{"title":"Percepción de los medicamentos genéricos en pobladores en un distrito del Perú","authors":"Ambrocio Teodoro Esteves Pairazaman, José Rincón Chávez, Consuelo Berta Horna Sandoval, Flor Lidia Bustamante Fustamante, Yolanda Ruiz Vargas","doi":"10.56499/jppres23.1658_11.6.1114","DOIUrl":"https://doi.org/10.56499/jppres23.1658_11.6.1114","url":null,"abstract":"Context: In the Peruvian context, generic drugs are those pharmaceutical products whose names correspond to the active ingredient of the drug and are not identified by a brand name; brand name drugs, on the other hand, are pharmaceutical products whose names are determined by the drug manufacturer. Aims: To know the perception of generic drugs by a Peruvian population. Methods: The type of research was applied, deductive method, non-experimental design, quantitative approach and cross-sectional. The sample consisted of 218 inhabitants, who were submitted to a questionnaire where the study variable was measured. Results: The main results showed that the level of information on generic drugs among the study sample was low (74,3%), as was consumption (66,5%), the level of confidence in these drugs was low (64,7%) and, finally, the inhabitants indicated that they had little access to generic drugs in their area (68,8%). Conclusions: The general perception of the study population towards generic drugs was low.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135216651","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":"Analysis of factors affecting enoxaparin effectiveness on coagulation, inflammation, and clinical outcomes in patients with COVID-19","authors":"Budi Suprapti, Liana Debora, Rifdah Atikah Safitri, Dewi Kusumawati, Arina Dery Puspitasari","doi":"10.56499/jppres23.1683_11.6.1106","DOIUrl":"https://doi.org/10.56499/jppres23.1683_11.6.1106","url":null,"abstract":"Context: Hypercoagulopathy is a COVID-19 extra-pulmonary manifestation has drawn the attention of the scientists due to its risk of thromboembolism. Enoxaparin is an anticoagulant used to prevent hypercoagulopathy. Many factors have been associated with enoxaparin effectiveness. Aims: To analyze factors affecting enoxaparin effectiveness on coagulation, inflammation, and clinical outcomes. Methods: This retrospective cohort study involved hospitalized adult patients with COVID-19 from November 2020 to April 2021. Patients’ age, gender, body mass index (BMI), comorbidity, and laboratory results were extracted from medical records. Factors influencing enoxaparin efficacy on coagulation, inflammation, and clinical outcomes were analyzed using path analysis with SmartPLS 3.0 software. D-dimer and platelet values was determined as coagulation outcomes and C-reactive protein (CRP) value as an inflammation outcome. Clinical outcomes comprised of mortality, ventilator usage, and length of stay. Results: A total of 269 patients fulfilled the inclusion criteria. Most of the subjects were male (58%), 66% had comorbidities, 48.3% were aged ≥60 years old, and 65.8% had a BMI ≥ 25 kg/m2. Path analysis showed that age, BMI, and comorbidity affected disease severity (p<0.05). Disease severity strongly influenced enoxaparin dosage (p=0.000). Dosage affected platelet value, ventilator usage, and mortality (p<0.05). Gender did not influence disease severity, and dosage displayed no significant effect on length of stay, CRP, and D-dimer (p>0.05). Conclusions: Dosage is the main factor influencing enoxaparin efficacy on coagulation, inflammation, and clinical outcomes. The dosage is strongly affected by disease severity, in which is predominantly influenced by age, BMI, and comorbidity.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135161537","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}
Ermin Rachmawati, Mohammad S. Rohman, Nashi Widodo, Mifetika Lukitasari, Dwi A. Nugroho, Feri E. Hermanto, Mukhamad N. Kholis
{"title":"The analysis of coffee-green tea-turmeric combination against cardiac-metabolic syndrome using metabolite profiling, gene expression, and in silico approach","authors":"Ermin Rachmawati, Mohammad S. Rohman, Nashi Widodo, Mifetika Lukitasari, Dwi A. Nugroho, Feri E. Hermanto, Mukhamad N. Kholis","doi":"10.56499/jppres23.1702_11.6.961","DOIUrl":"https://doi.org/10.56499/jppres23.1702_11.6.961","url":null,"abstract":"Context: The development of functional drinks to inhibit oxidative stress and inflammation as a critical process in inducing heart damage in metabolic syndrome is required. Coffee, tea, and turmeric have all been shown to offer health advantages. Aims: To investigate the effect of coffee, green tea, turmeric extract (ECGTT) against cardiac-metabolic syndrome (MetS). Methods: The secondary metabolites from coffee, green tea, and turmeric were identified using LC-HRMS. Male Sprague–Dawley rats were divided into four groups (n = 4) representing normal, MetS, MetS with ECGTT treatment doses: 300/100/150 mg/BW and 300/100/250 mg/BW group. Upon the end of treatment periods, expression of tumor necrosis factor-alpha (TNFα), interleukin-6 (IL-6), nuclear factor kappa B (NF-κB), NADPH oxidase (NOX2), SERCA2a were measured from the heart. A computational approach including network pharmacology, protein-protein interaction (PPI) network, molecular docking, and dynamic was performed to understand the molecular mechanism of ECGTT against cardiac damage in MetS. Results: Chlorogenic acid (CGA), epigallocatechin gallate (EGCG), and curcumin were identified as the main metabolites in ECGTT. The ECGTT administration decreased the TNFα, IL-6, NF-κB, and NOX2 and increased SERCA2a expression(p<0.05). Moreover, the PPI result suggested that angiotensin II receptor type 1 (AGTR1) was the key regulator of cardiac injury-MetS induced. CGA, EGCG, and curcumin bind to AGTR1 with smaller binding energy than metformin and showed stability of structure and interaction among those metabolites into AGTR1. Conclusions: Coffee, green tea, and turmeric might prevent heart dysfunction in MetS through modulation of oxidative stress and inflammation.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136371345","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}
Angel T. Alvarado, Ana María Muñoz, Roberto O. Ybañez-Julca, Mario Pineda-Pérez, Nesquen Tasayco-Yataco, María R. Bendezú, Jorge A. García, Felipe Surco-Laos, Haydee Chávez, Doris Laos-Anchante, Aura Molina-Cabrera, Carmela Ferreyra-Paredes, Nelly Vega-Ramos, Patricia Castillo-Romero, Javier Chávez-Espinoza, Juan Panay-Centeno, Eliades Yarasca-Carlos
{"title":"SLCO1B1 and CYP3A4 allelic variants associated with pharmacokinetic interactions and adverse reactions induced by simvastatin and atorvastatin used in Peru: Clinical implications","authors":"Angel T. Alvarado, Ana María Muñoz, Roberto O. Ybañez-Julca, Mario Pineda-Pérez, Nesquen Tasayco-Yataco, María R. Bendezú, Jorge A. García, Felipe Surco-Laos, Haydee Chávez, Doris Laos-Anchante, Aura Molina-Cabrera, Carmela Ferreyra-Paredes, Nelly Vega-Ramos, Patricia Castillo-Romero, Javier Chávez-Espinoza, Juan Panay-Centeno, Eliades Yarasca-Carlos","doi":"10.56499/jppres23.1686_11.6.934","DOIUrl":"https://doi.org/10.56499/jppres23.1686_11.6.934","url":null,"abstract":"Context: Statins reduce the risk of stroke and prevent cardiac events in people with atherosclerosis and diabetes mellitus; and could affect the proliferation, migration, and survival of cancer cells. Aims: To review the most up-to-date and available scientific evidence on the allelic variants of SLCO1B1 and CYP3A4 associated with pharmacokinetic interactions and adverse reactions induced by simvastatin and atorvastatin used in Peru, and their clinical implications. Methods: The bibliographic search was carried out in the PubMed/Medline, Google Scholar and Science Direct databases. The keywords were: “statin”, “atorvastatin”, “simvastatin” in combination with “pharmacokinetics”, “pharmacogenetics”, “CYP3A4”, “SLCO1B1” or “drug interactions” considering the eligibility criteria defined by the PRISMA-2020 international statement. Results: Scientific evidence indicates a significant association between SLCO1B1 rs4149056 c.521T>C (521CC and 521TC) and increased plasma levels, area under the plasma concentration curve (AUC) and maximum plasma concentration (Cmax) of simvastatin, compared to wild-type SLCO1B1*1/*1 521TT (p<0.05). SLCO1B1 521C is not associated with atorvastatin (p>0.05). Patients with SLCO1B1 521CC had a significantly higher risk of myopathy and rhabdomyolysis induced by simvastatin compared to TT (p<0.05). An association was also found between CYP3A4*1/*22/CYP3A4*3/*22 and increased pharmacokinetic parameters of simvastatin compared to CYP3A4*1/*1 (p< 0.05). Conclusions: Based on the review of the published scientific evidence, it is concluded that individuals carrying the allelic variants SLCO1B1 (c.521T>C), CYP3A4*1/*22 and CYP3A4*3/*22 could be associated with an increase in the pharmacokinetic parameters and with an increased risk of myopathy and rhabdomyolysis induced by simvastatin, and not by atorvastatin.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136306979","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}
Widhya Aligita, Marlia Singgih, Entris Sutrisno, I Ketut Adnyana
{"title":"Hepatoprotective study of Indonesian water kefir against CCl4-induced liver injury in rats","authors":"Widhya Aligita, Marlia Singgih, Entris Sutrisno, I Ketut Adnyana","doi":"10.56499/jppres23.1732_11.6.1002","DOIUrl":"https://doi.org/10.56499/jppres23.1732_11.6.1002","url":null,"abstract":"Context: Water kefir is a fermented beverage that is typically made in the home by inoculating a sugar-rich solution with a microbial community (water kefir grains). Several studies on the metabolite content and hepatoprotective effects of water kefir have been published, but carbon tetrachloride (CCl4)-induced acute liver injury has not been studied. Aims: To evaluate the efficacy of water kefir in vivo against hepatoprotective CCl4-induced acute liver injury and to in silico investigate metabolites that play an important role in hepatoprotective mechanisms. Methods: The present study aimed to investigate the hepatoprotective activity of water kefir in an animal model caused by CCl4. Furthermore, using molecular docking, the metabolites found in water kefir were evaluated for their role in the NF-κB and Nrf2 signaling pathways. Results: Water kefir significantly and dose-dependently alleviated acute liver injury caused by CCl4. Water kefir administration at all doses produced results comparable to the positive control (Curcuma extract). Molecular docking simulations showed that, compared to Nrf2, the 25 metabolites were more likely to interact with the NF-B receptor. Fumaric acid is the strong metabolite that interacts with the NF-κB receptor with a free energy of binding and an inhibition constant of -6.66 kcal/mol and 13.22 µM, respectively. Conclusions: Water kefir administration improved the condition of liver damage, characterized by a decrease in serum levels of AST, ALT, TNF-, TGF-, and an improvement in the liver tissue profile. In silico evaluation showed that the metabolites in water kefir were able to interact with target proteins in the NF-B and Nrf2 pathways. It was concluded that water kefir improves the condition of the liver by reducing the level of necrosis and fibrosis.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136372519","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}
Orlando Pérez-Delgado, Pablo Alejandro Millones-Gómez, Alejandro Valencia-Arias, David Yeret Rodríguez-Salazar
{"title":"Risk factors for oral cancer: Thematic trends and research agenda","authors":"Orlando Pérez-Delgado, Pablo Alejandro Millones-Gómez, Alejandro Valencia-Arias, David Yeret Rodríguez-Salazar","doi":"10.56499/jppres23.1712_11.5.887","DOIUrl":"https://doi.org/10.56499/jppres23.1712_11.5.887","url":null,"abstract":"Context: Oral cancer is difficult to define due to several factors. It's known as oral squamous cell carcinoma (OSCC) and is common in the head and neck. Geographic variations in the impact of OSCC highlight the need for research on risk factors and treatment trends. Aims: To identify the main research trends of studies on oral cancer risk factors in the scientific literature in the Scopus database and Web of Science. Methods: This was an exploratory study of the risk factors for oral cancer designed considering the eligibility criteria defined by the PRISMA-2020 international statement, that is, inclusion and exclusion. Results: A total of 215 documents from Scopus and Web of Science were subjected to bibliometric analysis. The years 2020 and 2021 were the most productive, with 18 and 22 articles, respectively. The leading author in productivity and impact was Johnson N, the leading journal was Oral Oncology, followed by the International Journal of Cancer, and the main contributing countries were the United States, the United Kingdom and India. The main thematic cluster was composed of concepts such as Tobacco and Alcohol as the major risk factors; concepts such as Mortality or Head and Neck were positioned as emerging within the scientific literature. Conclusions: The main risk factors, i.e., alcohol and tobacco consumption, are relevant in terms of mortality in the consumer population, which is why their role should be determined in future studies.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135248708","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}
Syafruddin Ilyas, Putra Santoso, Yurnadi Hanafi Midoen, Putri Cahaya Situmorang
{"title":"Improvement of spermatozoa concentration due to maximal exercise with Vitis gracilis Wall.","authors":"Syafruddin Ilyas, Putra Santoso, Yurnadi Hanafi Midoen, Putri Cahaya Situmorang","doi":"10.56499/jppres23.1685_11.5.874","DOIUrl":"https://doi.org/10.56499/jppres23.1685_11.5.874","url":null,"abstract":"Context: Swimming is a common form of exercise; however, excessive exercise might reduce sperm count by lowering testosterone levels and increasing the production of free radicals, commonly known as reactive oxygen species (ROS). In Indonesia, Vitis gracilis Wall. is a traditional remedy for increasing stamina. Aims: To assess the concentration of spermatozoa after vigorous physical activity and V. gracilis administration, as well as the histological and apoptotic changes in testicular histology that occur via caspase-3 expression. Methods: This study was conducted on six groups of rats: the control group (G+), a group of rats subjected to vigorous swimming then administered 0.2 mg/kg BW vit C (GVitC), and three groups of rats subjected to vigorous swimming then administered 100, 125, or 150 mg/kg BW V. gracilis (G100, G125, and G150). Testicular tissue and blood serum samples were extracted from the rats subjected to vigorous swimming. Testicular tissue was immunohistochemically stained using caspase-3 antibody and TUNEL assays, while blood samples were analysed using ELISA. Results: V. gracilis administration significantly affected IL-6 and testosterone levels (p<0.00). Testosterone had a greater impact on spermatozoa concentration than IL-6. Caspase-3 expression and the proportion of apoptotic cells were both markedly reduced. Conclusions: Administering 125 mg/kg BW V. gracilis can help to increase sperm concentration by reducing apoptosis through altering caspase-3 and IL-6 levels, thereby preventing inflammation. This plant might be a viable molecular therapeutic target for staminal medicines.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135249032","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}
Aty Widyawaruyanti, Hilkatul Ilmi, Lidya Tumewu, Dwi Ayu Fitrianingtyas, Yesinta Kurniawati, Alfin Laila Najiha, Hanifah Khairun Nisa, Che Puteh Osman, Nor Hadiani Ismail, Achmad Fuad Hafid
{"title":"Antimalarial and toxicological assessment of the tablet (AS201-01) ethyl acetate fraction of Andrographis paniculata Nees in animal models","authors":"Aty Widyawaruyanti, Hilkatul Ilmi, Lidya Tumewu, Dwi Ayu Fitrianingtyas, Yesinta Kurniawati, Alfin Laila Najiha, Hanifah Khairun Nisa, Che Puteh Osman, Nor Hadiani Ismail, Achmad Fuad Hafid","doi":"10.56499/jppres23.1679_11.5.863","DOIUrl":"https://doi.org/10.56499/jppres23.1679_11.5.863","url":null,"abstract":"Context: Andrographis paniculata has been used as a traditional medicine to treat malaria. The ethyl acetate fraction of A. paniculata containing diterpene lactone compounds was developed into a tablet dosage form, AS201-01. Aims: To determine the antimalarial activity and toxicity of AS201-01 to guarantee its efficacy and safety. Methods: Antimalarial assay in male Balb/c mice based on Peter’s four-day suppressive test at a dose of 6.25, 12.5, 25, and 50 mg/kg BW and 10 mg/kg BW of chloroquine as a positive control. In acute toxicity, AS201-01 was administered orally at a dose of 5, 50, 200, and 2,000 mg/kg BW in male rats (Wistar rats) and observed for 14 days to identify signs of toxicity and mortality. Meanwhile, AS201-01 was administered at 50, 327, and 1,000 mg/kg BW per day for 28 days in male and female rats to assess subchronic toxicity. Results: AS201-01 has antimalarial activity and exhibited the highest suppressive effect at 50 mg/kg BW dose with inhibition of 73.48%. Meanwhile, chloroquine at 10 mg/kg BW has an inhibition of 97.94%. AS201-01 was highly active as an antimalarial with an ED50 value of 5.95 mg/kg BW and increased survival time. Administration of AS201-01 is relatively safe in acute and subchronic toxicity studies. No clinical signs and mortality were observed in either study. The 50% lethal dose (LD50) was above 2,000 mg/kg BW. Conclusions: AS201-01 is effective as an antimalarial and non-toxic when administered orally at an equivalent therapeutic dose in an animal model.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200599","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}
Nelson Daniel, Fisranda Ferdinand, Parikesit Arli Aditya
{"title":"In silico targeting CYP51 of Naegleria fowleri using bioactive compounds from Indonesian plants","authors":"Nelson Daniel, Fisranda Ferdinand, Parikesit Arli Aditya","doi":"10.56499/jppres23.1693_11.5.841","DOIUrl":"https://doi.org/10.56499/jppres23.1693_11.5.841","url":null,"abstract":"Context: Given the elusive nature of Primary Amoebic Meningoencephalitis (PAM), caused by Naegleria fowleri, early detection is vital, yet challenging due to limited clinical indicators. This research leverages Indonesia's rich biodiversity to explore novel sources of traditional medicine. Aims: To evaluate the potential compounds from Indonesian plants that possess antiamoebic and antifungal properties for inhibiting the N. fowleri CYP51 protein, crucial for cell integrity. Methods: Initially, 92 compounds were screened, and six were shortlisted following ADMETox evaluation. Subsequent steps encompassed QSAR analysis, molecular docking, and molecular dynamics simulations. Results: The QSAR analysis verified the activity potential of these six compounds, progressing them to molecular docking analysis. Among these, curcumenol from Curcuma longa emerged as a promising contender, displaying the lowest binding affinity at -9.2 kcal/mol, indicative of superior binding compared to other ligands. Molecular dynamics simulations underscored the stability of all compounds, with root mean square fluctuation (RMSF) values within 1-3 Å. Conclusions: Consequently, employing a comprehensive approach spanning ADMETox, QSAR, molecular docking, and dynamics simulations, curcumenol emerged as the prime candidate for inhibiting the N. fowleri CYP51 protein, suggesting its potential as a PAM therapeutic agent.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135200352","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}
Dini Kesuma, Galih S. Putra, Tegar A. Yuniarta, Farida Suhud, I G.A. Sumartha, Sawitri Boengas, Melanny I. Sulistyowaty, Tjie Kok
{"title":"Synthesis and in vitro activity tests of N-benzoyl-N'-phenylthiourea derivatives as macrophage migration inhibitory factor","authors":"Dini Kesuma, Galih S. Putra, Tegar A. Yuniarta, Farida Suhud, I G.A. Sumartha, Sawitri Boengas, Melanny I. Sulistyowaty, Tjie Kok","doi":"10.56499/jppres23.1657_11.5.902","DOIUrl":"https://doi.org/10.56499/jppres23.1657_11.5.902","url":null,"abstract":"Context: The COVID-19 pandemic in 2020 resulted in widespread mortalities due to cytokine storms in the affected patients. Macrophage migration inhibitory factor (MIF) is one of the most interesting targets in developing anti-COVID-19 drugs. Some thiourea compounds have been identified as having potential as MIF inhibitors. Aims: To investigate MIF inhibitory activity of N-benzoyl-N'-phenylthiourea derivatives. Methods: The study consists of in-silico activity prediction of designed compounds using a molecular docking approach against MIF protein (PDB ID: 1LJT). Afterwards, the designed compounds were synthesized and tested in vitro using the tautomerase activity approach. Results: The molecular docking study showed that all designed compounds possess comparable docking scores to the native ligand of the protein. MIF Assay performed on compounds (1) and (2) indicated a decrease in tautomerase activity of the MIF target protein of only 10.1 and 6.2%, respectively, compared to the positive control. Conclusions: In silico results predicted better bioactivity against MIF protein, but the result does not translate to the in vitro assay, where two of the designed compounds possess only low inhibitory activity.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135255124","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}