Pub Date : 2023-12-12DOI: 10.3897/pharmacia.70.e109965
Alexandra Petrova, Rumyana Simeonova, C. Voycheva, Yonko Savov, Lyubomir Marinov, V. Balabanova, R. Gevrenova, D. Zheleva-Dimitrova
The high-fat (HF) diets can be used to generate a valid rodent model for metabolic syndrome (METS). The aim of this study was to compare three different diets, namely a high-fat, high-carbohydrate diet (HF-HCD), a high-fat lard-based diet (HFD), and a cafeteria diet (CFD), in terms of the ability to induce METS. The next step was to characterize the syndrome according to the biochemical and histopathological changes in the liver and pancreas, and to determine the optimal animal model. As a result, all diets disturbed significantly the serum biochemical parameters. HF-HCD and CFD increased the uric acid levels and reduced the weight gain in comparison with the standard chow diet (SCD) and HFD. The HFD and CFD induced the highest fasting glycemia levels. Although the animals fed with HF-HCD had the lowest body weight, the most serious histopathological changes in the pancreas, hypertension, and oxidative stress were noted in them.
{"title":"Metabolic syndrome: comparison of three diet-induced experimental models","authors":"Alexandra Petrova, Rumyana Simeonova, C. Voycheva, Yonko Savov, Lyubomir Marinov, V. Balabanova, R. Gevrenova, D. Zheleva-Dimitrova","doi":"10.3897/pharmacia.70.e109965","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109965","url":null,"abstract":"The high-fat (HF) diets can be used to generate a valid rodent model for metabolic syndrome (METS). The aim of this study was to compare three different diets, namely a high-fat, high-carbohydrate diet (HF-HCD), a high-fat lard-based diet (HFD), and a cafeteria diet (CFD), in terms of the ability to induce METS. The next step was to characterize the syndrome according to the biochemical and histopathological changes in the liver and pancreas, and to determine the optimal animal model. As a result, all diets disturbed significantly the serum biochemical parameters. HF-HCD and CFD increased the uric acid levels and reduced the weight gain in comparison with the standard chow diet (SCD) and HFD. The HFD and CFD induced the highest fasting glycemia levels. Although the animals fed with HF-HCD had the lowest body weight, the most serious histopathological changes in the pancreas, hypertension, and oxidative stress were noted in them.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"9 6","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139009059","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 : 2023-12-12DOI: 10.3897/pharmacia.70.e109119
Yasmiwar Susilawati, R. M. Febriyanti, E. Febrina, A. Chaerunisaa, S. Sumiwi
Background: Roselle (Hibiscus sabdariffa L.) calyces have been used in traditional medicine as diuretics, mild laxatives, and antihypertensive agents but to date, a comprehensive study of its pharmacological activity and safety has not been conducted. Aims of the study: The current study aims to provide a comprehensive evaluation of the antihypertensive efficacy and toxicity profile of Roselle (H. sabdariffa L.) calyces extract. Utilizing animal models, the investigation assessed the dose-dependent pharmacological effects and safety of H. sabdariffa L. Results: The findings indicate that the extract exerts a significant antihypertensive effect at a dose of 250 mg/kg body weight (BW), lowering systolic and diastolic blood pressures by 10.12% and 11.63%, respectively. Ethyl acetate fractions administered at 112.5 mg/kg BW demonstrated greater efficacy than n-hexane and aqueous fractions, suggesting that the active compounds likely possess semi-polar properties. Acute toxicity testing yielded an LD50 of 8.75 g/kg BW for male rats and 7.5 g/kg BW for female rats, classifying the extract as slightly toxic. The sub-chronic toxicity study shows that H. sabdariffa L. demonstrates an effect on bodyweight and urea levels in male and female rats, while the change in the blood parameters, creatinine level, and the liver index was only observed in female rats. Conclusions: These data suggest that H. sabdariffa L. extract exhibits therapeutic promise but should be administered cautiously, preferably at doses lower than 250 mg/kg BW, due to potential toxicity.
{"title":"A comprehensive in vivo study of the antihypertensive properties and toxicity of roselle (Hibiscus sabdariffa L.)","authors":"Yasmiwar Susilawati, R. M. Febriyanti, E. Febrina, A. Chaerunisaa, S. Sumiwi","doi":"10.3897/pharmacia.70.e109119","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e109119","url":null,"abstract":"Background: Roselle (Hibiscus sabdariffa L.) calyces have been used in traditional medicine as diuretics, mild laxatives, and antihypertensive agents but to date, a comprehensive study of its pharmacological activity and safety has not been conducted.\u0000 Aims of the study: The current study aims to provide a comprehensive evaluation of the antihypertensive efficacy and toxicity profile of Roselle (H. sabdariffa L.) calyces extract. Utilizing animal models, the investigation assessed the dose-dependent pharmacological effects and safety of H. sabdariffa L.\u0000 Results: The findings indicate that the extract exerts a significant antihypertensive effect at a dose of 250 mg/kg body weight (BW), lowering systolic and diastolic blood pressures by 10.12% and 11.63%, respectively. Ethyl acetate fractions administered at 112.5 mg/kg BW demonstrated greater efficacy than n-hexane and aqueous fractions, suggesting that the active compounds likely possess semi-polar properties. Acute toxicity testing yielded an LD50 of 8.75 g/kg BW for male rats and 7.5 g/kg BW for female rats, classifying the extract as slightly toxic. The sub-chronic toxicity study shows that H. sabdariffa L. demonstrates an effect on bodyweight and urea levels in male and female rats, while the change in the blood parameters, creatinine level, and the liver index was only observed in female rats. Conclusions: These data suggest that H. sabdariffa L. extract exhibits therapeutic promise but should be administered cautiously, preferably at doses lower than 250 mg/kg BW, due to potential toxicity.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"10 10","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139009220","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 : 2023-12-12DOI: 10.3897/pharmacia.70.e107698
Viktor V. Yotov, Raina Ardasheva, A. Mihaylova, N. Doncheva, Ilia Kostadinov, V. Turiyski
Weightlessness significantly impacts physiological systems. In the current study, we investigate the effects of 7 days exposure of rats to simulated microgravity (using a modified rat-modeled random positioning machine, working with four experimental animals simultaneously) on local carrageenan-induced inflammation and serum levels of liver enzymes, metabolites (glucose, urea, creatinine), and metabolic hormones (thyroid-stimulating hormone – TSH, aldosterone, cortisol). Male Wistar rats (n=12, m=200 ± 20 g) were evenly divided into RPM (experimental) and RPM-K (control) groups. The RPM rats showed a notable mass decrease compared to the controls. A significant increase in the carrageenan-induced inflammatory response was reached on the 24th hour in the RPM group compared to the RPM-K. Simulated microgravity resulted in lower serum glucose, creatinine, cortisol, and elevated urea levels. In conclusion, 7 days of exposure to random positioning machine-simulated microgravity promotes a pro-inflammatory state, potentially affecting insulin sensitivity, glucose utilization, and muscle catabolism.
{"title":"Simulated microgravity affects carrageenan-induced inflammation process in rats","authors":"Viktor V. Yotov, Raina Ardasheva, A. Mihaylova, N. Doncheva, Ilia Kostadinov, V. Turiyski","doi":"10.3897/pharmacia.70.e107698","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e107698","url":null,"abstract":"Weightlessness significantly impacts physiological systems. In the current study, we investigate the effects of 7 days exposure of rats to simulated microgravity (using a modified rat-modeled random positioning machine, working with four experimental animals simultaneously) on local carrageenan-induced inflammation and serum levels of liver enzymes, metabolites (glucose, urea, creatinine), and metabolic hormones (thyroid-stimulating hormone – TSH, aldosterone, cortisol). Male Wistar rats (n=12, m=200 ± 20 g) were evenly divided into RPM (experimental) and RPM-K (control) groups. The RPM rats showed a notable mass decrease compared to the controls. A significant increase in the carrageenan-induced inflammatory response was reached on the 24th hour in the RPM group compared to the RPM-K. Simulated microgravity resulted in lower serum glucose, creatinine, cortisol, and elevated urea levels. In conclusion, 7 days of exposure to random positioning machine-simulated microgravity promotes a pro-inflammatory state, potentially affecting insulin sensitivity, glucose utilization, and muscle catabolism.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"40 8","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139008401","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 : 2023-12-11DOI: 10.3897/pharmacia.70.e114080
N. Penkova, Pepa Atanasova, R. Penkov, P. Hrischev, L. Peychev, Z. Peychev
Background: Local regulation of gastrointestinal tract digestion is performed by a large number of hormones produced by the mucosal enteroendocrine cells. Some of the earliest differentiating cells in the gastrointestinal tract are enteroendocrine cells. Serotonin-producing cells - EC cells are found mostly in the stomach and duodenum. Aim: The aim of our study is to establish the presence and to make morphological and morphofunctional characteristic of ЕС cells in the developing gastrointestinal tract of a human. Materials and methods: Our study was performed with biopsy specimen from human stomach and duodenum and fragments of gastrointestinal tract of human embryos 6th gestation week, studied by immunohistochemical, electron microscopy and morphometric methods. Results: EC cells have already been differentiated in the 6th gestation week. Embryonic EC cells had identical characteristics with those of adults. They were in two morphofunctional conditions: stage of increased synthesis and stage of relative secretory rest. Conclusion: In the early embryonic period - 6th gestation week EC cells have already been differentiated. The occurrence of EC cells with hormonal production prior to the definitive differentiation of tissues presupposes participation of serotonin in the digestive tube histogenetic processes.
{"title":"Serotonin production of the developing gastrointestinal tract of human embryos in 6th gestation week","authors":"N. Penkova, Pepa Atanasova, R. Penkov, P. Hrischev, L. Peychev, Z. Peychev","doi":"10.3897/pharmacia.70.e114080","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114080","url":null,"abstract":"Background: Local regulation of gastrointestinal tract digestion is performed by a large number of hormones produced by the mucosal enteroendocrine cells. Some of the earliest differentiating cells in the gastrointestinal tract are enteroendocrine cells. Serotonin-producing cells - EC cells are found mostly in the stomach and duodenum.\u0000 Aim: The aim of our study is to establish the presence and to make morphological and morphofunctional characteristic of ЕС cells in the developing gastrointestinal tract of a human.\u0000 Materials and methods: Our study was performed with biopsy specimen from human stomach and duodenum and fragments of gastrointestinal tract of human embryos 6th gestation week, studied by immunohistochemical, electron microscopy and morphometric methods.\u0000 Results: EC cells have already been differentiated in the 6th gestation week. Embryonic EC cells had identical characteristics with those of adults. They were in two morphofunctional conditions: stage of increased synthesis and stage of relative secretory rest.\u0000 Conclusion: In the early embryonic period - 6th gestation week EC cells have already been differentiated. The occurrence of EC cells with hormonal production prior to the definitive differentiation of tissues presupposes participation of serotonin in the digestive tube histogenetic processes.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"45 8","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139010358","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 : 2023-12-11DOI: 10.3897/pharmacia.70.e114927
Thana Thanayutsiri, Thapakorn Charoenying, Prasopchai Patrojanasophon, Boonnada Pamornpathomkul, P. Opanasopit, T. Ngawhirunpat, T. Rojanarata, Prasopchai Patrojanasophon
A new assay of captopril (CTP) tablets was developed based on digital image colorimetry using Ellman’s reagent. For the first time, a facile technique of increasing the analytical path was applied in this work to enhance the sensitivity. For this purpose, the reaction solutions were photographed using a smartphone while they were contained in two 1-cm pathlength cuvettes which were placed side by side. The Red-Green-Blue (RGB) in term of [B/(R+G+B)] was used to plot a standard curve. Compared to using a single cuvette, double cuvettes resulted in more precise analytical signals and better linearity (r2 of 0.9992). Additionally, CTP could be analyzed at low concentrations (2.5–25 µM) with LOD of 0.70 µM and LOQ of 2.13 µM, thus lowering the reagent consumption. The assay was proven to be valid, and it was greener, faster, and more affordable than the pharmacopeial chromatographic method, thereby suitable for pharmaceutical quality control.
{"title":"Facile, sensitive and reagent-saving smartphone-based digital image colorimetric assay of captopril tablets enabled by long-pathlength RGB acquisition","authors":"Thana Thanayutsiri, Thapakorn Charoenying, Prasopchai Patrojanasophon, Boonnada Pamornpathomkul, P. Opanasopit, T. Ngawhirunpat, T. Rojanarata, Prasopchai Patrojanasophon","doi":"10.3897/pharmacia.70.e114927","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114927","url":null,"abstract":"A new assay of captopril (CTP) tablets was developed based on digital image colorimetry using Ellman’s reagent. For the first time, a facile technique of increasing the analytical path was applied in this work to enhance the sensitivity. For this purpose, the reaction solutions were photographed using a smartphone while they were contained in two 1-cm pathlength cuvettes which were placed side by side. The Red-Green-Blue (RGB) in term of [B/(R+G+B)] was used to plot a standard curve. Compared to using a single cuvette, double cuvettes resulted in more precise analytical signals and better linearity (r2 of 0.9992). Additionally, CTP could be analyzed at low concentrations (2.5–25 µM) with LOD of 0.70 µM and LOQ of 2.13 µM, thus lowering the reagent consumption. The assay was proven to be valid, and it was greener, faster, and more affordable than the pharmacopeial chromatographic method, thereby suitable for pharmaceutical quality control.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"38 9","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139010452","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 : 2023-12-08DOI: 10.3897/pharmacia.70.e108670
Wafaa Yusuf Khalaf, Rita Sabah Elias, Leaqaa Abdulredha Raheem
A new eight series of 3-(2-oxo-2H-chromen-3-yl)-5-(substituted phenyl)-1H-pyrazole-1-carbaldehyde derivatives (9–16) were designed and created from coumarin-chalcone derivatives (1–8). The structures of the derivatives were established by using melting point, mass spectrum, IR, 1HNMR, and 13C NMR spectroscopic methods. In vitro antiproliferative activities were evaluated against MCF-7 breast cancer cell line using Microculture Tetrazolium (MTT) assay. The results showed that the compounds 9, 12- 14 has a moderate activity against MCF-7 breast cancer cell line with IC50 61.44, 70.11, 22.6 and 25.99 µg/mL respectively, while the compounds 10,11, 15 and 16 were found to be inactive against studied cell line within IC50 > 100 µg/mL. The possible binding interaction between studied compounds (9–16) and human ER-α (PDB ID: 1ERR) were studied by molecular docking. The results revealed that only the compounds 11 and 16 form π -H interaction with ER-α (PDB ID: 1ERR) within the highest negative values of binding affinity -7.04260 and -7.17308 kcal.mol-1 respectively than the other compounds, while Raloxifene used here as a positive control form a strong ionic bonding with Asp 351 within the binding affinity -9.61928 kcal/mol which is more negative value than the studied compounds.
{"title":"Design, synthesis and molecular docking study of coumarin pyrazoline derivatives against MCF-7 breast cancer cell line","authors":"Wafaa Yusuf Khalaf, Rita Sabah Elias, Leaqaa Abdulredha Raheem","doi":"10.3897/pharmacia.70.e108670","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e108670","url":null,"abstract":"A new eight series of 3-(2-oxo-2H-chromen-3-yl)-5-(substituted phenyl)-1H-pyrazole-1-carbaldehyde derivatives (9–16) were designed and created from coumarin-chalcone derivatives (1–8). The structures of the derivatives were established by using melting point, mass spectrum, IR, 1HNMR, and 13C NMR spectroscopic methods. In vitro antiproliferative activities were evaluated against MCF-7 breast cancer cell line using Microculture Tetrazolium (MTT) assay. The results showed that the compounds 9, 12- 14 has a moderate activity against MCF-7 breast cancer cell line with IC50 61.44, 70.11, 22.6 and 25.99 µg/mL respectively, while the compounds 10,11, 15 and 16 were found to be inactive against studied cell line within IC50 > 100 µg/mL. The possible binding interaction between studied compounds (9–16) and human ER-α (PDB ID: 1ERR) were studied by molecular docking. The results revealed that only the compounds 11 and 16 form π -H interaction with ER-α (PDB ID: 1ERR) within the highest negative values of binding affinity -7.04260 and -7.17308 kcal.mol-1 respectively than the other compounds, while Raloxifene used here as a positive control form a strong ionic bonding with Asp 351 within the binding affinity -9.61928 kcal/mol which is more negative value than the studied compounds.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"30 48","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138588992","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 : 2023-12-08DOI: 10.3897/pharmacia.70.e115762
Y. Assyov, Iliana Ganeva, Stefan Ikonomov, Iveta Nedeva, Toni Velikov, Z. Kamenov, T. Velikova
This review explores the intricate relationship between interleukin-6 (IL-6) and sarcopenia, a prevalent condition characterized by progressive skeletal muscle loss, particularly in aging populations. Emphasizing the rising prevalence and health challenges posed by sarcopenia, the paper delves into the multifunctional roles of IL-6 in immune response, inflammation and inflammaging associated with sarcopenia. Significantly elevated in sarcopenic individuals, IL-6 prompts an exploration of its molecular impact on muscle wasting. The review critically assesses IL-6 as a potential biomarker for sarcopenia diagnosis and prognosis while also examining therapeutic interventions targeting IL-6 signaling pathways, offering a foundation for future research and the development of targeted therapeutic strategies to alleviate the impact of this debilitating condition.
{"title":"Interleukin-6: Unravelling its role in sarcopenia pathogenesis and exploring therapeutic avenues","authors":"Y. Assyov, Iliana Ganeva, Stefan Ikonomov, Iveta Nedeva, Toni Velikov, Z. Kamenov, T. Velikova","doi":"10.3897/pharmacia.70.e115762","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e115762","url":null,"abstract":"This review explores the intricate relationship between interleukin-6 (IL-6) and sarcopenia, a prevalent condition characterized by progressive skeletal muscle loss, particularly in aging populations. Emphasizing the rising prevalence and health challenges posed by sarcopenia, the paper delves into the multifunctional roles of IL-6 in immune response, inflammation and inflammaging associated with sarcopenia. Significantly elevated in sarcopenic individuals, IL-6 prompts an exploration of its molecular impact on muscle wasting. The review critically assesses IL-6 as a potential biomarker for sarcopenia diagnosis and prognosis while also examining therapeutic interventions targeting IL-6 signaling pathways, offering a foundation for future research and the development of targeted therapeutic strategies to alleviate the impact of this debilitating condition.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"76 6","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138587043","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 : 2023-12-07DOI: 10.3897/pharmacia.70.e112271
I. Sopyan, Wuri Ariestika Sari, S. Megantara, T. Rusdiana
A Carvedilol is a member of BCS class II, it has a low solubility and bioavailability. This work intends to increase the solubility of carvedilol using a multicomponent crystal method. Based on in silico investigations showed that carvedilol-arginine formed one hydrogen bond and carvedilol-glycine formed two hydrogen bonds. Compared to the solubility of pure carvedilol, CVD: GLY multicomponent crystal ratios of 1:1, 1:2, and 2:1 resulted in increases in solubility of 1.9 times, 2.6 times, and 2.5 times respectively. The solubility of the multicomponent crystals in the CVD:ARG however, did not increase. The best dissolution profile was provided by multicomponent crystal CVD: GLY (1:2), with a % dissolution of 86.03% in HCl medium pH 1.45 and 29.5% in phosphate buffer medium pH 6.8. The results of characterization included FTIR, DSC, PXRD, and SEM evaluation of CVD: GLY multicomponent crystal (1:2) indicated the formation of a new solid crystalin phase. CVD: GLY multicomponent crystal (1:2) showing the best solubility and dissolution profile as compared to pure carvedilol.
{"title":"Solubility enhancement of carvedilol by multicomponent crystal approach using glycine and arginine as coformers","authors":"I. Sopyan, Wuri Ariestika Sari, S. Megantara, T. Rusdiana","doi":"10.3897/pharmacia.70.e112271","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e112271","url":null,"abstract":"A Carvedilol is a member of BCS class II, it has a low solubility and bioavailability. This work intends to increase the solubility of carvedilol using a multicomponent crystal method. Based on in silico investigations showed that carvedilol-arginine formed one hydrogen bond and carvedilol-glycine formed two hydrogen bonds. Compared to the solubility of pure carvedilol, CVD: GLY multicomponent crystal ratios of 1:1, 1:2, and 2:1 resulted in increases in solubility of 1.9 times, 2.6 times, and 2.5 times respectively. The solubility of the multicomponent crystals in the CVD:ARG however, did not increase. The best dissolution profile was provided by multicomponent crystal CVD: GLY (1:2), with a % dissolution of 86.03% in HCl medium pH 1.45 and 29.5% in phosphate buffer medium pH 6.8. The results of characterization included FTIR, DSC, PXRD, and SEM evaluation of CVD: GLY multicomponent crystal (1:2) indicated the formation of a new solid crystalin phase. CVD: GLY multicomponent crystal (1:2) showing the best solubility and dissolution profile as compared to pure carvedilol.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"115 7","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138590722","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 beginning of the twenty-first century, obesity has become a concerning world-wide issue due to its high prevalence in modern society. It is a metabolic disorder, caused by excessive accumulation of adipose tissue in the human organism – the main reason for which is increased caloric intake and decreased caloric expenditure in combination with dysregulation of hunger. It is a chronic systematic disease that leads to the development of a large number of health complications, the most common of which are: diabetes mellitus type 2, arterial hypertension, atherosclerosis, sleep apnea, different types of cancer and more. During the last decade, significant advancements have been made in regard to treatment of many endocrine and metabolic conditions, using pharmacological means, and some of these novel medications have proven to be an effective therapy for obesity. There is emerging evidence that such drugs can exhibit an effect over the human gut microbiota – the complex system of commensal bacteria located in the gastrointestinal tract, which could affect appetite, mucosal integrity, nutrient absorption, and that interaction can be the key to understanding the pathogenesis of obesity and its treatment.
{"title":"Pharmacological methods for weight reduction and their connection with the human gut microbiota","authors":"Venelin Dimitrov Denchev, Teodora Svetoslavova Handjieva-Darlenska","doi":"10.3897/pharmacia.70.e114567","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114567","url":null,"abstract":"In the beginning of the twenty-first century, obesity has become a concerning world-wide issue due to its high prevalence in modern society. It is a metabolic disorder, caused by excessive accumulation of adipose tissue in the human organism – the main reason for which is increased caloric intake and decreased caloric expenditure in combination with dysregulation of hunger. It is a chronic systematic disease that leads to the development of a large number of health complications, the most common of which are: diabetes mellitus type 2, arterial hypertension, atherosclerosis, sleep apnea, different types of cancer and more.\u0000 During the last decade, significant advancements have been made in regard to treatment of many endocrine and metabolic conditions, using pharmacological means, and some of these novel medications have proven to be an effective therapy for obesity. There is emerging evidence that such drugs can exhibit an effect over the human gut microbiota – the complex system of commensal bacteria located in the gastrointestinal tract, which could affect appetite, mucosal integrity, nutrient absorption, and that interaction can be the key to understanding the pathogenesis of obesity and its treatment.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"26 26","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138602627","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 : 2023-12-04DOI: 10.3897/pharmacia.70.e112502
A. M. Muhar, Adrian Joshua Velaro, Arya Tjipta Prananda, S. E. Nugraha, Gamze Çamlik, Siddhanshu Wasnik, Satirah Zainal Abidin, O. Sjofjan, Muhammad Andika Yudha Harahap, Muhammad Faridz Syahrian, N. Taslim, N. Mayulu, H. Permatasari, F. Nurkolis, Putri Cahaya Situmorang, R. A. Syahputra
Polyscias scutellaria (PS), an increasingly recognized botanical marvel, has emerged as a remarkable reservoir of natural antioxidants and anti-inflammatory compounds, holding immense potential for enhancing health and promoting overall well-being. In this comprehensive investigation, we meticulously examined the multifaceted properties of PS through various parameters, including DPPH scavenging activity, total phenol, and total flavonoid content in its ethanol extract (EEPS), ethyl acetate extract (EAPS), and n-hexane extract (nhPS). Additionally, we conducted in-depth assessments of cellular responses to EEPS and EAPS, encompassing cell viability, nitric oxide (NO) production, and the modulation of pivotal pro-inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), interleukin-1β (IL-1β), and interleukin-12 (IL-12), utilizing the RAW 264.7 cell line as a model system.Our findings illuminate the exceptional antioxidant prowess of PS extracts, with EEPS, EAPS, and nhPS displaying noteworthy DPPH scavenging activities. These results underscore their potential in quenching harmful free radicals and mitigating oxidative stress. Furthermore, our investigation unveils the promising anti-inflammatory attributes of EEPS and EAPS, as evidenced by their capacity to preserve cellular viability, dampen NO production, and suppress the secretion of critical pro-inflammatory mediators (TNF-α, IL-6, IL-1β, and IL-12) in RAW 264.7 cells. These remarkable anti-inflammatory effects hint at the therapeutic potential of PS in ameliorating chronic inflammatory conditions and bolstering the body’s immune response.In conclusion, Polyscias scutellaria stands as an emerging botanical champion, offering a wealth of natural antioxidants and anti-inflammatory compounds that hold great promise for optimizing health and well-being. This study opens exciting avenues for future research to elucidate the precise bioactive constituents within PS and unravel their intricate mechanisms of action, paving the way for the development of innovative therapeutic interventions and wellness-enhancing products. The remarkable properties of PS underscore its potential as a cornerstone of holistic health and a valuable asset in the pursuit of a vibrant and balanced life. Graphical abstract
{"title":"Polyscias scutellaria: An emerging source of natural antioxidants and anti-inflammatory compounds for health","authors":"A. M. Muhar, Adrian Joshua Velaro, Arya Tjipta Prananda, S. E. Nugraha, Gamze Çamlik, Siddhanshu Wasnik, Satirah Zainal Abidin, O. Sjofjan, Muhammad Andika Yudha Harahap, Muhammad Faridz Syahrian, N. Taslim, N. Mayulu, H. Permatasari, F. Nurkolis, Putri Cahaya Situmorang, R. A. Syahputra","doi":"10.3897/pharmacia.70.e112502","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e112502","url":null,"abstract":"Polyscias scutellaria (PS), an increasingly recognized botanical marvel, has emerged as a remarkable reservoir of natural antioxidants and anti-inflammatory compounds, holding immense potential for enhancing health and promoting overall well-being. In this comprehensive investigation, we meticulously examined the multifaceted properties of PS through various parameters, including DPPH scavenging activity, total phenol, and total flavonoid content in its ethanol extract (EEPS), ethyl acetate extract (EAPS), and n-hexane extract (nhPS). Additionally, we conducted in-depth assessments of cellular responses to EEPS and EAPS, encompassing cell viability, nitric oxide (NO) production, and the modulation of pivotal pro-inflammatory cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), interleukin-1β (IL-1β), and interleukin-12 (IL-12), utilizing the RAW 264.7 cell line as a model system.Our findings illuminate the exceptional antioxidant prowess of PS extracts, with EEPS, EAPS, and nhPS displaying noteworthy DPPH scavenging activities. These results underscore their potential in quenching harmful free radicals and mitigating oxidative stress. Furthermore, our investigation unveils the promising anti-inflammatory attributes of EEPS and EAPS, as evidenced by their capacity to preserve cellular viability, dampen NO production, and suppress the secretion of critical pro-inflammatory mediators (TNF-α, IL-6, IL-1β, and IL-12) in RAW 264.7 cells. These remarkable anti-inflammatory effects hint at the therapeutic potential of PS in ameliorating chronic inflammatory conditions and bolstering the body’s immune response.In conclusion, Polyscias scutellaria stands as an emerging botanical champion, offering a wealth of natural antioxidants and anti-inflammatory compounds that hold great promise for optimizing health and well-being. This study opens exciting avenues for future research to elucidate the precise bioactive constituents within PS and unravel their intricate mechanisms of action, paving the way for the development of innovative therapeutic interventions and wellness-enhancing products. The remarkable properties of PS underscore its potential as a cornerstone of holistic health and a valuable asset in the pursuit of a vibrant and balanced life.\u0000 \u0000 Graphical abstract\u0000","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"11 22","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138603567","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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