{"title":"Green Synthesis, Characterization, In Silico ADMET Profiling, Molecular Docking Studies of 3, 4-Dihydropyrimidin-2-(1H)-ones Against Voltage-Gated Calcium Channel (4MS2) Receptor","authors":"","doi":"10.33140/jpr.07.01.07","DOIUrl":"https://doi.org/10.33140/jpr.07.01.07","url":null,"abstract":"The present work involves design, synthesis and evaluation of derivatives of 3,4-dihydropyrimidine 2 one. Using pyrimdine as a core structure for design of novel pyrimidine derivatives which are calcium channel blocker, Derivatives of 3,4-dihydropyrinidine-2-one was synthesized by microwave assisted synthesis method. There are ten derivatives are synthesized by microwave assisted synthesis in laboratory. The entire synthesized compound was tested using Insilco parameters like Pass online data, SwissADME parameters and toxicity parameters by using protox II. All the synthesized compound tested by pass online software for its biological activity. All the synthesized compounds reflelects various activities like antihypertensive, antianginal, antiviral, antifungal and all of them are calcium channel blockers.","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42151027","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}
{"title":"Investigation of Solvent Efficiency in Extraction of Bioactive Constituents from Peels, Leaves and Tubers of Sweet Potato","authors":"","doi":"10.33140/jpr.07.01.08","DOIUrl":"https://doi.org/10.33140/jpr.07.01.08","url":null,"abstract":"The effectiveness of solvents in extracting phytochemicals from leaves, peels and tubers of sweet potato was studied with a view of knowing the best solvent for extraction as well as establishing the availability of bioactive constituents in different parts of sweet potato. The peels, leaves and tubers of sweet potato were obtained, cut, air-dried, ground, sieved with 40 mm mesh and separately extracted using six different solvents (acetone, ethyl acetate, methanol, ethanol, water and chloroform) at ratio 1:10 for 72 h. The extracts obtained using six different solvents on peels, leaves and tubers of sweet potato were screened for phytochemicals. It was observed that all the three parts of sweet potato considered were rich in phytochemicals, although the peels and tubers contained relatively higher bioactive constituents than that available in the leaves. The extraction efficiency of the solvents in obtaining bioactive constituents from leaves, peels and tubers of sweet potato is highest in ethanol, followed by methanol, acetone and ethyl acetate while the least were in chloroform and water.","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44169999","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}
Zeliha Keskin Alkaç, D. A. Özek, H. Yüce, Fatih Ahmet Korkak, Sumeyye Aslan, N. Türkmen, S. Ünüvar
{"title":"Pharmacokinetic Interaction of Favipiravir with Citalopram and Pioglitazone","authors":"Zeliha Keskin Alkaç, D. A. Özek, H. Yüce, Fatih Ahmet Korkak, Sumeyye Aslan, N. Türkmen, S. Ünüvar","doi":"10.18579/jopcr/v21i4.28","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.28","url":null,"abstract":"The current study's objective was to investigate the interactions of favipiravir with pioglitazone and citalopram. 25 Spraque-Dawley female rats were used in the study. Rats in groups 1 and 4 were given pioglitazone (1 mg/kg/day) for 7 days and rats in groups 2 and 5 were given citalopram (1.5 mg/kg/day) for 7 days. Rats in groups 3, 4, and 5 were given a loading dose (50 mg/kg) on the 6th day of the study and a maintenance dose of favipiravir (30 mg/kg) on the 7th day of the study. After the last drug administration, blood samples were taken from the rats at 15, 30, and 45 minutes, and 1, 2, 4, 6, and 8 hours. Plasma concentrations of drugs were determined by high-performance liquid chromatography (HPLC). The aldehyde oxidase (AO) and xanthine oxidase (XO) activities in liver tissues were determined by enzyme-linked immunosorbent assay (ELISA). Pioglitazone changed the pharmacokinetics of favipiravir and increased t1/2, AUC, MRT and Cl values. Favipiravir did not affect the pharmacokinetics of pioglitazone at a steady state. When used together, favipiravir significantly decreased Cl while increasing citalopram's t1/2, AUC, and MRT values. While citalopram increased the t1/2, Cmax, AUMC, and Cl values of favipiravir, it decreasing the AUC value. Pharmacokinetic drug interactions have been determined between favipiravir and AO substrates or modulators. It is thought that if the results obtained are supported by human studies, it will guide the concomitant use of these drugs in the clinic to prevent the occurrence of adverse reactions. Keywords: Drug-drug interaction, Favipiravir, Pioglitazone, Citalopram, Aldehyde oxidase","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48919253","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}
{"title":"Levo Cetirizine - the Drug with Numerous Plus to Cure Allergic Syndrome Compared to other Treatment Systems","authors":"K. Upasana, Saini Sunil, Bharkatiya Meenakshi","doi":"10.18579/jopcr/v21i4.ms221204","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.ms221204","url":null,"abstract":"Many drugs are available to treat allergic condition. This review focused on why antihistaminics are best choice for treatment of allergic disorder especially allergic rhinitis (AR). AR is a chronic inflammatory disease. AR can be detected by its characteristics of nasal congestion, nasal itching, sneezing, rhinorrhoea, pruritis, redness, tearing and itching of eyes. This is very common and increases day after day. Allergic rhinitis is not lethal but interferes with daily schedule in a sustained manner. It is also observed that after COVID-19, stimuli reactions such as allergic condition, breathing difficulties and nasal irritation are quite common. It is very necessary to treat AR with an effective and powerful medicine because nowadays, many factors trigger these responses such as the environment, food products, pollution, etc. Before treatment of any symptoms it is very necessary to know it pathogenesis. Hence, in this review, we discuss the introduction of AR, its pathogenesis, diagnostics, classification and treatment. We also understand why levocetirizine, a third-generation antihistamine, is superior to all other antihistamines and the most favourable in paediatric patients in many ways. Keywords: Allergic rhinitis, Antihistaminic, Levocetirizine, COVID19, Asthma, Nasal congestion","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42845743","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}
Menavath Tulasi Naik Ram, Sai Kushal Gunturu, A. Shaik, Yadlapalli Jaya Prasanth Babu, Sardena Siyonu Kumari
{"title":"Studies of Antibacterial Activity of the Seed Extract of Solanum surattense Burm. F .","authors":"Menavath Tulasi Naik Ram, Sai Kushal Gunturu, A. Shaik, Yadlapalli Jaya Prasanth Babu, Sardena Siyonu Kumari","doi":"10.18579/jopcr/v21i4.22.24","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.22.24","url":null,"abstract":"Crude Flavonoids extracted from crushed seeds of dried ripe fruits of Solanum surattense Burm F. were screened for antimicrobial activity against two bacteria – Streptococcus mutans and Aggregatibacter actinomycetemcomitans – which were found to be major contributers for occurrence of Dental caries. Minimum inhibitory concentration, Minimum bactericidal concentration, and Time Kill curve of the extract against each sensitive test pathogen, were evaluated. The flavonoid extract showed good antimicrobial activity against Streptococcus mutans than towards Aggregatibacter actinomycetemcomitans. MIC & MBC of Streptococcus mutans is 25µg/mL & 25µg/mL respectively. MIC & MBC of Aggregatibacter actinomycetemcomitans is 50µg/mL & 50µg/mL respectively. Time Kill Curve of Streptococcus mutans and Aggregatibacter actinomycetemcomitans was 2hr and 2hr respectively. Keywords: Solanum surattense, Streptococcus mutans, Aggregatibacter actinomycetemcomitans, Minimum inhibitory concentration, Minimum bactericidal concentration, Time kill curve","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44360093","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}
{"title":"Development and Validation of Stability Indicating RP-HPLC Method for the Simultaneous Determination of Cabotegravir and Rilpivirine in Bulk and Injection Dosage Form","authors":"A. Suneetha, M. Lakshmi, K. Jyothi, B. Priyanka","doi":"10.18579/jopcr/v21i4.22.15","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.22.15","url":null,"abstract":"A simple, sensitive, specific, accurate, and stability-indicating reversed phase high performance liquid chromatographic method was developed for the simultaneous determination of cabotegravir and rilpivirine in injection dosage form, using a Waters Model No.2695 series compact system fitted with Agilent - C18 column (BDS) (150 X 4.6 mm, 5μm) and a mobile phase composed of 0.01N KH2PO4 buffer (pH: 4.8): acetonitrile (70:30v/v). The 260 nm wavelength was chosen. The retention times of cabotegravir and rilpivirine were found to be 2.30 and 3.187 minutes, respectively. Linearity was established for cabotegravir and rilpivirine in the range of 25-150 µg/mL and 37.5-225µg/mL respectively: with correlation coefficient (r2) of 0.9999 for both the drugs. Cabotegravir and rilpivirine were found to have %RSDs of 0.4 and 0.3 respectively, for system precision. The proposed methods intra- and inter-day precision assessments showed a relative standard deviation (%RSD) below the maximum permitted level of 2.0. Accuracy was carried out in triplicate, and the percentage recovery was 100.25% for cabotegravir and 99.79% for rilpivirine, respectively. The limit of detection and limit of quantification for cabotegravir were found to be 0.24 and 0.74 μg/mL, respectively and 1.10 and 3.34 μg/mL, for rilpivirine respectively. Both medications were put to a range of stress conditions, including thermal, acidic, basic, oxidative, and photolytic stress. The findings demonstrated that, with the exception of heat, UV, and neutral environments, considerable degradation was found in acidic, basic, and oxidative conditions where a good separation of drug peaks was seen in the presence of the degradation products. As a result, this technique can be used to quantitatively to analyze cabotegravir and rilpivirine in bulk drug and injection dosage forms. Keywords: Cabotegravir, RP HPLC, Rilpivirine, ICH guidelines","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48771030","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}
P. Patel, Hiren Patel, Hiren Bhagiya, Bhavisha Kacha, Austin Christian
{"title":"Type-2 Diabetes Mellitus: A Review of Current Trends","authors":"P. Patel, Hiren Patel, Hiren Bhagiya, Bhavisha Kacha, Austin Christian","doi":"10.18579/jopcr/v21i4.22.21","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.22.21","url":null,"abstract":"Diabetes mellitus type 2 is a chronic metabolic condition whose incidence has been continuously growing around the world. As a result of this tendency, it is quickly becoming an epidemic in some parts of the world, with the number of individuals affected anticipated to double in the next decade as the world's population ages, adding to the already existing load on healthcare providers, particularly in poor developing countries. World Health Organization (WHO) guidelines are still used for screening and diagnosis, which include both clinical and laboratory characteristics. There is currently no cure for the disease; however, therapy options include lifestyle changes, obesity management, oral hypoglycemic medications, and insulin sensitizers such as metformin, a biguanide that reduces insulin resistance which is used as first line medication especially for obese patients. The traditional herbal medicine like garlic, neem, bitter gourd, aloe vera, onion, methi, amla, jamun, baheda etc. are also used for the treatment of the diabetes. Other effective medication includes non-sulfonylurea secretagogues, thiazolidinediones, alpha glucoside inhibitors, and insulin. Recent research into the biology of type 2 diabetes has led to the development of new medications such as glucagon-like peptide 1 analogues: dipeptidyl peptidase inhibitors, sodium glucose cotransporter 2 inhibitors, and 11-hydroxysteroid dehydrogenase 1 inhibitors, insulin releasing glucokinase activators. The novel drug delivery improves the treatment of diabetes by the inhaled insulin. Keywords: Type 2 diabetes mellitus, Diabetes complications, Diabetes diagnosis, Diabetes management, Antidiabetic newer drugs, Antidiabetic herbal drugs","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46380150","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}
Enwa Felix Oghenemaro, Jemikalajah Daniel Johnson, Oyubu L Obaro, A. Collins, Ukah Faith Erezi
{"title":"In-Vitro Evaluation of the Antibacterial Activity of the Methanol Leave Extract of Lawsonia Inermis Against Methicillin-Resistant Staphylococcus Aureus (MRSA)","authors":"Enwa Felix Oghenemaro, Jemikalajah Daniel Johnson, Oyubu L Obaro, A. Collins, Ukah Faith Erezi","doi":"10.18579/jopcr/v21i4.22.27","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.22.27","url":null,"abstract":"This study is to determine the antibacterial efficacy of Lawsonia inermis against methicillin-resistant Staphylococcus aureus (MRSA) which has become a leading cause of infections. The leaves of Lawsonia inermis also known as Henna or lalley leave were subjected to extraction with seventy percent (70%) methanol using the cold maceration technique after which phytochemical screening and partitioning were carried out following standard procedures, hence, three fractions of the methanol extract of Lawsonia inermis (crude extract, aqueous and chloroform fractions) were used against thirty strains of MRSA by using the agar well-diffusion and minimum inhibitory concentration as a determination method. Preliminary phytochemical screening revealed the presence of Alkaloids, Saponins, Tannins, Terpnoids, and steroids. A two old serial dilution was done for each of the fractions viz; 100mg/ml, 50mg/ml, 25mg/ml, 12.5mg/ml and 6.25mg/ml. The various dilutions were used on the test organism and there was increase in zones of inhibitions with increase in extract concentrations. At 100mg/ml, the crude fraction had a maximum inhibition zone of 15.30mm which was higher than the inhibition zone of the standard antibiotic used, and a minimum inhibition zone of 9 mm as compared to the standard antibiotic used having a minimum inhibition zone of 4.33mm. Among all the fractions used, the crude fraction of the methanol extract of Lawsonia inermis showed the best activity against the test organism (MRSA) Methicilin Resistant Staphylococcus aureus. Others showed lesser activity as compared to the standard antibiotic used. Keywords: Lawsonia inermis linn, MRSA, Crude extract","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42268919","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}
S. Y. Sabo, J. Gotep, Naandong Faith Bako, S. Otimenyin
{"title":"Androgenic and Spermatogenic Effects of Methanolic Root Extract of Waltheria indica (linn) in Male Wistar Rats","authors":"S. Y. Sabo, J. Gotep, Naandong Faith Bako, S. Otimenyin","doi":"10.18579/jopcr/v21i4.22.25","DOIUrl":"https://doi.org/10.18579/jopcr/v21i4.22.25","url":null,"abstract":"Waltheria indica is a common shrub found in many parts of Northern Nigeria for the management of several diseases. Although the ability of Waltheria indica to treat infertility, erectile dysfunction and impotency in male has been reported in ethno-medicine, there is no scientific study to verify its action on androgens and spermatogenic parameters. This study seeks to evaluate the effect of methanolic root extract of Waltheria indica on androgens and spermatogenesis in albino rats. Rats were grouped into four: 1, 2, 3 and 4 where 1(the control) received orally 1mL of normal saline. Groups 2, 3 and 4 received orally on daily basis, graded doses of 50, 100 and 200 mg/kg body weight of the plant extract, respectively, for 40 days. Administration of plant extract resulted in enhanced levels of testosterone, follicular stimulating hormone, luteinizing hormone, sperm count, sperm viability, and sperm mobility, testicular gamma glutamyl transferase, testicular alkaline phosphatase, testicular acid phosphatase and testicular cholesterol. The results show that methanolic root extract of Waltheria indica has demonstrated androgenic and spermatogenic activity which further substantiates its claimed traditional use in the management of infertility in male folk. Keywords: Waltheria indica root extract, infertility, erectile dysfunction, impotency in male, androgenic effect, spermatogenic effect","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42643535","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}
{"title":"ULK1/2 Inhibitor: Essential Component of Autophagic Cell Death Machinery","authors":"P. Sidat, M. Noolvi, Rahul Patil, Sanket Rathod","doi":"10.18579/jopcr/v21i3.4","DOIUrl":"https://doi.org/10.18579/jopcr/v21i3.4","url":null,"abstract":"","PeriodicalId":16706,"journal":{"name":"Journal of Pharmaceutical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45205850","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}