Pub Date : 2023-11-16DOI: 10.3897/pharmacia.70.e108995
Beyza Ozgen, S. P. Şenol, Dilsah Ezgi Yilmaz, Meryem Temiz-Reşitoğlu, Omer Bahceli, B. Tunctan
Objectives: This study aimed to investigate the effect of the gasdermin D (GSDMD) and mixed lineage kinase domain-like pseudokinase (MLKL) inhibitor, necrosulfonamide (NSA), on lipopolysaccharide (LPS)-induced hyperalgesia in mice. Methods: Reaction time to a thermal stimulus within 30 seconds was measured in male mice injected with saline, LPS, and/or NSA after 6 hours using the hot plate test. Immunoblotting studies were performed to determine changes in caspase-11/GSDMD-mediated pyroptosis, receptor-interacting serine/threonine-protein kinase (RIPK) 1/RIPK3/MLKL necrosome-mediated necroptosis, demyelination, and remyelination in the brains and spinal cords of animals. Results: NSA demonstrated significant antinociceptive activity compared with LPS-treated mice. In the tissues of LPS-treated mice, NSA decreased expression of caspase-11 p20, p30-GSDMD, interleukin-1β, high-mobility-group-box 1, and semaphorin 3A, and activity of RIPK1, RIPK3, and MLKL. NSA also increased the expression of myelin proteolipid protein. Conclusion: Therefore, NSA may have therapeutic potential in the treatment of inflammatory painful conditions due to bacterial infections.
{"title":"Pyroptosis and necroptosis inhibitor necrosulfonamide ameliorates lipopolysaccharide-induced inflammatory hyperalgesia in mice","authors":"Beyza Ozgen, S. P. Şenol, Dilsah Ezgi Yilmaz, Meryem Temiz-Reşitoğlu, Omer Bahceli, B. Tunctan","doi":"10.3897/pharmacia.70.e108995","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e108995","url":null,"abstract":"Objectives: This study aimed to investigate the effect of the gasdermin D (GSDMD) and mixed lineage kinase domain-like pseudokinase (MLKL) inhibitor, necrosulfonamide (NSA), on lipopolysaccharide (LPS)-induced hyperalgesia in mice. Methods: Reaction time to a thermal stimulus within 30 seconds was measured in male mice injected with saline, LPS, and/or NSA after 6 hours using the hot plate test. Immunoblotting studies were performed to determine changes in caspase-11/GSDMD-mediated pyroptosis, receptor-interacting serine/threonine-protein kinase (RIPK) 1/RIPK3/MLKL necrosome-mediated necroptosis, demyelination, and remyelination in the brains and spinal cords of animals. Results: NSA demonstrated significant antinociceptive activity compared with LPS-treated mice. In the tissues of LPS-treated mice, NSA decreased expression of caspase-11 p20, p30-GSDMD, interleukin-1β, high-mobility-group-box 1, and semaphorin 3A, and activity of RIPK1, RIPK3, and MLKL. NSA also increased the expression of myelin proteolipid protein. Conclusion: Therefore, NSA may have therapeutic potential in the treatment of inflammatory painful conditions due to bacterial infections.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"26 6","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139267582","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 : 2023-11-16DOI: 10.3897/pharmacia.70.e108012
R. Ruswanto, R. Mardianingrum, A. Septian, Arry Yanuar
The SIRT1 is overexpressed in a number of cancers. As a result, inhibiting SIRT1 may be used as a cancer treatment technique. Modification of 1-benzoyl-3-methylthiourea derivatives was carried out in this study by changing the aromatic side. The designed compounds (94) were subjected to in silico docking, pharmacokinetics, and preclinical testing. In the docking sample, the (4-decyl-N-(methylcarbamothioyl)benzamide (91), 2-(benzyloxy)-N-(methylcarbamo-thioyl)benzamide (93) and N-(methylcarbamothioyl)-2-naphthamide (94) were predicted to display better inhibition of SIRT1, so they were chosen for subsequent molecular dynamic studies. The compound 93 is proposed as a possible anticancer candidate that inhibits SIRT1 based on the screening results from molecular docking, pharmacokinetic predictions, and molecular dynamics.
{"title":"The design and virtual screening of thiourea derivatives as a Sirtuin-1 inhibitor","authors":"R. Ruswanto, R. Mardianingrum, A. Septian, Arry Yanuar","doi":"10.3897/pharmacia.70.e108012","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e108012","url":null,"abstract":"The SIRT1 is overexpressed in a number of cancers. As a result, inhibiting SIRT1 may be used as a cancer treatment technique. Modification of 1-benzoyl-3-methylthiourea derivatives was carried out in this study by changing the aromatic side. The designed compounds (94) were subjected to in silico docking, pharmacokinetics, and preclinical testing. In the docking sample, the (4-decyl-N-(methylcarbamothioyl)benzamide (91), 2-(benzyloxy)-N-(methylcarbamo-thioyl)benzamide (93) and N-(methylcarbamothioyl)-2-naphthamide (94) were predicted to display better inhibition of SIRT1, so they were chosen for subsequent molecular dynamic studies. The compound 93 is proposed as a possible anticancer candidate that inhibits SIRT1 based on the screening results from molecular docking, pharmacokinetic predictions, and molecular dynamics.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"31 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139267476","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 : 2023-11-15DOI: 10.3897/pharmacia.70.e111111
Anselmania Kartini Dhey, Eka Rasuna Andriani, Berliana Mardawati, Bunga Nur Annisa, R. Kristiana, Vera Permatasari, Gian Primahana, M. Prastya, P. Lotulung, T. Mozef, Akhmad Darmawan, S. Fajriah, Chairil Anwar, W. Haryadi
Aglaia foveolata Pannell (A. foveolata) is a type of plant that has many benefits, including the skin, leaves, roots, and seeds as medicinal ingredients. The potential of this plant is inseparable from the content of various bioactive compounds. This study aims to isolate, characterize the active compound from the stem bark of A. foveolata and test its activity as an antioxidant with the ABTS method, cytotoxic (MCF-7 cancer cells) with the MTT method, and antibacterial (bacterial strains ATCC and MDR) with the MIC. There are four isolated compounds obtained, namely (1) 17,24-epoxy-25-hydroxybaccharan-3-one, (2) β-stigmasterol glucoside, (3) Eichlerianic acid, and (4) 17,24-epoxy-25 -hydroxy-3- oxobaccharan-21-oic acid, which is a class of triterpenoid and steroid compounds. The best activity as an antioxidant was compound 3 (25.68 µg/mL); cytotoxic activity against MCF-7 cells namely compound 4 (94.59 µg/mL); antibacterial activity against ATCC strains: (1) P. aeruginosa namely compound 3 (29.4 µg/mL), (2) E. coli, (3) S. aureus, (4) B. subtilis for compounds 1, 2, and 4 have the same activity (62.5 µg/mL) while compound 3 was not active; MDR bacterial strains: (1) P. aeruginosa namely compound 4 (62.5 µg/mL), (2) E. coli namely compound 3 (62.5 µg/mL), (3) S. aureus namely compound 4 (62 .5 µg/mL), (4) B. subtilis namely compound 4 (62.5 µg/mL) and (5) K. pneumoniae namely compound 1 (125 µg/mL).
{"title":"Isolation and activity test of antioxidant, antibacterial, and cytotoxic compounds from the stem bark of Aglaia foveolata Pannell","authors":"Anselmania Kartini Dhey, Eka Rasuna Andriani, Berliana Mardawati, Bunga Nur Annisa, R. Kristiana, Vera Permatasari, Gian Primahana, M. Prastya, P. Lotulung, T. Mozef, Akhmad Darmawan, S. Fajriah, Chairil Anwar, W. Haryadi","doi":"10.3897/pharmacia.70.e111111","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111111","url":null,"abstract":"Aglaia foveolata Pannell (A. foveolata) is a type of plant that has many benefits, including the skin, leaves, roots, and seeds as medicinal ingredients. The potential of this plant is inseparable from the content of various bioactive compounds. This study aims to isolate, characterize the active compound from the stem bark of A. foveolata and test its activity as an antioxidant with the ABTS method, cytotoxic (MCF-7 cancer cells) with the MTT method, and antibacterial (bacterial strains ATCC and MDR) with the MIC. There are four isolated compounds obtained, namely (1) 17,24-epoxy-25-hydroxybaccharan-3-one, (2) β-stigmasterol glucoside, (3) Eichlerianic acid, and (4) 17,24-epoxy-25 -hydroxy-3- oxobaccharan-21-oic acid, which is a class of triterpenoid and steroid compounds. The best activity as an antioxidant was compound 3 (25.68 µg/mL); cytotoxic activity against MCF-7 cells namely compound 4 (94.59 µg/mL); antibacterial activity against ATCC strains: (1) P. aeruginosa namely compound 3 (29.4 µg/mL), (2) E. coli, (3) S. aureus, (4) B. subtilis for compounds 1, 2, and 4 have the same activity (62.5 µg/mL) while compound 3 was not active; MDR bacterial strains: (1) P. aeruginosa namely compound 4 (62.5 µg/mL), (2) E. coli namely compound 3 (62.5 µg/mL), (3) S. aureus namely compound 4 (62 .5 µg/mL), (4) B. subtilis namely compound 4 (62.5 µg/mL) and (5) K. pneumoniae namely compound 1 (125 µg/mL).","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"17 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139271048","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 : 2023-11-10DOI: 10.3897/pharmacia.70.e113771
Khairul Putra Surbakti, Riessa Melani, R. A. Dwi Pujiastuti
Background : Patients suffering from primary headaches such as migraine, tension-type headache, and cluster headache frequently report cognitive problems, particularly with attention and memory. The aim of this study was to see if there was a link between pain intensity and cognitive function in people who had primary headaches. Methods : This cross-sectional study included 69 primary headache patients (37 migraines, 27 tension-type headaches and 5 cluster headaches; age range 18–80 year). Migraine, tension-type headache and cluster headache diagnosis were determined according to the International Classification of Headache Disorders 3 rd edition beta version (ICHD-3 beta) diagnostic criteria. All eligible subjects underwent cognitive function examination using Montreal Cognitive Assessment Indonesian version (MoCA-INA), Trail Making test A (TMT-A), Trail Making test B (TMT-B), Trail Making test C (TMT-C), Forward Digit Span and Backward Digit Span. The intensity of pain was assessed using Numeric Rating Scale (NRS). Results : There were 69 primary headache patients included in this study, 52 (75.4%) patients had abnormal MoCA-INA, 52(75.4%) patients had abnormal Forward Digit Span and 48(69.6%) patients had abnormal Backward Digit Span. There was significant correlation between pain intensity and cognitive function in migraine, TTH and cluster headaches patients. The MoCA-INA, Forward Digit Span and Backward Digit Span had negative correlations with pain intensity, whereas TMT A-time, TMT A-error, TMT B-time and TMT B-error had positive correlation. Conclusion : There were significant associations between pain intensity of and cognitive function in primary headaches with p<0.05. It is suggested that the more severe pain intensity, the more impair of cognitive function.
{"title":"Association between pain intensity and cognitive function in primary headache","authors":"Khairul Putra Surbakti, Riessa Melani, R. A. Dwi Pujiastuti","doi":"10.3897/pharmacia.70.e113771","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113771","url":null,"abstract":"Background : Patients suffering from primary headaches such as migraine, tension-type headache, and cluster headache frequently report cognitive problems, particularly with attention and memory. The aim of this study was to see if there was a link between pain intensity and cognitive function in people who had primary headaches. Methods : This cross-sectional study included 69 primary headache patients (37 migraines, 27 tension-type headaches and 5 cluster headaches; age range 18–80 year). Migraine, tension-type headache and cluster headache diagnosis were determined according to the International Classification of Headache Disorders 3 rd edition beta version (ICHD-3 beta) diagnostic criteria. All eligible subjects underwent cognitive function examination using Montreal Cognitive Assessment Indonesian version (MoCA-INA), Trail Making test A (TMT-A), Trail Making test B (TMT-B), Trail Making test C (TMT-C), Forward Digit Span and Backward Digit Span. The intensity of pain was assessed using Numeric Rating Scale (NRS). Results : There were 69 primary headache patients included in this study, 52 (75.4%) patients had abnormal MoCA-INA, 52(75.4%) patients had abnormal Forward Digit Span and 48(69.6%) patients had abnormal Backward Digit Span. There was significant correlation between pain intensity and cognitive function in migraine, TTH and cluster headaches patients. The MoCA-INA, Forward Digit Span and Backward Digit Span had negative correlations with pain intensity, whereas TMT A-time, TMT A-error, TMT B-time and TMT B-error had positive correlation. Conclusion : There were significant associations between pain intensity of and cognitive function in primary headaches with p&lt;0.05. It is suggested that the more severe pain intensity, the more impair of cognitive function.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":" 11","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135141498","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 : 2023-11-09DOI: 10.3897/pharmacia.70.e113558
Yulistiani Yulistiani, Nur Fauzi Hamidi, Febriansyah Nur Utomo, Khusnul Fitri Hamidah
Background : The existence of the COVID-19 pandemic has caused a shift in medicine use in patients. Objective : This study aims to determine patterns and differences in medicine use at Airlangga University Hospital before (2018 and 2019) and after (2020–2022) the COVID-19 pandemic based on ABC, VEN and ABC-VEN matrix analysis. Methods : This study is a retrospective cross-sectional study. Data on all patients’ medicine use items between January 1 st , 2018 – December 31 st , 2022 which obtained from the hospital information system will be analyzed according to category based on the principles of ABC analysis, VEN, and the ABC-VEN combination and a statistical t-test analysis in SPSS to find out differences in medicine use at the Universitas Airlangga Hospital in the pre-pandemic era of COVID-19 versus the era of the COVID-19 pandemic. Results : Based on the results of the study, a total of 6893 drug items were obtained. There was a significant shift in the pattern of non-essential medicines use prescribed to patients after the COVID-19 pandemic (p < 0,05). Conclusion : There was a shift in the pattern of use of prescribed non-essential medicines after the COVID-19 pandemic compared to before the pandemic occurred.
{"title":"Shifts in drugs use after the COVID-19 pandemic based on the analysis of ABC, VEN and ABC-VEN matrix","authors":"Yulistiani Yulistiani, Nur Fauzi Hamidi, Febriansyah Nur Utomo, Khusnul Fitri Hamidah","doi":"10.3897/pharmacia.70.e113558","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113558","url":null,"abstract":"Background : The existence of the COVID-19 pandemic has caused a shift in medicine use in patients. Objective : This study aims to determine patterns and differences in medicine use at Airlangga University Hospital before (2018 and 2019) and after (2020–2022) the COVID-19 pandemic based on ABC, VEN and ABC-VEN matrix analysis. Methods : This study is a retrospective cross-sectional study. Data on all patients’ medicine use items between January 1 st , 2018 – December 31 st , 2022 which obtained from the hospital information system will be analyzed according to category based on the principles of ABC analysis, VEN, and the ABC-VEN combination and a statistical t-test analysis in SPSS to find out differences in medicine use at the Universitas Airlangga Hospital in the pre-pandemic era of COVID-19 versus the era of the COVID-19 pandemic. Results : Based on the results of the study, a total of 6893 drug items were obtained. There was a significant shift in the pattern of non-essential medicines use prescribed to patients after the COVID-19 pandemic (p &lt; 0,05). Conclusion : There was a shift in the pattern of use of prescribed non-essential medicines after the COVID-19 pandemic compared to before the pandemic occurred.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":" 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135291019","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 : 2023-11-07DOI: 10.3897/pharmacia.70.e111415
Ni Made Dwi Sandhiutami, Yesi Desmiaty, Yati Sumiyati, Asma Fauziyah Baihaqi, Myra Gracia
This study aims to evaluate effect of Colocasia esculenta and Zingiber officinale combined extract (CEZO) in osteoarthritis rats. Twenty-four Wistar rats were split into normal group, positive group, negative group, and CEZO group on 29 th to 43 rd day (n = 6). All rats were injected with Na-iodoacetate intraarticularly on first day, unless for the normal group, and then observing the diameter of knee edema until the 28 th day (OA rats). On the 43 rd day, rats were euthanasia for measurements of hematology, spleen weight, and inflammatory mediators of nitric oxide, matrix metalloproteinase 9, Interleukin-6, and tumor necrosis factor-α using ELISA kit. Our experiments showed that CEZO 90 mg/kgBW was able to decrease knee edema, leukocytes, lymphocytes, spleen enlargement, the concentration of mediators inflammatory NO, TNF-α, IL-6, and protect cartilage degradation by decreased MMP-9 significantly in OA rats. Conclusion of the research is the CEZO 90 mg/kgBW supplementation has potential to be used in osteoarthritis.
{"title":"The potential of Colocasia esculenta tuber and Zingiber officinale rhizome combined extracts to ameliorate inflammation in monosodium iodoacetate-osteoarthritis rat model","authors":"Ni Made Dwi Sandhiutami, Yesi Desmiaty, Yati Sumiyati, Asma Fauziyah Baihaqi, Myra Gracia","doi":"10.3897/pharmacia.70.e111415","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111415","url":null,"abstract":"This study aims to evaluate effect of Colocasia esculenta and Zingiber officinale combined extract (CEZO) in osteoarthritis rats. Twenty-four Wistar rats were split into normal group, positive group, negative group, and CEZO group on 29 th to 43 rd day (n = 6). All rats were injected with Na-iodoacetate intraarticularly on first day, unless for the normal group, and then observing the diameter of knee edema until the 28 th day (OA rats). On the 43 rd day, rats were euthanasia for measurements of hematology, spleen weight, and inflammatory mediators of nitric oxide, matrix metalloproteinase 9, Interleukin-6, and tumor necrosis factor-α using ELISA kit. Our experiments showed that CEZO 90 mg/kgBW was able to decrease knee edema, leukocytes, lymphocytes, spleen enlargement, the concentration of mediators inflammatory NO, TNF-α, IL-6, and protect cartilage degradation by decreased MMP-9 significantly in OA rats. Conclusion of the research is the CEZO 90 mg/kgBW supplementation has potential to be used in osteoarthritis.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"15 10","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135480569","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 : 2023-11-07DOI: 10.3897/pharmacia.70.e107406
Fathoni Ega Mulyana, Stephanus Satria Wira Waskitha, Deni Pranowo, Melati Khairuddean, Tutik Dwi Wahyumingsih
Malaria remains an endemic disease in tropical regions, urgently needed the search for effective antimalarial agents due to resistance against existing drugs. This study investigated the potential antimalarial activity of pyridine-based chalcone derivatives against P. falciparum 3D7 and FCR3 strains. The chalcones were synthesized through a one-pot method using various pyridine carbaldehyde, resulting in yields ranging from 53.74 to 86.37%, and all products were characterized using FTIR, GC-MS, and NMR spectroscopies. Among the six chalcones tested, chalcone A [1-(2-methoxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one] displayed the highest antimalarial activity with IC 50 values of 0.48 and 0.31 μg/mL against P. falciparum 3D7 and FCR3 strains, respectively, and a resistance index of 0.65. Molecular docking studies highlighted the interaction of the carbonyl group of all chalcones with Asn108 amino acid residue in the P f DHFR-TS active site via hydrogen bonding, demonstrating their potential as the antimalarial agent. Notably, the positioning of methoxy and pyridine substituents significantly influenced the antimalarial activity of the chalcones.
{"title":"Synthesis of chalcone derivatives with methoxybenzene and pyridine moieties as potential antimalarial agents","authors":"Fathoni Ega Mulyana, Stephanus Satria Wira Waskitha, Deni Pranowo, Melati Khairuddean, Tutik Dwi Wahyumingsih","doi":"10.3897/pharmacia.70.e107406","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e107406","url":null,"abstract":"Malaria remains an endemic disease in tropical regions, urgently needed the search for effective antimalarial agents due to resistance against existing drugs. This study investigated the potential antimalarial activity of pyridine-based chalcone derivatives against P. falciparum 3D7 and FCR3 strains. The chalcones were synthesized through a one-pot method using various pyridine carbaldehyde, resulting in yields ranging from 53.74 to 86.37%, and all products were characterized using FTIR, GC-MS, and NMR spectroscopies. Among the six chalcones tested, chalcone A [1-(2-methoxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one] displayed the highest antimalarial activity with IC 50 values of 0.48 and 0.31 μg/mL against P. falciparum 3D7 and FCR3 strains, respectively, and a resistance index of 0.65. Molecular docking studies highlighted the interaction of the carbonyl group of all chalcones with Asn108 amino acid residue in the P f DHFR-TS active site via hydrogen bonding, demonstrating their potential as the antimalarial agent. Notably, the positioning of methoxy and pyridine substituents significantly influenced the antimalarial activity of the chalcones.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"323 4","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135475176","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 : 2023-11-02DOI: 10.3897/pharmacia.70.e108922
Hendy Suhendy, Irda Fidrianny, Muhamad Insanu
This article provides an overview of Ipomoea batatas L., the Ipomoea genus. The review covers traditional uses, nutritional value, phytochemical compounds, pharmacological activities, and toxicity studies. Data were collected from scientific databases and search engines. Sweet potatoes are used in various countries for traditional uses such as dietary fiber sources, treating allergies, and providing energy in diabetes mellitus treatment. The primary phytochemical compounds in Ipomoea batatas are phenolic compounds, flavonoids, anthocyanins, and carotenoids. Sweet potato contains several nutritional constituents: vitamin C, protein, fiber, carbohydrates, β-carotene, and minerals. Sweet potato exhibits various pharmacological activities, such as antioxidant, aphrodisiac, anticancer, and anti-inflammatory. The types of phytochemical compounds in each part of the plant are different. Each pharmacological activity and mechanism of action depends on the phytochemical compounds, part and variety of the plant, and extraction solvent. However, further study is required to investigate the chronic toxicity of Ipomoea batatas .
{"title":"Phytochemical compounds and pharmacological activities of Ipomoea batatas L.: An updated review","authors":"Hendy Suhendy, Irda Fidrianny, Muhamad Insanu","doi":"10.3897/pharmacia.70.e108922","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e108922","url":null,"abstract":"This article provides an overview of Ipomoea batatas L., the Ipomoea genus. The review covers traditional uses, nutritional value, phytochemical compounds, pharmacological activities, and toxicity studies. Data were collected from scientific databases and search engines. Sweet potatoes are used in various countries for traditional uses such as dietary fiber sources, treating allergies, and providing energy in diabetes mellitus treatment. The primary phytochemical compounds in Ipomoea batatas are phenolic compounds, flavonoids, anthocyanins, and carotenoids. Sweet potato contains several nutritional constituents: vitamin C, protein, fiber, carbohydrates, β-carotene, and minerals. Sweet potato exhibits various pharmacological activities, such as antioxidant, aphrodisiac, anticancer, and anti-inflammatory. The types of phytochemical compounds in each part of the plant are different. Each pharmacological activity and mechanism of action depends on the phytochemical compounds, part and variety of the plant, and extraction solvent. However, further study is required to investigate the chronic toxicity of Ipomoea batatas .","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"18 10","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135932966","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 : 2023-11-01DOI: 10.3897/pharmacia.70.e110191
Asmaa Abdelaziz Mohamed, Noor Zuhair Kbah, Osama N. Wennas
This study aimed to consolidate rupatadine fumarate (RF) into nanoparticles to control its release. Ten RF nanoparticles were developed by nanoprecipitation using poly (lactic-co-glycolic acid) (PLGA) , polyvinyl alcohol (PVA), and Poloxamer 407 (Kolliphor P 407) in different percentages. A valid reverse-phase HPLC method was developed to assess RF in the formulated nanoparticles. The RF nanoparticles were tested chemically and morphologically. RF nanoparticles containing PLGA and PVA and Kolliphor P 407 have zeta potentials ranging from -24.4 mV±0.24 to -26.7 mV±0.05, higher than other formulations, and their release profiles were optimised. The formula (RPX3) had the best zeta potential (-26.7 mV±0.05), released about 86% of RF after 8 h and extended for 24 h. In summary, the formulation (RPX3), including 2:10:3:1.5 ratios of the drug PLGA: PVA: Kolliphor P 407 was the optimised RF-loaded nanoparticles formulation.
{"title":"Poly (lactic-co-glycolic acid) nanoparticles for drug delivery of rupatadine fumarate: development and evaluation","authors":"Asmaa Abdelaziz Mohamed, Noor Zuhair Kbah, Osama N. Wennas","doi":"10.3897/pharmacia.70.e110191","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e110191","url":null,"abstract":"This study aimed to consolidate rupatadine fumarate (RF) into nanoparticles to control its release. Ten RF nanoparticles were developed by nanoprecipitation using poly (lactic-co-glycolic acid) (PLGA) , polyvinyl alcohol (PVA), and Poloxamer 407 (Kolliphor P 407) in different percentages. A valid reverse-phase HPLC method was developed to assess RF in the formulated nanoparticles. The RF nanoparticles were tested chemically and morphologically. RF nanoparticles containing PLGA and PVA and Kolliphor P 407 have zeta potentials ranging from -24.4 mV±0.24 to -26.7 mV±0.05, higher than other formulations, and their release profiles were optimised. The formula (RPX3) had the best zeta potential (-26.7 mV±0.05), released about 86% of RF after 8 h and extended for 24 h. In summary, the formulation (RPX3), including 2:10:3:1.5 ratios of the drug PLGA: PVA: Kolliphor P 407 was the optimised RF-loaded nanoparticles formulation.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"319 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135320500","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}
Invasive fungal infections cause serious illness and death worldwide. Long-term therapeutic and preventative use of antifungal drugs in high-risk patients has caused resistance. Triazole antifungals are widely used to prevent and treat fungal infections, and therapeutic drug monitoring has been suggested to improve outcomes, reduce toxicity, and prevent drug resistance. Common methods used for monitoring triazole antifungal drugs in biological matrices such as blood, serum, and plasma include bioassay and instrumentation methods, especially liquid chromatography. Sample preparation is needed to remove interference from liquid chromatography for reliable results. This paper evaluates the use of liquid chromatography to analyze triazole antifungal agents. We provided various chromatographic techniques combined with different detector types to analyze triazole antifungal drugs in biological matrices. We also compared chromatography systems with different sample preparation methods in order to select the most suitable analytical method for bioanalysis.
{"title":"Separation and analysis of triazole antifungal in biological matrices by liquid chromatography: a review","authors":"Untung Gunawan, Slamet Ibrahim, Atthar Luqman Ivansyah, Sophi Damayanti","doi":"10.3897/pharmacia.70.e111511","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111511","url":null,"abstract":"Invasive fungal infections cause serious illness and death worldwide. Long-term therapeutic and preventative use of antifungal drugs in high-risk patients has caused resistance. Triazole antifungals are widely used to prevent and treat fungal infections, and therapeutic drug monitoring has been suggested to improve outcomes, reduce toxicity, and prevent drug resistance. Common methods used for monitoring triazole antifungal drugs in biological matrices such as blood, serum, and plasma include bioassay and instrumentation methods, especially liquid chromatography. Sample preparation is needed to remove interference from liquid chromatography for reliable results. This paper evaluates the use of liquid chromatography to analyze triazole antifungal agents. We provided various chromatographic techniques combined with different detector types to analyze triazole antifungal drugs in biological matrices. We also compared chromatography systems with different sample preparation methods in order to select the most suitable analytical method for bioanalysis.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"312 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135321700","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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