Pub Date : 2023-12-04DOI: 10.3897/pharmacia.70.e115795
V. Karamfilova, Iveta Nedeva, Tsvetan Gatev, A. Gateva, Y. Assyov, Antonina Gerganova, Dobrin Popov, T. Velikova, Z. Kamenov
Background: Fetuin-A is a multifunctional liver-derived glycoprotein that is associated with insulin resistance and might play a role in the pathogenesis of prediabetes and type 2 diabetes (T2DM). Objective: This study evaluated the relationship of Fetuin-A with metabolic and vascular parameters in patients with prediabetes and T2DM. Materials and methods: total 120 obese patients were included. They were divided into three groups: group 1 – without carbohydrate disturbances, group 2 – with prediabetes and group 3 – with type 2 diabetes mellitus. Results: Higher Fetuin-A serum levels were observed in patients with prediabetes and T2DM compared to those with normoglycemia. Fetuin-A ≥821 mcg/ml increased the risk for T2DM 32-fold. Additionally, we found positive correlations between Fetuin-A, vibration perception threshold and toe-brachial index and a negative correlation with neuropathy disability score. Conclusion: Fetuin-A could be predictive for incidents of prediabetes and T2DM.
{"title":"Relationship of serum Fetuin-A with metabolic and vascular parameters in patients with prediabetes and type 2 diabetes mellitus","authors":"V. Karamfilova, Iveta Nedeva, Tsvetan Gatev, A. Gateva, Y. Assyov, Antonina Gerganova, Dobrin Popov, T. Velikova, Z. Kamenov","doi":"10.3897/pharmacia.70.e115795","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e115795","url":null,"abstract":"Background: Fetuin-A is a multifunctional liver-derived glycoprotein that is associated with insulin resistance and might play a role in the pathogenesis of prediabetes and type 2 diabetes (T2DM).\u0000 Objective: This study evaluated the relationship of Fetuin-A with metabolic and vascular parameters in patients with prediabetes and T2DM.\u0000 Materials and methods: total 120 obese patients were included. They were divided into three groups: group 1 – without carbohydrate disturbances, group 2 – with prediabetes and group 3 – with type 2 diabetes mellitus.\u0000 Results: Higher Fetuin-A serum levels were observed in patients with prediabetes and T2DM compared to those with normoglycemia. Fetuin-A ≥821 mcg/ml increased the risk for T2DM 32-fold. Additionally, we found positive correlations between Fetuin-A, vibration perception threshold and toe-brachial index and a negative correlation with neuropathy disability score.\u0000 Conclusion: Fetuin-A could be predictive for incidents of prediabetes and T2DM.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"5 15","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138603319","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e113287
Bhavana Madupoju, Subhakar Raju Rapaka, N. Malothu, P. K. Desu, A. Areti
Purpose: In the present study, N-acetyl cysteine (NAC)-Solid Lipid Nanoparticles (SLNs) were developed employing the Quality by Design (QBD) approach for the application of hepatoprotective activity. Methods: Using Box-Behnken Design (BBD) three independent variables (Soya lecithin, polysorbate content, and homogenization speed) and four dependent variables (% entrapment efficiency (EE), % drug release (DR), zeta potential (ZP), and particle size (PS)) were chosen for the study. The formulations were prepared by the hot homogenization method and characterized with SEM, FTIR, DSC, and XRD and evaluated their % EE, % DR, PS, and ZP. Developed SLNs were tested for their hepatoprotective activity by an in vivo mice model and compared the effectiveness with free NAC and Silymarin. Results: The optimized NAC-SLNs were found optimum with spherical and intact chemical structure (88.95% EE, 97.15% DR, -43.01 mv ZP, < 200 nm of PS) exhibiting Higuchi model of drug release. In terms of MDA levels, NAC-SLNs had a strong protective impact MDA level (23.09±0.01–21.84±0.01 u mole/mg protein) and were efficient in increasing GPx (16.89±0.01–20.71±0.02 unit/mg protein), GSH (18.94±0.57–24.21±1.00 unit/mg protein), which were reduced in the CCl4-intoxicated group. NAC-SLNs were more effective than NAC at inhibiting the liver enzymes SGOT (150.01±1.5–132.01±0.6 mg/dL), SGPT (100.73±1.1–91.98±2.8 mg/dL), ALP (147.07±0.8–124.79±0.5 mg/dL), and LDH (290.37±3.04–228.25±2.03U/L). Conclusion: The study concludes that NAC-SLNs therapy was not only substantially more effective than NAC, but it also had effects equivalent to a well-known hepatoprotective and antioxidant drug Silymarin.
{"title":"Hepatoprotective activity of QBD-based optimized N-acetyl cysteine solid lipid nanoparticles against CCL4-induced liver injury in mice","authors":"Bhavana Madupoju, Subhakar Raju Rapaka, N. Malothu, P. K. Desu, A. Areti","doi":"10.3897/pharmacia.70.e113287","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e113287","url":null,"abstract":"Purpose: In the present study, N-acetyl cysteine (NAC)-Solid Lipid Nanoparticles (SLNs) were developed employing the Quality by Design (QBD) approach for the application of hepatoprotective activity. Methods: Using Box-Behnken Design (BBD) three independent variables (Soya lecithin, polysorbate content, and homogenization speed) and four dependent variables (% entrapment efficiency (EE), % drug release (DR), zeta potential (ZP), and particle size (PS)) were chosen for the study. The formulations were prepared by the hot homogenization method and characterized with SEM, FTIR, DSC, and XRD and evaluated their % EE, % DR, PS, and ZP. Developed SLNs were tested for their hepatoprotective activity by an in vivo mice model and compared the effectiveness with free NAC and Silymarin. Results: The optimized NAC-SLNs were found optimum with spherical and intact chemical structure (88.95% EE, 97.15% DR, -43.01 mv ZP, < 200 nm of PS) exhibiting Higuchi model of drug release. In terms of MDA levels, NAC-SLNs had a strong protective impact MDA level (23.09±0.01–21.84±0.01 u mole/mg protein) and were efficient in increasing GPx (16.89±0.01–20.71±0.02 unit/mg protein), GSH (18.94±0.57–24.21±1.00 unit/mg protein), which were reduced in the CCl4-intoxicated group. NAC-SLNs were more effective than NAC at inhibiting the liver enzymes SGOT (150.01±1.5–132.01±0.6 mg/dL), SGPT (100.73±1.1–91.98±2.8 mg/dL), ALP (147.07±0.8–124.79±0.5 mg/dL), and LDH (290.37±3.04–228.25±2.03U/L). Conclusion: The study concludes that NAC-SLNs therapy was not only substantially more effective than NAC, but it also had effects equivalent to a well-known hepatoprotective and antioxidant drug Silymarin.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"42 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139207934","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e114938
D. Tsvetkova, Lily Peykova, Lily Andonova-Dimitrova, I. Pencheva
Cannabis sativa L. is a medicinal plant from family Cannabaceae with many pharmacological activities. The recent appearance of a number of cannabis products in the pharmaceutical market has led to increased requirements for regulation and quality control. The control of Cannabis sativa L. is subject to the Psychotropic Substances Convention, which includes the addictive psychoactive delta-9-tetrahydrocannabinol (THC), and to the Narcotic Drugs Convention, which includes the illicit products: herbal and liquid cannabis, resin, extracts and tinctures of flowering or fruiting tops containing THC. Approved by the FDA for use in chemotherapy are Marinol caps. (THC) and Cesamet caps., containing the synthetic THC-derivative Nabilon. There is no harmonized European Union legislation on the use of cannabis and Cannabidiol (CBD), which antagonizes the THC-psychotropic effect. Legitimate products include seeds, oil, extracts, and seed tinctures of the industrial cannabis chemotype, containing primarily Cannabidiol and less than 0.2% THC. Sativex oral spray (THC/CBD = 1:1) is approved for muscle spasticity in multiple sclerosis. Cannabidiol was not used as a food ingredient in the European Union before 15.05.1997 and is a „novel food” according to Regulation 2015/2283. Flour; protein powder and cannabis seed oil are not „novel foods”. Cannabidiol as Epidiolex is FDA approved for epilepsy forms Lennox-Gastaut and Dravet.
{"title":"Regulation and control of the use of Cannabis and Cannabidiol in „novel foods”","authors":"D. Tsvetkova, Lily Peykova, Lily Andonova-Dimitrova, I. Pencheva","doi":"10.3897/pharmacia.70.e114938","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114938","url":null,"abstract":"Cannabis sativa L. is a medicinal plant from family Cannabaceae with many pharmacological activities. The recent appearance of a number of cannabis products in the pharmaceutical market has led to increased requirements for regulation and quality control. The control of Cannabis sativa L. is subject to the Psychotropic Substances Convention, which includes the addictive psychoactive delta-9-tetrahydrocannabinol (THC), and to the Narcotic Drugs Convention, which includes the illicit products: herbal and liquid cannabis, resin, extracts and tinctures of flowering or fruiting tops containing THC. Approved by the FDA for use in chemotherapy are Marinol caps. (THC) and Cesamet caps., containing the synthetic THC-derivative Nabilon. There is no harmonized European Union legislation on the use of cannabis and Cannabidiol (CBD), which antagonizes the THC-psychotropic effect. Legitimate products include seeds, oil, extracts, and seed tinctures of the industrial cannabis chemotype, containing primarily Cannabidiol and less than 0.2% THC. Sativex oral spray (THC/CBD = 1:1) is approved for muscle spasticity in multiple sclerosis. Cannabidiol was not used as a food ingredient in the European Union before 15.05.1997 and is a „novel food” according to Regulation 2015/2283. Flour; protein powder and cannabis seed oil are not „novel foods”. Cannabidiol as Epidiolex is FDA approved for epilepsy forms Lennox-Gastaut and Dravet.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"41 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139200464","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e108120
Viviane Annisa, T. Sulai̇man, A. Nugroho, A. Nugroho
Ketoconazole has low solubility in intestinal pH, whereas drug absorption is largest in the small intestine, which can reduce the bioavailability of the drug. Alginate can be combined with a suitable polymer and cross-linked with divalent ions and another polymer to enhance the solubility of the drug. Ketoconazole could be loaded into a matrix polymer consisting of alginate and anionic polymer through hydrogen bonds formed with the N atom of the ketoconazole. The method employed to produce ketoconazole beads involved ionic gelation with CaCl2 as a cross- linking agent, and various polymer combinations were used: alginate 100:0 (AL100), alginate:pectin 75:25 (AP75) and 50:50 (AP50), alginate:gum acacia 75:25 (AG75) and 50:50 (AG50), and alginate:carrageenan 75:25 (AK75) and 50:50 (AK50). The beads were characterized by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), X-ray diffraction (XRD), swelling study, in vitro drug release study, and solubility determination. The incorporation of ketoconazole into combination matrices of AL100, AG75, AP75, AP50, and AK75 resulted in significantly higher solubility in FaSSIF-2X (Fasted State Simulated Intestinal Fluid) at pH 6.5 compared to pure ketoconazole.
{"title":"A novel formulation of ketoconazole entrapped in alginate with anionic polymer beads for solubility enhancement: Preparation and characterization","authors":"Viviane Annisa, T. Sulai̇man, A. Nugroho, A. Nugroho","doi":"10.3897/pharmacia.70.e108120","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e108120","url":null,"abstract":"Ketoconazole has low solubility in intestinal pH, whereas drug absorption is largest in the small intestine, which can reduce the bioavailability of the drug. Alginate can be combined with a suitable polymer and cross-linked with divalent ions and another polymer to enhance the solubility of the drug. Ketoconazole could be loaded into a matrix polymer consisting of alginate and anionic polymer through hydrogen bonds formed with the N atom of the ketoconazole. The method employed to produce ketoconazole beads involved ionic gelation with CaCl2 as a cross- linking agent, and various polymer combinations were used: alginate 100:0 (AL100), alginate:pectin 75:25 (AP75) and 50:50 (AP50), alginate:gum acacia 75:25 (AG75) and 50:50 (AG50), and alginate:carrageenan 75:25 (AK75) and 50:50 (AK50). The beads were characterized by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), Fourier transform infrared (FT-IR), X-ray diffraction (XRD), swelling study, in vitro drug release study, and solubility determination. The incorporation of ketoconazole into combination matrices of AL100, AG75, AP75, AP50, and AK75 resulted in significantly higher solubility in FaSSIF-2X (Fasted State Simulated Intestinal Fluid) at pH 6.5 compared to pure ketoconazole.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"97 5","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139205905","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e115179
Shina Pashova-Dimova, Peter Petrov, S. Karachanak-Yankova, Anastas Pashov
The role of peptide probes’ conformational flexibility in extracting immunosignatures has not been sufficiently studied. Immunosignatures profile the antibody diversity and prove promising for early cancer detection and multi-disease diagnostics. A novel tool for modeling antibody repertoires, the concept of antibody reactivity graphs, proved instrumental in this respect. Serum samples from patients with Alzheimer’s disease (AD), frontotemporal dementia (FTD), dementia of unknown etiology (DUE), and healthy controls were probed using a set of 130 7-mer peptides relevant to neurodegenerative diseases. Results show that linear peptides probed with IgM yielded higher graph density compared to IgG, indicating different levels of polyspecificities. Additionally, the impact of peptide topology and antibody isotype on feature selection was studied using recursive feature elimination. Findings reveal that IgM assays on linear peptides offer superior diagnostic differentiation of neurodegenerative diseases and define the degree of agreement between IgG and IgM immunosignatures with linear or cyclic peptides.
{"title":"Neurodegenerative diseases associated antibody repertoire signatures in mimotope arrays based on cyclic versus linear peptides","authors":"Shina Pashova-Dimova, Peter Petrov, S. Karachanak-Yankova, Anastas Pashov","doi":"10.3897/pharmacia.70.e115179","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e115179","url":null,"abstract":"The role of peptide probes’ conformational flexibility in extracting immunosignatures has not been sufficiently studied. Immunosignatures profile the antibody diversity and prove promising for early cancer detection and multi-disease diagnostics. A novel tool for modeling antibody repertoires, the concept of antibody reactivity graphs, proved instrumental in this respect. Serum samples from patients with Alzheimer’s disease (AD), frontotemporal dementia (FTD), dementia of unknown etiology (DUE), and healthy controls were probed using a set of 130 7-mer peptides relevant to neurodegenerative diseases. Results show that linear peptides probed with IgM yielded higher graph density compared to IgG, indicating different levels of polyspecificities. Additionally, the impact of peptide topology and antibody isotype on feature selection was studied using recursive feature elimination. Findings reveal that IgM assays on linear peptides offer superior diagnostic differentiation of neurodegenerative diseases and define the degree of agreement between IgG and IgM immunosignatures with linear or cyclic peptides.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"11 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139208101","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e111822
Ayah Kamel Saeed Kamal, Wamidh H. Talib
Breast cancer (BC) is the most prevalent malignancy in women and the first tumor type in the world. Ketogenic diets (KD), which are high in fat, low in carbohydrates, and sufficient in protein, can be used alone or as adjuvants with cancer drug medication as cancer therapy or prevention methods. Probiotics are nonpathogenic microorganisms or groups of bacteria that live in the gut and nourish the host body. In this work, we tested a new KD-probiotic combination against breast cancer implanted in mice. Several combination of probiotics (1×109 CFU/0.5ml) and KD (14.1 kcal/2g) reduced tumor size and enhanced cure rate. KD and combination therapy groups increased beta-hydroxybutyrate (β-OHB) while decrease blood glucose, and IGF-1.IFN-γ, IL-2, IL-4, and IL-10 serum levels were measured to assess immune reaction to various therapies. Combination and probiotics therapy raised IFN-γ, and IL-4 levels, however IL-10 level did decrease in all treated group with highest decrease in combination group. In the safety profile, probiotics, ketogenic diet, and their combination were safe. Overall, the combination of a ketogenic diet and probiotics has the potential to be utilized in the future development of anti-cancer nutrition to augment conventional therapies. Graphical abstract. Summary of the effect of Ketogenic diet, Probiotics and its combination on EMP-6 breast cancer cell and in vivo:
{"title":"Combination of ketogenic diet and probiotics inhibits breast cancer in mice by immune system modulation and reduction of Insulin growth factor-1","authors":"Ayah Kamel Saeed Kamal, Wamidh H. Talib","doi":"10.3897/pharmacia.70.e111822","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111822","url":null,"abstract":"Breast cancer (BC) is the most prevalent malignancy in women and the first tumor type in the world. Ketogenic diets (KD), which are high in fat, low in carbohydrates, and sufficient in protein, can be used alone or as adjuvants with cancer drug medication as cancer therapy or prevention methods. Probiotics are nonpathogenic microorganisms or groups of bacteria that live in the gut and nourish the host body. In this work, we tested a new KD-probiotic combination against breast cancer implanted in mice. Several combination of probiotics (1×109 CFU/0.5ml) and KD (14.1 kcal/2g) reduced tumor size and enhanced cure rate. KD and combination therapy groups increased beta-hydroxybutyrate (β-OHB) while decrease blood glucose, and IGF-1.IFN-γ, IL-2, IL-4, and IL-10 serum levels were measured to assess immune reaction to various therapies. Combination and probiotics therapy raised IFN-γ, and IL-4 levels, however IL-10 level did decrease in all treated group with highest decrease in combination group. In the safety profile, probiotics, ketogenic diet, and their combination were safe. Overall, the combination of a ketogenic diet and probiotics has the potential to be utilized in the future development of anti-cancer nutrition to augment conventional therapies. Graphical abstract. Summary of the effect of Ketogenic diet, Probiotics and its combination on EMP-6 breast cancer cell and in vivo:","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"166 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139199046","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 : 2023-11-30DOI: 10.3897/pharmacia.70.e114989
Preslav Enchev, Y. Zarev, I. Ionkova
This study investigates the bioproduction of astragalosides I, II and IV from endemic Astracantha aitosensis (arnacantha) and Astragalus membranaceus species, and the biotechnological methods for increased efficiency. The extracts from established in vitro cultures, including A. aitosensis callus, shoots and roots and A. membranaceus hairy roots, showed higher astragaloside concentrations than native roots. Specifically, in vitroA. aitosensis cultures produced astragaloside I and II at 0.06 and 0.10 mg/g DW, which were absent in native roots. The production of A. membranaceuss hairy roots exceeds 8 to 15 times astragaloside I and II (0.80 and 0.90 mg/g DW) production when compared to native roots (0.10 and 0.05 mg/g DW), and around 3 times high amount related to astragaloside IV. Addressing astragaloside production challenges, this research also reveals biotechnology approaches as an alternative for sustainable production of this rare cycloartane saponins, conserving the natural habitats. A pilot reproducible in vitro cellular platform has been created, and protocol for specific, unconventional induction of the biosynthesis of the desired target compounds, exploiting the enzymatic system of plant cells from the unexplored plant species A. aitosensis has been established. Our findings clearly show the possibility of using in vitro cultures of A. aitosensis and A. membranaceus for biotechnology production of cycloartane type saponins.
本研究探讨了从当地特有的黄芪（Astracantha aitosensis，arnacantha）和黄芪（Astragalus membranaceus）物种中生物生产黄芪皂苷 I、II 和 IV，以及提高效率的生物技术方法。从已建立的体外培养物（包括黄芪胼胝体、芽和根以及膜荚黄芪毛根）中提取的黄芪皂苷浓度高于原生根。具体来说，A. aitosensis 体外培养物产生的黄芪皂苷 I 和 II 的含量分别为 0.06 和 0.10 毫克/克（干重），而本地根中则没有。与本地根（0.10 和 0.05 毫克/克 DW）相比，A. membranaceuss 发根的黄芪皂苷 I 和 II 产量（0.80 和 0.90 毫克/克 DW）超过 8 至 15 倍，黄芪皂苷 IV 的产量也高出 3 倍左右。针对黄芪皂苷生产面临的挑战，这项研究还揭示了一种生物技术方法，可用于可持续生产这种稀有的环木菠萝烷皂苷，保护自然栖息地。我们建立了一个试验性可重复体外细胞平台，并制定了利用未开发植物物种 A. aitosensis 植物细胞的酶系统，特异性地、非传统地诱导所需目标化合物生物合成的方案。我们的研究结果清楚地表明，有可能利用艾托斯草（A. aitosensis）和膜草（A. membranaceus）的体外培养物进行环木菠萝烷类皂甙的生物技术生产。
{"title":"Biotechnological approaches for sustainable production of astragaloside I, II and IV from endemic species of Astracantha aitosensis (Ivan.) and Astragalus membranaceus (fisch.) by in vitro cultures","authors":"Preslav Enchev, Y. Zarev, I. Ionkova","doi":"10.3897/pharmacia.70.e114989","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e114989","url":null,"abstract":"This study investigates the bioproduction of astragalosides I, II and IV from endemic Astracantha aitosensis (arnacantha) and Astragalus membranaceus species, and the biotechnological methods for increased efficiency. The extracts from established in vitro cultures, including A. aitosensis callus, shoots and roots and A. membranaceus hairy roots, showed higher astragaloside concentrations than native roots. Specifically, in vitroA. aitosensis cultures produced astragaloside I and II at 0.06 and 0.10 mg/g DW, which were absent in native roots. The production of A. membranaceuss hairy roots exceeds 8 to 15 times astragaloside I and II (0.80 and 0.90 mg/g DW) production when compared to native roots (0.10 and 0.05 mg/g DW), and around 3 times high amount related to astragaloside IV. Addressing astragaloside production challenges, this research also reveals biotechnology approaches as an alternative for sustainable production of this rare cycloartane saponins, conserving the natural habitats. A pilot reproducible in vitro cellular platform has been created, and protocol for specific, unconventional induction of the biosynthesis of the desired target compounds, exploiting the enzymatic system of plant cells from the unexplored plant species A. aitosensis has been established. Our findings clearly show the possibility of using in vitro cultures of A. aitosensis and A. membranaceus for biotechnology production of cycloartane type saponins.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"10 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139200601","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}
The purpose of this study was to develop and evaluate an antioxidant body gel scrub formulation including Areca seed extract and Areca beads. The Areca seed ethanol extract had an IC50 of 183.30 µg/ml, a radical scavenging activity of 49.196%, and a total phenolic content of 21.21 ± 2.32 µg/ml. With a pH of 6.98 at 25 °C and a viscosity of 5,590.457 cP, the optimized formulation contained 1% w/w Areca seed extract, 5% w/w polyvinyl alcohol, 0.5% w/w Carbomer Ultrez 21, and 5% w/w Areca microbeads. The formulation had a radical scavenging efficiency of 68.66%. Stability tests were carried out under accelerated heating cooling conditions at 40 ± 2 °C, 75 % RH for 48 hours, followed by 4 °C for 48 hours each cycle for 24 days (6 cycles) and 30 days for 4 °C and 30 ± 2 °C, 75% RH, and no significant changes in physical or chemical properties were observed. This body gel scrub formulation shows potential for use in skincare applications due to its antioxidant activity and stability.
{"title":"Formulation and development of a body gel scrub using Areca catechu L. seed extract and microbeads","authors":"J. Chingunpitak, Attawadee Sae Yoon, Katanyoo Pannoi, Kittipoom Horkul, Noppakrit Tungtongsakul","doi":"10.3897/pharmacia.70.e106321","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e106321","url":null,"abstract":"The purpose of this study was to develop and evaluate an antioxidant body gel scrub formulation including Areca seed extract and Areca beads. The Areca seed ethanol extract had an IC50 of 183.30 µg/ml, a radical scavenging activity of 49.196%, and a total phenolic content of 21.21 ± 2.32 µg/ml. With a pH of 6.98 at 25 °C and a viscosity of 5,590.457 cP, the optimized formulation contained 1% w/w Areca seed extract, 5% w/w polyvinyl alcohol, 0.5% w/w Carbomer Ultrez 21, and 5% w/w Areca microbeads. The formulation had a radical scavenging efficiency of 68.66%. Stability tests were carried out under accelerated heating cooling conditions at 40 ± 2 °C, 75 % RH for 48 hours, followed by 4 °C for 48 hours each cycle for 24 days (6 cycles) and 30 days for 4 °C and 30 ± 2 °C, 75% RH, and no significant changes in physical or chemical properties were observed. This body gel scrub formulation shows potential for use in skincare applications due to its antioxidant activity and stability.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"54 2","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139254645","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 : 2023-11-21DOI: 10.3897/pharmacia.70.e111923
V. Goranova-Marinova, D. Grekova, Vania Georgieva, K. Andreevska, Yana Gvozdeva, Margarita Kassarova, Zhanet Grudeva-Popova
Aim. The aim of this study is to evaluate treatment retrospectively, response to the therapy and outcomes in patients with chronic myeloid leukemia (CML) and to what extent the European recommendations of LeukemiaNET (ELN) are followed at the Hematology Clinic, University Hospital “St. Georgi”, MU Plovdiv. Methods. All patients with Ph+, BCR-ABL1+ CML who were treated and observed between 01.01.2018 and 12.31.2022 at the clinic were included in the study and were analyzed retrospectively. Results. One hundred and eighty-eight patients with a mean age of 61.26 (21–91) years were analyzed. 151 (80.3%) were in chronic phase (CP), 27 (14.4%) in accelerating one and 10 (5.3%) in blast crisis. The actual overall survival rate was 79.26%, while for CP it is very high – 86.75%, and the mortality rate is 20.74%. All patients received some form of tyrosine kinase inhibitors therapy (TKIs-therapy). The first line TKI was imatinib in 120 patients (64%), and 68 (36%) received a second-generation TKI. Treatment response was monitored with TKIs by RT-qPCR. Conclusion.CML patients treated in the hematology clinic receive standard care in accordance with ELN and BMSH recommendations. Overall survival (OS) in routine care is comparable to published data from international studies. Molecular monitoring provides a good basis for disease control in CP. There are unmet needs in the treatment of patients in advanced stages.
{"title":"Analysis of the pharmacotherapeutic effectiveness of the tyrosine kinase inhibitors therapy in patients with Chronic Myeloid Leukemia in a single hematology center in Plovdiv, Bulgaria","authors":"V. Goranova-Marinova, D. Grekova, Vania Georgieva, K. Andreevska, Yana Gvozdeva, Margarita Kassarova, Zhanet Grudeva-Popova","doi":"10.3897/pharmacia.70.e111923","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111923","url":null,"abstract":"Aim. The aim of this study is to evaluate treatment retrospectively, response to the therapy and outcomes in patients with chronic myeloid leukemia (CML) and to what extent the European recommendations of LeukemiaNET (ELN) are followed at the Hematology Clinic, University Hospital “St. Georgi”, MU Plovdiv. Methods. All patients with Ph+, BCR-ABL1+ CML who were treated and observed between 01.01.2018 and 12.31.2022 at the clinic were included in the study and were analyzed retrospectively. Results. One hundred and eighty-eight patients with a mean age of 61.26 (21–91) years were analyzed. 151 (80.3%) were in chronic phase (CP), 27 (14.4%) in accelerating one and 10 (5.3%) in blast crisis. The actual overall survival rate was 79.26%, while for CP it is very high – 86.75%, and the mortality rate is 20.74%. All patients received some form of tyrosine kinase inhibitors therapy (TKIs-therapy). The first line TKI was imatinib in 120 patients (64%), and 68 (36%) received a second-generation TKI. Treatment response was monitored with TKIs by RT-qPCR. Conclusion.CML patients treated in the hematology clinic receive standard care in accordance with ELN and BMSH recommendations. Overall survival (OS) in routine care is comparable to published data from international studies. Molecular monitoring provides a good basis for disease control in CP. There are unmet needs in the treatment of patients in advanced stages.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"135 43","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139252216","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 : 2023-11-21DOI: 10.3897/pharmacia.70.e111097
N. Fareed, H. Kassab
Background: Osteoarthritis is a chronic pathology of the joints causing disability and morbidity. Diacerein is a disease-modifying agent indicated for osteoarthritis management with enhanced performance and have much lower side effects profile than conventional non-steroidal anti-inflammatory drugs. Oral administration of Diacerein is associated with a laxative effect , thus causing treatment discontinuation. Aim: This study aimed to evaluate the activity of Diacerein novasome-based transdermal gel compared with standard oral treatment in the management of induced osteoarthritis in a rat model. Materials and methods: A single intra-articular injection of monosodium iodoacetate was administered to the left knee joint, resulting in the development of Osteoarthritis. Disease progression and the effect of both routes of Diacerein treatment were evaluated by morphological, biochemical, histological, and radiological studies. Results: Osteoarthritis was successfully induced in rats’ knee joints. Morphological studies revealed that both Diacerein treatments significantly reduced joint swelling as compared to the untreated group. The serum TNF-α and IL-1β levels were significantly lower in both Diacerein treatment groups as compared to the untreated group throughout the course of the study. Histological and radiological findings confirmed that transdermal Diacerein treatment protects against cartilage degradation like oral treatment. Conclusion: Novasomal technology proved its efficacy as a carrier for the transdermal delivery of Diacerein. The in-vivo study on an animal model of osteoarthritis showed that Diacerein transdermal gels provided sufficient pharmacological activity for the attenuation of the disease. This finding could support its use as an alternative to the standard oral treatment to avoid side effects.
{"title":"A comparative study of oral diacerein and transdermal diacerein as Novasomal gel in a model of MIA induced Osteoarthritis in rats","authors":"N. Fareed, H. Kassab","doi":"10.3897/pharmacia.70.e111097","DOIUrl":"https://doi.org/10.3897/pharmacia.70.e111097","url":null,"abstract":"Background: Osteoarthritis is a chronic pathology of the joints causing disability and morbidity. Diacerein is a disease-modifying agent indicated for osteoarthritis management with enhanced performance and have much lower side effects profile than conventional non-steroidal anti-inflammatory drugs. Oral administration of Diacerein is associated with a laxative effect , thus causing treatment discontinuation. Aim: This study aimed to evaluate the activity of Diacerein novasome-based transdermal gel compared with standard oral treatment in the management of induced osteoarthritis in a rat model. Materials and methods: A single intra-articular injection of monosodium iodoacetate was administered to the left knee joint, resulting in the development of Osteoarthritis. Disease progression and the effect of both routes of Diacerein treatment were evaluated by morphological, biochemical, histological, and radiological studies. Results: Osteoarthritis was successfully induced in rats’ knee joints. Morphological studies revealed that both Diacerein treatments significantly reduced joint swelling as compared to the untreated group. The serum TNF-α and IL-1β levels were significantly lower in both Diacerein treatment groups as compared to the untreated group throughout the course of the study. Histological and radiological findings confirmed that transdermal Diacerein treatment protects against cartilage degradation like oral treatment. Conclusion: Novasomal technology proved its efficacy as a carrier for the transdermal delivery of Diacerein. The in-vivo study on an animal model of osteoarthritis showed that Diacerein transdermal gels provided sufficient pharmacological activity for the attenuation of the disease. This finding could support its use as an alternative to the standard oral treatment to avoid side effects.","PeriodicalId":20086,"journal":{"name":"Pharmacia","volume":"56 2 1","pages":""},"PeriodicalIF":1.1,"publicationDate":"2023-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139253613","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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