International Journal of Pharmaceutical Sciences and Drug Research最新文献_第3页

A Stability Indicating Reverse Phase High Performance Liquid Chromatography Method for Related Substances of Sofosbuvir in Tablet Dosage Form 片剂索非布韦相关物质的稳定性指示反相高效液相色谱法

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150501

Binal N Patel, Hitesh J Vekaria

{"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":"55 1","pages":""},"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}

引用次数: 0

Ameliorating Effect of Capparis aphylla Roth. in Adjuvant-induced Arthritis in rats with Reference to Changes in Reactants RF, CRP, Radiological Erosions Capparis aphylla Roth.对佐剂诱发的大鼠关节炎的改善作用，以及反应物 RF、CRP 和放射性侵蚀的变化

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150503

Sainika H Kanzaria, T. Gandhi, K. Patel

{"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":"5 1","pages":""},"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}

引用次数: 0

Evaluation of Myricetin loaded Nanoemulsion Formulation for the Management of Diabetic Wound Healing in Experimental Animals 评估含 Myricetin 的纳米乳剂配方对实验动物糖尿病伤口愈合的管理作用

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150507

Tanvir Y. Shaikh, S. Lodhi

{"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":"42 1","pages":""},"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}

引用次数: 0

Acute Intermittent Hypoxia Therapy alters Cognitive Behavioral Parameters in Wistar Albino Rats 急性间歇性缺氧疗法会改变 Wistar 白化大鼠的认知行为参数

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150512

S. Roshan, Dharani Gunaseelan, Sherin Benazsir, Nithya Pandian, Swaminathan K. Jayachandran, Mahesh Kandasmy, Anusuyadevi Muthuswamy

{"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":"15 1","pages":""},"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}

引用次数: 0

Design and Computational Evaluation of New Carbamate Derivatives for the Inhibition of Monoacylglycerol Lipase Enzyme by using Docking 利用 Docking 设计和计算评估用于抑制单酰基甘油脂肪酶的新型氨基甲酸酯衍生物

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150515

Abhishek Kashyap, Dimpy Rani, Suresh Kumar, Shailendra Bhatt

{"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":"72 1","pages":""},"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}

引用次数: 0

In-vitro Anthelmintic Potential of Leaf Extracts of Amaranthus tricolor Linn. 三色苋叶提取物的体外驱虫潜力

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150508

Manju Tripathi, V. B. Adsul, E. Khatiwora, V.B Jadhav

{"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":"18 1","pages":""},"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}

引用次数: 0

Preliminary Pharmacological Screening of Corchorus olitorius Extracts for Anti-inflammatory and Wound Healing Activity 欧石蒜提取物抗炎和伤口愈合活性的初步药理筛选

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150502

P. C. Pradhan, M. Kori

{"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":"1 1","pages":""},"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}

引用次数: 0

Synthesis of Some Quinoline Oximes by an Efficient Method and their Biological Screening 用高效方法合成一些喹啉肟并对其进行生物学筛选

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-10-20 DOI: 10.25004/ijpsdr.2023.150506

Fahad T Saleh, Abdul Ahad, Prashant D. Netankar, A. A. Sheikh, S. U. Asema

{"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":"245 1","pages":""},"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}

引用次数: 0

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 一些新型 3-(((1H-苯并[d]咪唑-2-基)甲基)硫)-5H-[1,2,4] 三嗪并[5,6-b]吲哚衍生物的设计、合成、分子对接、抗结核、抗菌和抗氧化研究

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-08-25 DOI: 10.25004/ijpsdr.2023.150414

Sreelatha Kamera, Vishnu K Sharma, Srivani M, A. Garlapati

{"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":"65 1","pages":""},"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}

引用次数: 0

ANTI-INFLAMMATORY EFFECTS OF VITEX ALTISSIMA LEAF EXTRACT IN LIPOPOLYSACCHARIDE-INDUCED RAW 264.7 MACROPHAGES. 海荆叶提取物对脂多糖诱导的生264.7巨噬细胞的抗炎作用。

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2023-08-25 DOI: 10.25004/ijpsdr.2023.150410

Ajinza A Azeez, A. A. Rauf, B. T. Edwin

{"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":"19 1","pages":""},"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}

引用次数: 0