewer phytochemicals. Various concentrations (10–30 mg/mL) of each extract were studied in the bioassay, observing the time of paralysis and death of the earthworms. Albendazole was used as reference standard and normal saline as a control group. All extracts exhibited dose-dependent anthelmintic activity in both the parameters (paralysis and death) and were showing more potency than the standard drug. The acetone extract (30 mg/mL) exhibited the most promising activity, causing paralysis within 5 minutes and death of worms within 13 minutes. The result suggests that the acetone extract of A. tricolor Linn plant may be useful as an anthelmintic. In the present study, the traditional use of this leafy vegetable as vermicides was proved scientifically and suggests that A. tricolor Linn plant leaves are valuable source of active compounds possessing anthelmintic activity. The preliminary phytochemical evaluation suggests the strong presence of glycosidic and phenolic substances in acetone extract may be responsible for its exceptional vermicidal activity. A further investigation is sought to isolate and develop novel anthelmintic drug present in the plant. The data were verified as statistically significant using one-way ANOVA at 5 % significance level (p < 0.05, n = 3).
本研究旨在以丙酮、乙酸乙酯和乙醇为溶剂，研究苋科植物三色苋的驱虫潜力。对提取物中的植物化学成分进行了筛选，并评估了其对费氏伊蚊成虫的杀虫活性。所有提取物都含有植物化学成分，但含量相对较低。丙酮提取物中含有大部分植物化学成分，而乙醇提取物中含有较少的植物化学成分。在生物测定中研究了每种提取物的不同浓度（10-30 毫克/毫升），观察蚯蚓瘫痪和死亡的时间。阿苯达唑作为参考标准，生理盐水作为对照组。所有提取物在两个参数（瘫痪和死亡）上都表现出剂量依赖性的驱虫活性，并且比标准药物更有效。丙酮提取物（30 毫克/毫升）表现出最有希望的活性，可在 5 分钟内导致蠕虫瘫痪，13 分钟内导致蠕虫死亡。结果表明，A. tricolor Linn 植物的丙酮提取物可用作驱虫药。在本研究中，这种叶菜作为杀虫药的传统用途得到了科学证明，并表明 A. tricolor Linn 植物叶片是具有驱虫活性的活性化合物的宝贵来源。初步植物化学评估表明，丙酮提取物中含有大量糖苷和酚类物质，这可能是其具有特殊杀虫活性的原因。进一步的研究旨在分离和开发该植物中的新型驱虫药。在 5 % 的显著性水平（p < 0.05，n = 3）下，使用单向方差分析验证了数据的统计学意义。
{"title":"In-vitro Anthelmintic Potential of Leaf Extracts of Amaranthus tricolor Linn.","authors":"Manju Tripathi, V. B. Adsul, E. Khatiwora, V.B Jadhav","doi":"10.25004/ijpsdr.2023.150508","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150508","url":null,"abstract":"The present study was designed to investigate the anthelmintic potential of Amaranthus tricolor Linn plant of the Amaranthaceae family using acetone, ethyl acetate and ethanol as solvents. The extracts were screened for phytochemical constituents and evaluated for their vermicidal activity against adult Eisenia fetida earthworms. All the extracts contained phytochemicals, but comparatively. The acetone extract showed the presence of most of the phytochemicals, while ethanol extract contained fewer phytochemicals. Various concentrations (10–30 mg/mL) of each extract were studied in the bioassay, observing the time of paralysis and death of the earthworms. Albendazole was used as reference standard and normal saline as a control group. All extracts exhibited dose-dependent anthelmintic activity in both the parameters (paralysis and death) and were showing more potency than the standard drug. The acetone extract (30 mg/mL) exhibited the most promising activity, causing paralysis within 5 minutes and death of worms within 13 minutes. The result suggests that the acetone extract of A. tricolor Linn plant may be useful as an anthelmintic. In the present study, the traditional use of this leafy vegetable as vermicides was proved scientifically and suggests that A. tricolor Linn plant leaves are valuable source of active compounds possessing anthelmintic activity. The preliminary phytochemical evaluation suggests the strong presence of glycosidic and phenolic substances in acetone extract may be responsible for its exceptional vermicidal activity. A further investigation is sought to isolate and develop novel anthelmintic drug present in the plant. The data were verified as statistically significant using one-way ANOVA at 5 % significance level (p < 0.05, n = 3).","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316356","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150502
P. C. Pradhan, M. Kori
Aim of present study was to investigate the preliminary screening of aerial part of Corchorus olitorius extracts for anti-inflammatory and wound-healing activity on experimental animals. Different extracts with respective solvents i.e. petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extracts of C. olitorius were obtained by successive solvent extraction. All extracts were screened for anti-inflammatory activity using Xylene-induced ear edema in mice and wound healing effect was studied by using incision wound model in mice. The weight of the ear lobes and biochemical measurements, nitric oxide (NO) levels and MPO in the tissue sample were used to detect the anti-inflammatory effect. The wound healing effect was observed by measurement of tensile strength and protein and hydroxyproline level assessment in the healed tissues. Observations of present study were confirmed that ethanol extract of C. olitorius (EECO) was showed significant (p<0.05) inhibition in the ear edema of mice. NO and MPO activity was decreased significantly in EECO-treated mice. Wound healing potential was observed by significant improvement in tensile strength as well as protein and hydroxyproline level of healed tissue of EECO-treated mice. In conclusion, ethanol extract of C. olitorius was found most effective for anti-inflammatory through reduction of NO and MPO activity as well as wound healing potential in experimental mice.
本研究的目的是初步筛选欧石蒜气生部分提取物对实验动物的抗炎和伤口愈合活性。通过连续溶剂萃取法获得了不同的提取物和相应的溶剂，即石油醚、氯仿、乙酸乙酯、乙醇和水提取物。利用二甲苯诱导的小鼠耳部水肿对所有提取物进行了抗炎活性筛选，并利用小鼠切口模型研究了其伤口愈合效果。耳叶重量和生化指标、一氧化氮（NO）水平和组织样本中的 MPO 被用来检测抗炎效果。通过测量愈合组织的拉伸强度、蛋白质和羟脯氨酸水平评估，观察伤口愈合效果。本研究的观察结果表明，蛇床子乙醇提取物（EECO）对小鼠耳部水肿有显著的抑制作用（p<0.05）。经 EECO 处理的小鼠体内 NO 和 MPO 活性明显降低。经 EECO 处理的小鼠愈合组织的抗张强度、蛋白质和羟脯氨酸水平均有明显改善，从而观察到伤口愈合潜力。总之，通过降低小鼠体内的 NO 和 MPO 活性以及伤口愈合潜能，奥利司他的乙醇提取物被认为是最有效的抗炎药物。
{"title":"Preliminary Pharmacological Screening of Corchorus olitorius Extracts for Anti-inflammatory and Wound Healing Activity","authors":"P. C. Pradhan, M. Kori","doi":"10.25004/ijpsdr.2023.150502","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150502","url":null,"abstract":"Aim of present study was to investigate the preliminary screening of aerial part of Corchorus olitorius extracts for anti-inflammatory and wound-healing activity on experimental animals. Different extracts with respective solvents i.e. petroleum ether, chloroform, ethyl acetate, ethanol and aqueous extracts of C. olitorius were obtained by successive solvent extraction. All extracts were screened for anti-inflammatory activity using Xylene-induced ear edema in mice and wound healing effect was studied by using incision wound model in mice. The weight of the ear lobes and biochemical measurements, nitric oxide (NO) levels and MPO in the tissue sample were used to detect the anti-inflammatory effect. The wound healing effect was observed by measurement of tensile strength and protein and hydroxyproline level assessment in the healed tissues. Observations of present study were confirmed that ethanol extract of C. olitorius (EECO) was showed significant (p<0.05) inhibition in the ear edema of mice. NO and MPO activity was decreased significantly in EECO-treated mice. Wound healing potential was observed by significant improvement in tensile strength as well as protein and hydroxyproline level of healed tissue of EECO-treated mice. In conclusion, ethanol extract of C. olitorius was found most effective for anti-inflammatory through reduction of NO and MPO activity as well as wound healing potential in experimental mice.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316023","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-20DOI: 10.25004/ijpsdr.2023.150506
Fahad T Saleh, Abdul Ahad, Prashant D. Netankar, A. A. Sheikh, S. U. Asema
Quinoline scaffolds have gained substantial interest in the modern era of medicinal chemistry due to their wide range of biological applications. The present work reported the synthesis of various oxime derivatives of quinolines by the reaction of substituted 2-chloro-3-formyl-quinolines with hydroxyl amine hydrochloride. The reaction was mediated by aqueous ethanol, whereas hexamine was used as an efficient, non-toxic and easily available basic organocatalyst. The developed protocol has various advantages, including operational ease, affordability, an eco-friendly approach, and short reaction time. Moreover, the synthesized compounds were subjected to in-vitro antimicrobial activities. The antimicrobial evaluation of almost all the compounds found to be potent and effective. Compounds 4c, 4d, and 4f showed a broad spectrum of inhibition and were more effective when tested against specific Gram (-) and Gram (+) bacteria. In in-vitro antifungal evaluation, all synthesized compounds (4a-4g) showed good sensitivity against the tested fungal cultures except Aspergillus niger
{"title":"Synthesis of Some Quinoline Oximes by an Efficient Method and their Biological Screening","authors":"Fahad T Saleh, Abdul Ahad, Prashant D. Netankar, A. A. Sheikh, S. U. Asema","doi":"10.25004/ijpsdr.2023.150506","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150506","url":null,"abstract":"Quinoline scaffolds have gained substantial interest in the modern era of medicinal chemistry due to their wide range of biological applications. The present work reported the synthesis of various oxime derivatives of quinolines by the reaction of substituted 2-chloro-3-formyl-quinolines with hydroxyl amine hydrochloride. The reaction was mediated by aqueous ethanol, whereas hexamine was used as an efficient, non-toxic and easily available basic organocatalyst. The developed protocol has various advantages, including operational ease, affordability, an eco-friendly approach, and short reaction time. Moreover, the synthesized compounds were subjected to in-vitro antimicrobial activities. The antimicrobial evaluation of almost all the compounds found to be potent and effective. Compounds 4c, 4d, and 4f showed a broad spectrum of inhibition and were more effective when tested against specific Gram (-) and Gram (+) bacteria. In in-vitro antifungal evaluation, all synthesized compounds (4a-4g) showed good sensitivity against the tested fungal cultures except Aspergillus niger","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139316318","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-25DOI: 10.25004/ijpsdr.2023.150414
Sreelatha Kamera, Vishnu K Sharma, Srivani M, A. Garlapati
A series of novel 3-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-5H-[1,2,4]triazino[5,6-b]indole derivatives (3a-3j) were synthesized by reacting different substituted 5H-[1,2,4]triazino[5,6-b]indole-3-thiols with substituted (2-chloromethyl)-1H-benzo(d)imidazoles in the presence of KOH and water in good yields. The structures of the newly synthesized compounds were confirmed by spectroscopic techniques such as 1H-NMR, 13C-NMR, IR and mass spectrometry. The in-vitro antitubercular activity of the synthesized compounds was evaluated against Mycobacterium tuberculosis (Mtb) H37Rv (ATCC 27294) using MABA (Microplate Alamar Blue Assay) method. Compounds 3b, 3c, and 3i showed good antitubercular activity against Mtb with MIC value of 6.25 ± 0.00 μg/mL. Also, the in-vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using the two-fold serial dilution technique and most of the compounds exhibited moderate activities with MIC values in the range of 63.33 ± 1.44 to >500 ????g/mL against the tested microorganisms. The compounds (3a-3j) were also tested for their in-vitro antioxidant activities by DPPH radical scavenging activity method and among the series, compounds 3e, 3a, and 3g exhibited strong antioxidant activity with IC50 values of 10.85 ± 0.05, 12.18 ± 0.13 and 12.57 ± 0.17????g/mL respectively compared to the standard ascorbic acid (IC50 value, 5.85 ± 0.04 ????g/mL). Further, molecular docking studies were performed to investigate the binding affinities as well as the interaction of these compounds with Mtb InhA target protein. In-silico ADME predictions showed that all the synthesized compounds have drug-like properties and exhibited good oral bioavailability.
{"title":"Design, Synthesis, Molecular Docking, Antitubercular, Antimicrobial and Antioxidant Studies of Some Novel 3-(((1H-Benzo[d]imidazol-2- yl)methyl)thio)-5H-[1,2,4] Triazino[5,6-b]indole Derivatives","authors":"Sreelatha Kamera, Vishnu K Sharma, Srivani M, A. Garlapati","doi":"10.25004/ijpsdr.2023.150414","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150414","url":null,"abstract":"A series of novel 3-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-5H-[1,2,4]triazino[5,6-b]indole derivatives (3a-3j) were synthesized by reacting different substituted 5H-[1,2,4]triazino[5,6-b]indole-3-thiols with substituted (2-chloromethyl)-1H-benzo(d)imidazoles in the presence of KOH and water in good yields. The structures of the newly synthesized compounds were confirmed by spectroscopic techniques such as 1H-NMR, 13C-NMR, IR and mass spectrometry. The in-vitro antitubercular activity of the synthesized compounds was evaluated against Mycobacterium tuberculosis (Mtb) H37Rv (ATCC 27294) using MABA (Microplate Alamar Blue Assay) method. Compounds 3b, 3c, and 3i showed good antitubercular activity against Mtb with MIC value of 6.25 ± 0.00 μg/mL. Also, the in-vitro antimicrobial activities of the compounds were evaluated against various bacterial and fungal strains using the two-fold serial dilution technique and most of the compounds exhibited moderate activities with MIC values in the range of 63.33 ± 1.44 to >500 ????g/mL against the tested microorganisms. The compounds (3a-3j) were also tested for their in-vitro antioxidant activities by DPPH radical scavenging activity method and among the series, compounds 3e, 3a, and 3g exhibited strong antioxidant activity with IC50 values of 10.85 ± 0.05, 12.18 ± 0.13 and 12.57 ± 0.17????g/mL respectively compared to the standard ascorbic acid (IC50 value, 5.85 ± 0.04 ????g/mL). Further, molecular docking studies were performed to investigate the binding affinities as well as the interaction of these compounds with Mtb InhA target protein. In-silico ADME predictions showed that all the synthesized compounds have drug-like properties and exhibited good oral bioavailability.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139348994","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-25DOI: 10.25004/ijpsdr.2023.150410
Ajinza A Azeez, A. A. Rauf, B. T. Edwin
Vitex altissima has been conventionally utilized for its wide-ranging properties in the management of oxidative stress and inflammation. The present investigation was centered on the quantification of the anti-inflammatory efficacy of V. altissima. The samples were evaluated for their ability to impede the activity of proteinase, denature proteins, and stabilize the membrane of human red blood cells (HRBC). The present study investigated the inhibitory impact of extracts on the production of total cyclooxygenase, lipoxygenase-5 (5-LOX), myeloperoxidase (MPO), and nitric oxide (NO) using the RAW 264.7 cell line. Furthermore, the antioxidant properties were assessed through the employment of both DPPH assay and reducing power assay. According to the findings, the methanolic extract of V. altissima (VAME) was identified as the most efficacious fraction with anti-inflammatory and antioxidant properties. The findings indicate that the extracts exhibited dose-dependent inhibition of proteinase, protein denaturation, and hemolysis of HRBC membrane, which is beneficial. The extracts of V. altissima, when treated at concentrations that are not cytotoxic, were observed to have a significant effect in reducing the activity of COX, 5-LOX, and MPO in RAW 264.7 cell line treated with LPS. This resulted in a decrease in NO levels. The dose-dependent increase in in vitro anti-inflammatory activity of V. altissima suggests its potential use as a pharmacological agent for the management of diseases related to inflammation. Additional comprehensive phytochemical investigations, in conjunction with in vitro and in vivo analyses, are necessary to identify the active constituent within the extract.
传统上，人们利用荆芥的广泛特性来控制氧化应激和炎症。本研究的重点是对海荆的抗炎功效进行量化。对样品阻碍蛋白酶活性、使蛋白质变性和稳定人红细胞（HRBC）膜的能力进行了评估。本研究使用 RAW 264.7 细胞系研究了提取物对总环氧化酶、脂氧合酶-5（5-LOX）、髓过氧化物酶（MPO）和一氧化氮（NO）产生的抑制作用。此外，还通过 DPPH 法和还原力法对抗氧化特性进行了评估。研究结果表明，V. altissima 的甲醇提取物（VAME）是抗炎和抗氧化性最强的部分。研究结果表明，萃取物对蛋白酶、蛋白质变性和 HRBC 膜溶血具有剂量依赖性抑制作用，对人体有益。当 V. altissima 的萃取物以不具有细胞毒性的浓度处理时，观察到其对降低用 LPS 处理的 RAW 264.7 细胞系中 COX、5-LOX 和 MPO 的活性有显著效果。这导致了 NO 水平的下降。V. altissima 的体外抗炎活性呈剂量依赖性增加，这表明它有可能作为一种药剂用于治疗与炎症有关的疾病。有必要结合体外和体内分析进行更全面的植物化学研究，以确定提取物中的活性成分。
{"title":"ANTI-INFLAMMATORY EFFECTS OF VITEX ALTISSIMA LEAF EXTRACT IN LIPOPOLYSACCHARIDE-INDUCED RAW 264.7 MACROPHAGES.","authors":"Ajinza A Azeez, A. A. Rauf, B. T. Edwin","doi":"10.25004/ijpsdr.2023.150410","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150410","url":null,"abstract":"Vitex altissima has been conventionally utilized for its wide-ranging properties in the management of oxidative stress and inflammation. The present investigation was centered on the quantification of the anti-inflammatory efficacy of V. altissima. The samples were evaluated for their ability to impede the activity of proteinase, denature proteins, and stabilize the membrane of human red blood cells (HRBC). The present study investigated the inhibitory impact of extracts on the production of total cyclooxygenase, lipoxygenase-5 (5-LOX), myeloperoxidase (MPO), and nitric oxide (NO) using the RAW 264.7 cell line. Furthermore, the antioxidant properties were assessed through the employment of both DPPH assay and reducing power assay. According to the findings, the methanolic extract of V. altissima (VAME) was identified as the most efficacious fraction with anti-inflammatory and antioxidant properties. The findings indicate that the extracts exhibited dose-dependent inhibition of proteinase, protein denaturation, and hemolysis of HRBC membrane, which is beneficial. The extracts of V. altissima, when treated at concentrations that are not cytotoxic, were observed to have a significant effect in reducing the activity of COX, 5-LOX, and MPO in RAW 264.7 cell line treated with LPS. This resulted in a decrease in NO levels. The dose-dependent increase in in vitro anti-inflammatory activity of V. altissima suggests its potential use as a pharmacological agent for the management of diseases related to inflammation. Additional comprehensive phytochemical investigations, in conjunction with in vitro and in vivo analyses, are necessary to identify the active constituent within the extract.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139349071","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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