Bangkal (Nauclea subdita (Korth.) Steud.) is a tropical plant belonging to the Rubiaceae family, commonly found in South Kalimantan. This plant is one of the plants that has efficacy as a medicinal plant. This study aimed to quantitatively identify secondary metabolites and antioxidant activity in the n-hexane and ethyl acetate fractions of N. subdita leaves. The method of identification of secondary metabolites using the test tube. Antioxidant activity using the DPPH method based on IC50 value. The results of identifying secondary metabolites in the n-hexane fraction of N. subdita leaves contain alkaloids, flavonoids, steroids, and phenolic compounds, while the ethyl acetate fraction of N. subdita leaves contain alkaloids, flavonoids, steroids, tannins, saponins, and phenolics. The results of the antioxidant activity test of the n-hexane fraction and the ethyl acetate fraction of the leaves of N. subdita showed IC50 values of 229.61178±3.65919 and 54.54296±0.02236 ppm, respectively. Based on the IC50 value, the n-hexane fraction of N. subdita leaves had weak antioxidant activity, and the ethyl acetate fraction of N. subdita leaves had strong antioxidant activity.
{"title":"Antioxidant Activity of n-hexane and Etil Acetate Fractions of Bangkal (Nauclea subdita (Korth.) Steud.) Leaves","authors":"A. Arnida, Al Madani, S. Sutomo","doi":"10.33084/bjop.v6i2.4738","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4738","url":null,"abstract":"Bangkal (Nauclea subdita (Korth.) Steud.) is a tropical plant belonging to the Rubiaceae family, commonly found in South Kalimantan. This plant is one of the plants that has efficacy as a medicinal plant. This study aimed to quantitatively identify secondary metabolites and antioxidant activity in the n-hexane and ethyl acetate fractions of N. subdita leaves. The method of identification of secondary metabolites using the test tube. Antioxidant activity using the DPPH method based on IC50 value. The results of identifying secondary metabolites in the n-hexane fraction of N. subdita leaves contain alkaloids, flavonoids, steroids, and phenolic compounds, while the ethyl acetate fraction of N. subdita leaves contain alkaloids, flavonoids, steroids, tannins, saponins, and phenolics. The results of the antioxidant activity test of the n-hexane fraction and the ethyl acetate fraction of the leaves of N. subdita showed IC50 values of 229.61178±3.65919 and 54.54296±0.02236 ppm, respectively. Based on the IC50 value, the n-hexane fraction of N. subdita leaves had weak antioxidant activity, and the ethyl acetate fraction of N. subdita leaves had strong antioxidant activity.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85846189","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}
C. W. Sabandar, H. Kamaruddin, Reskiya Nur Insani, R. Amin, Z. Zulkifli, T. Tien
The edible part of Benicasa hispida (Thunb.) Cogn. fruit is traditionally used in Southeast Sulawesi to treat high blood pressure, typhoid fever, and body cooling. The present study evaluated the chemical compounds present in the 80% ethanol of the edible part of the plant using phytochemical screening and an LC-MS analysis, antioxidant activity based on assays on total phenolics content (TPC), total flavonoids content (TFC), and DPPH, and antimicrobial activity towards Salmonella typhi, Escherichia coli, Staphylococcus aureus, and Candida albicans. Phytochemical screening revealed the presence of tannins, flavonoids, terpenoids, steroids, and saponins in the extract. As many as eighteen compounds (1-18) were tentatively identified in the extract, including sugars, a simple phenolic, a tricarboxylic acid, a peptide, flavonoids, quinic acid derivatives, phytosterols, triterpenoids, and saponins. The extract exhibited remarkable antioxidant activity with an SC50 value of 23.4 µg/mL, although its TPC (1.1±0.1 mg GAE/g extract) and TFC (1.0±0.1 mg QE/g extract) values were considered in low amounts. The extract was found inactive to inhibit the microbial growths of all tested microbes. However, raffinose (3) present in the extract might be beneficial as a prebiotic to promote a healthy human gut. The study concludes that the 80% ethanol extract of the edible part of B. hispida fruit could be used to develop natural antioxidant agents and nutraceuticals.
{"title":"Tentative Identification of Compounds, Antioxidant, and Antimicrobial Activity of the Edible Part of Benincasa hispida L. fruit (Cucurbitaceae)","authors":"C. W. Sabandar, H. Kamaruddin, Reskiya Nur Insani, R. Amin, Z. Zulkifli, T. Tien","doi":"10.33084/bjop.v6i2.4350","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4350","url":null,"abstract":"The edible part of Benicasa hispida (Thunb.) Cogn. fruit is traditionally used in Southeast Sulawesi to treat high blood pressure, typhoid fever, and body cooling. The present study evaluated the chemical compounds present in the 80% ethanol of the edible part of the plant using phytochemical screening and an LC-MS analysis, antioxidant activity based on assays on total phenolics content (TPC), total flavonoids content (TFC), and DPPH, and antimicrobial activity towards Salmonella typhi, Escherichia coli, Staphylococcus aureus, and Candida albicans. Phytochemical screening revealed the presence of tannins, flavonoids, terpenoids, steroids, and saponins in the extract. As many as eighteen compounds (1-18) were tentatively identified in the extract, including sugars, a simple phenolic, a tricarboxylic acid, a peptide, flavonoids, quinic acid derivatives, phytosterols, triterpenoids, and saponins. The extract exhibited remarkable antioxidant activity with an SC50 value of 23.4 µg/mL, although its TPC (1.1±0.1 mg GAE/g extract) and TFC (1.0±0.1 mg QE/g extract) values were considered in low amounts. The extract was found inactive to inhibit the microbial growths of all tested microbes. However, raffinose (3) present in the extract might be beneficial as a prebiotic to promote a healthy human gut. The study concludes that the 80% ethanol extract of the edible part of B. hispida fruit could be used to develop natural antioxidant agents and nutraceuticals.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81679873","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}
Chronic inflammation is common in infectious diseases, rheumatoid arthritis, gout, and autoimmune diseases. However, using non-steroidal anti-inflammatory drugs (NSAIDs) is accompanied by dangerous side effects. Therefore, searching for safer alternative therapies without side effects is very important. A natural blend of ingredients produced by stingless bees from plants was potential as a remedy. Meanwhile, the potential of kelulut bee products from East Kalimantan as an anti-inflammatory is still unknown. This study aimed to compare the chemical composition of kelulut bee (Trigona apicalis) products and evaluate the anti-inflammatory effect of honey, propolis, and their combination. Propolis extract and honey were determined as secondary metabolites. An anti-inflammatory in vivo assay triggered the edema using carrageenan on male mice and measured its anti-inflammatory power value. Propolis extract and honey from T. apicalis have a promising anti-inflammatory effect and are significantly higher than the positive control. Meanwhile, combining propolis extract and honey did not enhance the anti-inflammatory effect. In addition, combining honey and propolis preparations with a ratio of 75 : 25 has a better effect on reducing edema volume than the other two combinations. Still, it is not better than the treatment with propolis extract or honey alone. The content of polyphenol compounds found in honey and propolis preparations is thought to have an important role in reducing edema volume.
{"title":"Phytochemical Analysis and Anti-Inflammatory Activity of The Combination of Trigona apicalis propolis Extract and Honey","authors":"Paula Mariana Kustiawan, Chaerul Fadly Mochtar Luthfi M, Sinta Ratna Dewi, Jati Pratiwi, Novia Misnawati Aisyiyah, Alfin Syahrian Dwi Nugraha, Irfan Muris Setiawan","doi":"10.33084/bjop.v6i2.4696","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4696","url":null,"abstract":"Chronic inflammation is common in infectious diseases, rheumatoid arthritis, gout, and autoimmune diseases. However, using non-steroidal anti-inflammatory drugs (NSAIDs) is accompanied by dangerous side effects. Therefore, searching for safer alternative therapies without side effects is very important. A natural blend of ingredients produced by stingless bees from plants was potential as a remedy. Meanwhile, the potential of kelulut bee products from East Kalimantan as an anti-inflammatory is still unknown. This study aimed to compare the chemical composition of kelulut bee (Trigona apicalis) products and evaluate the anti-inflammatory effect of honey, propolis, and their combination. Propolis extract and honey were determined as secondary metabolites. An anti-inflammatory in vivo assay triggered the edema using carrageenan on male mice and measured its anti-inflammatory power value. Propolis extract and honey from T. apicalis have a promising anti-inflammatory effect and are significantly higher than the positive control. Meanwhile, combining propolis extract and honey did not enhance the anti-inflammatory effect. In addition, combining honey and propolis preparations with a ratio of 75 : 25 has a better effect on reducing edema volume than the other two combinations. Still, it is not better than the treatment with propolis extract or honey alone. The content of polyphenol compounds found in honey and propolis preparations is thought to have an important role in reducing edema volume.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"45 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135434708","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}
Assalamu’alaikum Wr. Wb. Alhamdulillahirabbil ‘alamin. The next edition of the Borneo Journal of Pharmacy (Borneo J Pharm) was published in May 2023. This edition contains ten articles: Pharmacology-Toxicology, Pharmacognosy-Phytochemistry, Pharmaceutical, Analytical Pharmacy-Medicinal Chemistry, Natural Product Development, and Management Pharmacy. This edition includes writings from five countries: Indonesia, Nigeria, the Philippines, Taiwan, and the United States. The authors come from several institutions, including Universitas Ahmad Dahlan, Universitas Muhammadiyah Mataram, University of California, Los Angeles, National Research and Innovation Agency Republic of Indonesia, Universitas Muhammadiyah Prof. Dr. HAMKA, Universitas Muhammadiyah Kalimantan Timur, Universitas Gadjah Mada, Universitas Sembilanbelas November Kolaka, Universitas Halu Oleo, Universitas Lambung Mangkurat, Universitas Jenderal Achmad Yani, Ahmadu Bello University, Institut Kesehatan Helvetia, Taipei Medical University, Sekolah Tinggi Ilmu Farmasi Riau, University of the Philippines Manila, and Universitas Diponegoro. Editorial boards are fully aware that there is still room for improvement in this edition; hence with all humility, willing to accept constructive suggestions and feedback for improvements to the publication for the next editions. The editorial board would like to thank all editors and reviewers, and contributors of the scientific articles who have provided the repertoire in this issue. We hope all parties, especially the contributors, can re-participate for publication in the next edition on August 2023. Wassalamu’alaikum Wr. Wb.
{"title":"Cover, Content, and Editorial Note from Borneo J Pharm Vol. 6 No. 2 May 2023","authors":"C. E. O. Borneo J Pharm","doi":"10.33084/bjop.v6i2.5599","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.5599","url":null,"abstract":"Assalamu’alaikum Wr. Wb. \u0000Alhamdulillahirabbil ‘alamin. The next edition of the Borneo Journal of Pharmacy (Borneo J Pharm) was published in May 2023. This edition contains ten articles: Pharmacology-Toxicology, Pharmacognosy-Phytochemistry, Pharmaceutical, Analytical Pharmacy-Medicinal Chemistry, Natural Product Development, and Management Pharmacy. This edition includes writings from five countries: Indonesia, Nigeria, the Philippines, Taiwan, and the United States. The authors come from several institutions, including Universitas Ahmad Dahlan, Universitas Muhammadiyah Mataram, University of California, Los Angeles, National Research and Innovation Agency Republic of Indonesia, Universitas Muhammadiyah Prof. Dr. HAMKA, Universitas Muhammadiyah Kalimantan Timur, Universitas Gadjah Mada, Universitas Sembilanbelas November Kolaka, Universitas Halu Oleo, Universitas Lambung Mangkurat, Universitas Jenderal Achmad Yani, Ahmadu Bello University, Institut Kesehatan Helvetia, Taipei Medical University, Sekolah Tinggi Ilmu Farmasi Riau, University of the Philippines Manila, and Universitas Diponegoro. \u0000Editorial boards are fully aware that there is still room for improvement in this edition; hence with all humility, willing to accept constructive suggestions and feedback for improvements to the publication for the next editions. The editorial board would like to thank all editors and reviewers, and contributors of the scientific articles who have provided the repertoire in this issue. We hope all parties, especially the contributors, can re-participate for publication in the next edition on August 2023. \u0000Wassalamu’alaikum Wr. Wb.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"88 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79443565","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}
Leny Leny, Tetty Noverita Khairani Situmorang, Rensus Siagian, Ihsanul Hafiz, B. Iskandar
Treatment done on burn wounds is intended to provide local therapy to heal as quickly as possible. The content of secondary metabolites in the tapak dara (Catharanthus roseus (L.) G. Don) flower can help the healing process of burns, namely alkaloids, saponins, tannins, and flavonoids. Alkaloids act as antibacterial; saponins can trigger collagen formation; tannins as astringents that cause shrinkage of skin pores and stop minor bleeding in wounds; and flavonoids have anti-inflammatory effects. This study aimed to formulate an ointment of C. roseus flower ethanol extract and determine its physical characteristics such as organoleptic test, homogeneity, pH value, dispersion, and stability test of the preparation and examine the activity as a burn healer in white male rats. The research data were analyzed statistically using the ANOVA method, followed by the LSD test (least significant difference) to see how the ointment-containing extract reduced the diameter and percentage of the burn wounds. The results show that all ethanol extracts of C. roseus flower ointments met the requirements for its physical characteristic tests. It offers a good activity as a burn healer in white male rats. The most effective concentration is an ointment containing 15% of ethanol extract from C. roseus flower (F3 group), which shows a significant difference (p <0.05) from the blank and the other group formula in burn wound healing.
{"title":"Ointment Formulation of Tapak Dara (Catharanthus roseus (L.) G. Don) Flower Ethanol Extract and its Activity in Burn-Healing","authors":"Leny Leny, Tetty Noverita Khairani Situmorang, Rensus Siagian, Ihsanul Hafiz, B. Iskandar","doi":"10.33084/bjop.v6i2.3155","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.3155","url":null,"abstract":"Treatment done on burn wounds is intended to provide local therapy to heal as quickly as possible. The content of secondary metabolites in the tapak dara (Catharanthus roseus (L.) G. Don) flower can help the healing process of burns, namely alkaloids, saponins, tannins, and flavonoids. Alkaloids act as antibacterial; saponins can trigger collagen formation; tannins as astringents that cause shrinkage of skin pores and stop minor bleeding in wounds; and flavonoids have anti-inflammatory effects. This study aimed to formulate an ointment of C. roseus flower ethanol extract and determine its physical characteristics such as organoleptic test, homogeneity, pH value, dispersion, and stability test of the preparation and examine the activity as a burn healer in white male rats. The research data were analyzed statistically using the ANOVA method, followed by the LSD test (least significant difference) to see how the ointment-containing extract reduced the diameter and percentage of the burn wounds. The results show that all ethanol extracts of C. roseus flower ointments met the requirements for its physical characteristic tests. It offers a good activity as a burn healer in white male rats. The most effective concentration is an ointment containing 15% of ethanol extract from C. roseus flower (F3 group), which shows a significant difference (p <0.05) from the blank and the other group formula in burn wound healing.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82347068","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}
In the Philippines, Baguio City – known as the “City of Pines” – holds the country’s major source of temperate climate vegetables. With increased dietary awareness, the consumption of plant foods rich in antioxidants has become relevant. Twenty-nine methanolic extracts from Baguio-produced plant foods were evaluated for antioxidant potential using DPPH, ferric reduction antioxidant power (FRAP), metal chelation, superoxide anion, nitric oxide, hydroxyl radical scavenging activities, MTT reduction, and phytochemical tests. Fagopyrum tataricum leaves, Vaccinium myrtoides fruit, and Morus alba fruit showed the most effective DPP radical, concentration-dependent reducing power, but low metal chelating activity. Solanum tuberosum tuber (22.86±63.26%) showed effective concentration-dependent chelating activity at 125 μg/mL. Citrus aurantium fruit (26.77±9.24%) and Raphanus raphanistrum root (41.13±0.11%) demonstrated an effective scavenging activity against superoxide anions at 45.5 μg/mL. Significant nitric oxide scavenging activity was observed in some fruits. Brassica oleracea Cab leaves (54.36 ± 2.38%) showed the highest inhibitory activity against hydroxyl radicals at 166.7 μg/mL. Phytochemical analyses showed that most plant samples revealed the presence of glycosides, terpenes/terpenoids, and steroids/phytosterols, while few contained phenolic and tannin components. These phytochemicals may explain the dual behavior as an antioxidant or a prooxidant observed. Thus, determining food antioxidant component types and their concentration is necessary to maximize the potential to scavenge oxidants.
{"title":"Antioxidant Activity and Phytochemicals of Locally Consumed Plant Foods from Baguio City, Philippines","authors":"P. R. Bueno, Rachel Camille R. Cabrera, G. F. Yu","doi":"10.33084/bjop.v6i2.4546","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4546","url":null,"abstract":"In the Philippines, Baguio City – known as the “City of Pines” – holds the country’s major source of temperate climate vegetables. With increased dietary awareness, the consumption of plant foods rich in antioxidants has become relevant. Twenty-nine methanolic extracts from Baguio-produced plant foods were evaluated for antioxidant potential using DPPH, ferric reduction antioxidant power (FRAP), metal chelation, superoxide anion, nitric oxide, hydroxyl radical scavenging activities, MTT reduction, and phytochemical tests. Fagopyrum tataricum leaves, Vaccinium myrtoides fruit, and Morus alba fruit showed the most effective DPP radical, concentration-dependent reducing power, but low metal chelating activity. Solanum tuberosum tuber (22.86±63.26%) showed effective concentration-dependent chelating activity at 125 μg/mL. Citrus aurantium fruit (26.77±9.24%) and Raphanus raphanistrum root (41.13±0.11%) demonstrated an effective scavenging activity against superoxide anions at 45.5 μg/mL. Significant nitric oxide scavenging activity was observed in some fruits. Brassica oleracea Cab leaves (54.36 ± 2.38%) showed the highest inhibitory activity against hydroxyl radicals at 166.7 μg/mL. Phytochemical analyses showed that most plant samples revealed the presence of glycosides, terpenes/terpenoids, and steroids/phytosterols, while few contained phenolic and tannin components. These phytochemicals may explain the dual behavior as an antioxidant or a prooxidant observed. Thus, determining food antioxidant component types and their concentration is necessary to maximize the potential to scavenge oxidants.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77400551","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}
F. A. Ugbe, Gideon Adamu Shallangwa, Shallangwa Adamu Uzairu, I. Abdulkadir
Filariasis (Lymphatic filariasis and Onchocerciasis) is a common neglected tropical disease caused by parasitic nematodes called filarial worms, which often host the Wolbachia bacteria. A good treatment approach seeks Wolbachia as a drug target. Here, a computer-aided design of some boron-pleuromutilin analogs was conducted using the ligand-based drug design approach while performing molecular docking investigation and pharmacokinetics analyses to evaluate their drug-likeness properties. The newly designed compounds (49a, 49b, and 49c) showed improved inhibitory activities (pEC50) over those of the template and the clinically relevant pleuromutilins (retapamulin and lefamulin) in the order; 49b (pEC50 = 9.0409) > 49c (8.8175) > 49a (8.5930) > template (49) (8.4222) > retapamulin (6.7403) > lefamulin (6.1369). Standard docking performed with OTU deubiquitinase (6W9O) revealed the order of binding energies; 49c (-88.07 kcal/mol) > 49b (-84.26 kcal/mol) > doxycycline (-83.70 kcal/mol) > template (-82.57 kcal/mol) > 49a (-78.43 kcal/mol) > lefamulin (-76.83 kcal/mol) > retapamulin (-76.78 kcal/mol), with the new compounds all showing good pharmacological interactions with the receptor’s amino acids. The new analogs were also predicted to be orally bioavailable with better pharmacokinetic profiles than the template, retapamulin, lefamulin, and doxycycline having no more than one violation of Lipinski’s ROF. Therefore, the newly designed compounds could be considered potential anti-filarial drug candidates.
{"title":"In-Silico Design and Evaluation of the Anti-Wolbachia Potential of Boron-Pleuromutilins","authors":"F. A. Ugbe, Gideon Adamu Shallangwa, Shallangwa Adamu Uzairu, I. Abdulkadir","doi":"10.33084/bjop.v6i2.4677","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4677","url":null,"abstract":"Filariasis (Lymphatic filariasis and Onchocerciasis) is a common neglected tropical disease caused by parasitic nematodes called filarial worms, which often host the Wolbachia bacteria. A good treatment approach seeks Wolbachia as a drug target. Here, a computer-aided design of some boron-pleuromutilin analogs was conducted using the ligand-based drug design approach while performing molecular docking investigation and pharmacokinetics analyses to evaluate their drug-likeness properties. The newly designed compounds (49a, 49b, and 49c) showed improved inhibitory activities (pEC50) over those of the template and the clinically relevant pleuromutilins (retapamulin and lefamulin) in the order; 49b (pEC50 = 9.0409) > 49c (8.8175) > 49a (8.5930) > template (49) (8.4222) > retapamulin (6.7403) > lefamulin (6.1369). Standard docking performed with OTU deubiquitinase (6W9O) revealed the order of binding energies; 49c (-88.07 kcal/mol) > 49b (-84.26 kcal/mol) > doxycycline (-83.70 kcal/mol) > template (-82.57 kcal/mol) > 49a (-78.43 kcal/mol) > lefamulin (-76.83 kcal/mol) > retapamulin (-76.78 kcal/mol), with the new compounds all showing good pharmacological interactions with the receptor’s amino acids. The new analogs were also predicted to be orally bioavailable with better pharmacokinetic profiles than the template, retapamulin, lefamulin, and doxycycline having no more than one violation of Lipinski’s ROF. Therefore, the newly designed compounds could be considered potential anti-filarial drug candidates.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"114 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79228330","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}
Lisza Niarisessa, A. Puspitaningrum, Arief Rahman Afief, D. Perwitasari, Wirawan Adikusuma, Rocky Cheung, A. Septama, Lalu Muhammad Irham
Psoriasis is an autoimmune disease that causes inflammation on the skin's surface, characterized by the appearance of pink plaques covered with white scales. Currently, the availability of psoriasis vulgaris therapy is still limited. Therefore, considering the discovery of new drug candidates by utilizing genetic variations, such as single nucleotide polymorphisms (SNP) through drug repurposing, is a profitable method. The SNP associated with psoriasis was obtained from Genome-Wide Association Studies (GWAS) and Phenom-Wide Association Studies (PheWAS) databases. We identified 245 SNPs associated with psoriasis vulgaris with criteria of r2 >0.8. To prioritize the candidate of a gene associated with psoriasis, we used five criteria of functional annotation (missense/nonsense, cis-eQTL, PPI, KEGG, and KO mice) where if there were more than two criteria of assessment, they were defined as the risk gene of psoriasis vulgaris. Fifty-two genes were identified as the risk gene of psoriasis vulgaris, then expanded using the STRING database to obtain more gene candidates of drug targets. The result is 104 genes candidates for drug targets, of which 24 overlapped with 96 drugs, according to DrugBank. Of the 96 drugs that have been approved for other indications, we found that five drugs (ustekinumab, tildrakizumab, risankizumab, guselkumab, and etanercept) are currently in clinical trials for the treatment of psoriasis that target two genes (IL23A and TNF). We argue that these two genes are the most promising targets based on their high target scores on functional annotations. This research explains the potential that utilizing genomic variation can contribute to drug discovery.
{"title":"Identification of Biological Risk Genes and Candidate Drugs for Psoriasis Vulgaris by Utilizing the Genomic Information","authors":"Lisza Niarisessa, A. Puspitaningrum, Arief Rahman Afief, D. Perwitasari, Wirawan Adikusuma, Rocky Cheung, A. Septama, Lalu Muhammad Irham","doi":"10.33084/bjop.v6i2.4217","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4217","url":null,"abstract":"Psoriasis is an autoimmune disease that causes inflammation on the skin's surface, characterized by the appearance of pink plaques covered with white scales. Currently, the availability of psoriasis vulgaris therapy is still limited. Therefore, considering the discovery of new drug candidates by utilizing genetic variations, such as single nucleotide polymorphisms (SNP) through drug repurposing, is a profitable method. The SNP associated with psoriasis was obtained from Genome-Wide Association Studies (GWAS) and Phenom-Wide Association Studies (PheWAS) databases. We identified 245 SNPs associated with psoriasis vulgaris with criteria of r2 >0.8. To prioritize the candidate of a gene associated with psoriasis, we used five criteria of functional annotation (missense/nonsense, cis-eQTL, PPI, KEGG, and KO mice) where if there were more than two criteria of assessment, they were defined as the risk gene of psoriasis vulgaris. Fifty-two genes were identified as the risk gene of psoriasis vulgaris, then expanded using the STRING database to obtain more gene candidates of drug targets. The result is 104 genes candidates for drug targets, of which 24 overlapped with 96 drugs, according to DrugBank. Of the 96 drugs that have been approved for other indications, we found that five drugs (ustekinumab, tildrakizumab, risankizumab, guselkumab, and etanercept) are currently in clinical trials for the treatment of psoriasis that target two genes (IL23A and TNF). We argue that these two genes are the most promising targets based on their high target scores on functional annotations. This research explains the potential that utilizing genomic variation can contribute to drug discovery.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85378971","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}
Norfloxacin is an antimicrobial in treating urinary tract infections with low water solubility. This study aims to know the effect of norfloxacin-urea co-crystal formation on the solubility of norfloxacin and the potential for scale-up when prepared by ultrasound-assisted slurry co-crystallization method. Identification of the screening result of the norfloxacin-urea (1 : 1) co-crystal formation by a wet grinding method using an ethanol-acetone (1 : 1) solvent mixture was performed by powder X-ray diffractometer (PXRD). The ultrasound-assisted slurry co-crystallization method was used for co-crystal formation with five-fold the weight of norfloxacin and urea than the wet grinding method. The co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was observed for its crystal morphology and characterized by PXRD and differential scanning calorimeter (DSC). Solubility and dissolution tests in water and acetate buffer solution pH 4.0 were used to evaluate the physicochemical properties. Identification of co-crystal screening by PXRD revealed the formation of norfloxacin-urea co-crystal. The PXRD pattern of the norfloxacin-urea co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was similar to the wet grinding method. Norfloxacin-urea co-crystal has a different melting point and crystal morphology from pure norfloxacin and urea. The solubility and dissolution rate of norfloxacin-urea co-crystal was higher in water and not significantly different in acetate buffer solution pH 4.0 compared to pure norfloxacin. This study showed that the norfloxacin-urea co-crystal formation could enhance the solubility of norfloxacin in water and had the potential for scale-up when prepared using the ultrasound-assisted slurry co-crystallization method.
{"title":"Solubility and Scale-Up Potency of Norfloxacin-Urea Co-Crystal Prepared by Ultrasound-Assisted Slurry Co-Crystallization Method","authors":"Fikri Alatas, Dery Stiawan, Nur Achsan Al-Hakim","doi":"10.33084/bjop.v6i2.4173","DOIUrl":"https://doi.org/10.33084/bjop.v6i2.4173","url":null,"abstract":"Norfloxacin is an antimicrobial in treating urinary tract infections with low water solubility. This study aims to know the effect of norfloxacin-urea co-crystal formation on the solubility of norfloxacin and the potential for scale-up when prepared by ultrasound-assisted slurry co-crystallization method. Identification of the screening result of the norfloxacin-urea (1 : 1) co-crystal formation by a wet grinding method using an ethanol-acetone (1 : 1) solvent mixture was performed by powder X-ray diffractometer (PXRD). The ultrasound-assisted slurry co-crystallization method was used for co-crystal formation with five-fold the weight of norfloxacin and urea than the wet grinding method. The co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was observed for its crystal morphology and characterized by PXRD and differential scanning calorimeter (DSC). Solubility and dissolution tests in water and acetate buffer solution pH 4.0 were used to evaluate the physicochemical properties. Identification of co-crystal screening by PXRD revealed the formation of norfloxacin-urea co-crystal. The PXRD pattern of the norfloxacin-urea co-crystal product prepared by the ultrasound-assisted slurry co-crystallization method was similar to the wet grinding method. Norfloxacin-urea co-crystal has a different melting point and crystal morphology from pure norfloxacin and urea. The solubility and dissolution rate of norfloxacin-urea co-crystal was higher in water and not significantly different in acetate buffer solution pH 4.0 compared to pure norfloxacin. This study showed that the norfloxacin-urea co-crystal formation could enhance the solubility of norfloxacin in water and had the potential for scale-up when prepared using the ultrasound-assisted slurry co-crystallization method.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89759853","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}
Asma Lanuddin, Sari Wijayanti, Irma Novrianti, Dhea Erwina Suwanty
World Health Organization menetapkan Corona virus disease sebagai pandemi pada tahun 2020. Dua warga Indonesia terkonfirmasi Covid-19 saat awal virus tersebut terdeteksi. Panic buying dalam memenuhi kebutuhan sehari-hari adalah salah satu dampak yang ditimbulkan dari covid-19 terutama suplemen kesehatan seperti vitamin ataupun imunnomodulator dikarenakan kurangnya pemahaman dari masyarakat. Penelitian ini bertujuan untuk mengetahui pengaruh Covid-19 terhadap penjualan produk suplemen kesehatan di apotek “X” kota Tarakan. Penelitian ini merupakan penelitian analitik yang bersifat observasional. Data diperoleh dari dokumen penjualan di apotek “X” pada 12 bulan sebelum dan 12 bulan awal pandemi Covid-19. Adapun suplemen kesehatan yang diambil untuk penelitian ini adalah Becom C®, Becom Zet®, dan Imboost Force®. Data yang diperoleh dianalisis menggunakan paired sample T test. Dari hasil penelitian diketahui, bahwa suplemen kesehatan mengalami peningkatan penjualan yakni sebesar 314,41% - 808,42% dengan nilai P = 0,038 untuk Becom C®, 0,039 untuk Becom Zet® dan 0,011 untuk Imboost Force®. Dapat disimpulkan Covid-19 memberikan pengaruh positif terhadap peningkatan penjualan produk suplemen kesehatan di apotek “X” kota Tarakan.
{"title":"Pengaruh Pandemı Covıd-19 terhadap Penjualan Suplemen Kesehatan dı Apotek “X” Kota Tarakan","authors":"Asma Lanuddin, Sari Wijayanti, Irma Novrianti, Dhea Erwina Suwanty","doi":"10.57174/jborn.v3i1.76","DOIUrl":"https://doi.org/10.57174/jborn.v3i1.76","url":null,"abstract":"World Health Organization menetapkan Corona virus disease sebagai pandemi pada tahun 2020. Dua warga Indonesia terkonfirmasi Covid-19 saat awal virus tersebut terdeteksi. Panic buying dalam memenuhi kebutuhan sehari-hari adalah salah satu dampak yang ditimbulkan dari covid-19 terutama suplemen kesehatan seperti vitamin ataupun imunnomodulator dikarenakan kurangnya pemahaman dari masyarakat. Penelitian ini bertujuan untuk mengetahui pengaruh Covid-19 terhadap penjualan produk suplemen kesehatan di apotek “X” kota Tarakan. Penelitian ini merupakan penelitian analitik yang bersifat observasional. Data diperoleh dari dokumen penjualan di apotek “X” pada 12 bulan sebelum dan 12 bulan awal pandemi Covid-19. Adapun suplemen kesehatan yang diambil untuk penelitian ini adalah Becom C®, Becom Zet®, dan Imboost Force®. Data yang diperoleh dianalisis menggunakan paired sample T test. Dari hasil penelitian diketahui, bahwa suplemen kesehatan mengalami peningkatan penjualan yakni sebesar 314,41% - 808,42% dengan nilai P = 0,038 untuk Becom C®, 0,039 untuk Becom Zet® dan 0,011 untuk Imboost Force®. Dapat disimpulkan Covid-19 memberikan pengaruh positif terhadap peningkatan penjualan produk suplemen kesehatan di apotek “X” kota Tarakan.","PeriodicalId":9118,"journal":{"name":"Borneo Journal of Pharmacy","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91321210","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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