Pub Date : 2023-11-08DOI: 10.3390/scipharm91040053
Saverio Nucera, Rosa Maria Bulotta, Stefano Ruga, Rosamaria Caminiti, Maria Serra, Roberto Bava, Fabio Castagna, Carmine Lupia, Mariangela Marrelli, Filomena Conforti, Giancarlo Statti, Vincenzo Mollace, Ernesto Palma
Plants are an untapped natural resource; their secondary metabolites take part in a variety of pharmacological activities, making them an essential ingredient in the synthesis of novel medications and the source of reserve resources in this process. Hepatitis and liver cancer are two conditions that can result from non-alcoholic fatty liver disease (NAFLD). NAFLD is a condition that now affects a significant section of the global population. There is a need for preventative action on predisposing factors. Due to their effectiveness and few side effects, herbal medications are frequently utilized for the prevention and treatment of NAFLD. This review discusses the pathogenetic processes of NAFLD and the evidence brought to support the potential of botanical species and their derivatives in limiting the causes that predispose to the onset of NAFLD.
{"title":"Natural Products for the Treatment of Non-Alcoholic Fatty Liver Disease: A Comprehensive Review","authors":"Saverio Nucera, Rosa Maria Bulotta, Stefano Ruga, Rosamaria Caminiti, Maria Serra, Roberto Bava, Fabio Castagna, Carmine Lupia, Mariangela Marrelli, Filomena Conforti, Giancarlo Statti, Vincenzo Mollace, Ernesto Palma","doi":"10.3390/scipharm91040053","DOIUrl":"https://doi.org/10.3390/scipharm91040053","url":null,"abstract":"Plants are an untapped natural resource; their secondary metabolites take part in a variety of pharmacological activities, making them an essential ingredient in the synthesis of novel medications and the source of reserve resources in this process. Hepatitis and liver cancer are two conditions that can result from non-alcoholic fatty liver disease (NAFLD). NAFLD is a condition that now affects a significant section of the global population. There is a need for preventative action on predisposing factors. Due to their effectiveness and few side effects, herbal medications are frequently utilized for the prevention and treatment of NAFLD. This review discusses the pathogenetic processes of NAFLD and the evidence brought to support the potential of botanical species and their derivatives in limiting the causes that predispose to the onset of NAFLD.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"4 7","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135391673","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 : 2023-11-06DOI: 10.3390/scipharm91040051
Alba Alonso Llorente, Josefa Salgado Garrido, Oscar Teijido Hermida, Fabricio González Andrade, Alberto Valiente Martín, Ana Fanlo Villacampa, Jorge Vicente Romero
CYP2C19 is a highly polymorphic gene responsible for the metabolism of commonly used drugs. CYP2C19*1, the wild-type allele, is associated with normal enzyme activity, whereas CYP2C19*2 and CYP2C19*17 lead to null and increased enzyme activity, respectively. The use of different instruments to perform the same pharmacogenetic tests should not affect the reliability of the results reported to clinicians, as required by the ISO 15189 standard. Genotyping assays allowed for the identification of gene variants corresponding to the CYP2C19*2 and CYP2C19*17 haplotypes in 44 selected samples. Each sample was analyzed in duplicate using the Thermo Fisher Taqman Drug Metabolism probes CYP2C19*2: c_25986767_70 (rs4244285) and CYP2C19*17: c_469857_10 (rs12248560). The experiments were performed on two widely used types of real-time PCR analyzers: ABI PRSIM™7500 and QuantStudioTM12KFlex (both from Applied Biosystems, Thermofisher). The data were analyzed in a Thermo Fisher Cloud facility. The analysis was performed independently by two qualified professionals. Both different instruments and analysts’ interpretations were consistent in identifying the native homozygous, heterozygous, and mutant homozygous variants for CYP2C19*2 and CYP2C19*17. The results provided by both the primary and backup analyzers showed a perfect correlation. This would allow for the use of the backup analyzer in case the main one is not available.
{"title":"The Correlation of Two Different Real-Time PCR Devices for the Analysis of CYP2C19 Pharmacogenetic Results","authors":"Alba Alonso Llorente, Josefa Salgado Garrido, Oscar Teijido Hermida, Fabricio González Andrade, Alberto Valiente Martín, Ana Fanlo Villacampa, Jorge Vicente Romero","doi":"10.3390/scipharm91040051","DOIUrl":"https://doi.org/10.3390/scipharm91040051","url":null,"abstract":"CYP2C19 is a highly polymorphic gene responsible for the metabolism of commonly used drugs. CYP2C19*1, the wild-type allele, is associated with normal enzyme activity, whereas CYP2C19*2 and CYP2C19*17 lead to null and increased enzyme activity, respectively. The use of different instruments to perform the same pharmacogenetic tests should not affect the reliability of the results reported to clinicians, as required by the ISO 15189 standard. Genotyping assays allowed for the identification of gene variants corresponding to the CYP2C19*2 and CYP2C19*17 haplotypes in 44 selected samples. Each sample was analyzed in duplicate using the Thermo Fisher Taqman Drug Metabolism probes CYP2C19*2: c_25986767_70 (rs4244285) and CYP2C19*17: c_469857_10 (rs12248560). The experiments were performed on two widely used types of real-time PCR analyzers: ABI PRSIM™7500 and QuantStudioTM12KFlex (both from Applied Biosystems, Thermofisher). The data were analyzed in a Thermo Fisher Cloud facility. The analysis was performed independently by two qualified professionals. Both different instruments and analysts’ interpretations were consistent in identifying the native homozygous, heterozygous, and mutant homozygous variants for CYP2C19*2 and CYP2C19*17. The results provided by both the primary and backup analyzers showed a perfect correlation. This would allow for the use of the backup analyzer in case the main one is not available.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"20 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135590035","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-02DOI: 10.3390/scipharm91040050
Wilson Leonardo Villarreal Romero, Jorge Eliecer Robles Camargo, Geison Modesti Costa
Kalanchoe pinnata is a species widely used in traditional medicine in Latin America and southern Africa. This species has been reported to have different activities, such as antioxidant, anti-inflammatory, and cytotoxic, the latter being related to its flavonoid content. The aim of this study was to contribute to the standardization of the aqueous extract of flowers from Kalanchoe pinnata. Purification of chemical markers was carried out by centrifugal partition chromatography (CPC). Stability tests under stress conditions were conducted for the extract by using the chromatographic profiles analyzed by ultra-performance liquid chromatography coupled to photodiode array detection (UPLC-PDA) and ultra-high-performance liquid chromatography combined with quadrupole-time of flight–mass spectrometry (UHPLC-MS-QTOF), with quantification of flavonoids by a validated UPLC-PDA method. Physicochemical variables of the plant material were within the limits established by official guides. Thirteen flavonoids present in the extract were identified, the major compounds being quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside and quercetin 3-O-D-glucuronide, purified by CPC. A range of total flavonoids for the extract from 8–13% was determined. Finally, through stability tests, it was observed that the extract was stable in most conditions but evidenced moderate degradations upon acid and basic hydrolysis. Through qualitative and quantitative chemical characterizations, it was possible to chemically standardize the aqueous extract of flowers from K. pinnata, with a high content of flavonoids, under parameters required by the WHO and pharmacopoeias.
凤尾莲是一种在拉丁美洲和非洲南部广泛用于传统医学的物种。据报道，该植物具有不同的活性，如抗氧化、抗炎和细胞毒性，后者与其类黄酮含量有关。本研究旨在为凤尾莲花水提物的标准化提供依据。化学标记物采用离心分配色谱(CPC)纯化。采用超高效液相色谱耦合光电二极管阵列检测(UHPLC-MS-QTOF)和超高效液相色谱结合四极杆飞行时间质谱(UHPLC-MS-QTOF)对提取液进行了应力条件下的稳定性测试，并采用经过验证的uhplc - pda方法对黄酮类化合物进行了定量分析。植物材料的物理化学变量在官方指南规定的范围内。从提取物中鉴定出13种黄酮类化合物，主要化合物为槲皮素3-O-α- l-阿拉伯吡喃糖基-(1→2)-α- l-鼠李糖苷和槲皮素3-O- d -葡糖苷。测定了黄酮类化合物的含量范围为8 ~ 13%。最后，通过稳定性测试，观察到提取物在大多数条件下是稳定的，但在酸和碱水解下表现出适度的降解。通过定性和定量的化学表征，可以在世界卫生组织和药典要求的参数下，对黄酮含量高的桄榔子花水提物进行化学标准化。
{"title":"Phytochemical Standardization of an Extract Rich in Flavonoids from Flowers of Kalanchoe pinnata (Lam) Pers","authors":"Wilson Leonardo Villarreal Romero, Jorge Eliecer Robles Camargo, Geison Modesti Costa","doi":"10.3390/scipharm91040050","DOIUrl":"https://doi.org/10.3390/scipharm91040050","url":null,"abstract":"Kalanchoe pinnata is a species widely used in traditional medicine in Latin America and southern Africa. This species has been reported to have different activities, such as antioxidant, anti-inflammatory, and cytotoxic, the latter being related to its flavonoid content. The aim of this study was to contribute to the standardization of the aqueous extract of flowers from Kalanchoe pinnata. Purification of chemical markers was carried out by centrifugal partition chromatography (CPC). Stability tests under stress conditions were conducted for the extract by using the chromatographic profiles analyzed by ultra-performance liquid chromatography coupled to photodiode array detection (UPLC-PDA) and ultra-high-performance liquid chromatography combined with quadrupole-time of flight–mass spectrometry (UHPLC-MS-QTOF), with quantification of flavonoids by a validated UPLC-PDA method. Physicochemical variables of the plant material were within the limits established by official guides. Thirteen flavonoids present in the extract were identified, the major compounds being quercetin 3-O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside and quercetin 3-O-D-glucuronide, purified by CPC. A range of total flavonoids for the extract from 8–13% was determined. Finally, through stability tests, it was observed that the extract was stable in most conditions but evidenced moderate degradations upon acid and basic hydrolysis. Through qualitative and quantitative chemical characterizations, it was possible to chemically standardize the aqueous extract of flowers from K. pinnata, with a high content of flavonoids, under parameters required by the WHO and pharmacopoeias.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"38 3","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135974233","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 : 2023-10-18DOI: 10.3390/scipharm91040049
Kevin P. Lévuok-Mena, Oscar J. Patiño-Ladino, Juliet A. Prieto-Rodríguez
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes.
{"title":"In Vitro Inhibitory Activities against α-Glucosidase, α-Amylase, and Pancreatic Lipase of Medicinal Plants Commonly Used in Chocó (Colombia) for Type 2 Diabetes and Obesity Treatment","authors":"Kevin P. Lévuok-Mena, Oscar J. Patiño-Ladino, Juliet A. Prieto-Rodríguez","doi":"10.3390/scipharm91040049","DOIUrl":"https://doi.org/10.3390/scipharm91040049","url":null,"abstract":"Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"214 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135882956","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 : 2023-10-18DOI: 10.3390/scipharm91040048
Wan-Taek Lim, Chang-Eui Hong, Su-Yun Lyu
Korean mistletoe (Viscum album var. coloratum) has been traditionally used as a remedy for cancer, diabetes, and hypertension. This study investigated the immuno-modulatory effects of Korean mistletoe water extract, specifically on MDA-MB-231 cells, a highly metastatic breast cancer cell line, when co-cultured with THP-1 human macrophage cells. When compared to MDA-MB-231 cells cultured alone, the co-culture of MDA-MB-231/THP-1 cells treated with mistletoe extract showed a significant reduction in IL-6 secretion. Additionally, these co-cultures exhibited elevated levels of IL-4, TGF-β, and IFN-y. These results suggest that water extracts from mistletoe have the potential to induce mitochondria-targeted apoptosis in MDA-MB 231 cells stimulated by THP macrophages. Regarding apoptosis, in MDA-MB-231 cells co-cultured with THP-1 macrophages, mistletoe water extract treatment triggered a significant increase in Bax/Bcl-2 ratio, caspase-3 activation, and PARP inactivation. In addition, there was a significant increase in E-cadherin and a decrease in N-cadherin. Treatment of Korean mistletoe also led to significant reductions in both MMP-2 and -9. Furthermore, inhibition of cell migration in MDA-MB-231/THP-1 co-cultured cells was observed. In summary, this study highlights the potential of Korean mistletoe as a prospective drug for the treatment of triple-negative breast cancer, particularly through its ability to regulate human immunity.
槲寄生(Viscum album var. coloratum)历来被用作治疗癌症、糖尿病和高血压的药物。本研究研究了槲寄生水提取物与THP-1人巨噬细胞共培养时对高转移性乳腺癌细胞系MDA-MB-231细胞的免疫调节作用。与单独培养的MDA-MB-231细胞相比，槲寄生提取物处理的MDA-MB-231/THP-1细胞共培养显示IL-6分泌显著减少。此外，这些共培养物显示出IL-4、TGF-β和IFN-y水平升高。这些结果表明槲寄生水提取物有可能诱导THP巨噬细胞刺激的MDA-MB 231细胞线粒体靶向凋亡。在凋亡方面，在与THP-1巨噬细胞共培养的MDA-MB-231细胞中，槲寄生水提取物显著增加了Bax/Bcl-2比值、caspase-3活化和PARP失活。此外，E-cadherin显著升高，N-cadherin显著降低。槲寄生处理也导致MMP-2和-9的显著降低。进一步观察MDA-MB-231/THP-1共培养细胞对细胞迁移的抑制作用。总之，这项研究强调了韩国槲寄生作为治疗三阴性乳腺癌的前瞻性药物的潜力，特别是通过其调节人体免疫的能力。
{"title":"Immuno-Modulatory Effects of Korean Mistletoe in MDA-MB-231 Breast Cancer Cells and THP-1 Macrophages","authors":"Wan-Taek Lim, Chang-Eui Hong, Su-Yun Lyu","doi":"10.3390/scipharm91040048","DOIUrl":"https://doi.org/10.3390/scipharm91040048","url":null,"abstract":"Korean mistletoe (Viscum album var. coloratum) has been traditionally used as a remedy for cancer, diabetes, and hypertension. This study investigated the immuno-modulatory effects of Korean mistletoe water extract, specifically on MDA-MB-231 cells, a highly metastatic breast cancer cell line, when co-cultured with THP-1 human macrophage cells. When compared to MDA-MB-231 cells cultured alone, the co-culture of MDA-MB-231/THP-1 cells treated with mistletoe extract showed a significant reduction in IL-6 secretion. Additionally, these co-cultures exhibited elevated levels of IL-4, TGF-β, and IFN-y. These results suggest that water extracts from mistletoe have the potential to induce mitochondria-targeted apoptosis in MDA-MB 231 cells stimulated by THP macrophages. Regarding apoptosis, in MDA-MB-231 cells co-cultured with THP-1 macrophages, mistletoe water extract treatment triggered a significant increase in Bax/Bcl-2 ratio, caspase-3 activation, and PARP inactivation. In addition, there was a significant increase in E-cadherin and a decrease in N-cadherin. Treatment of Korean mistletoe also led to significant reductions in both MMP-2 and -9. Furthermore, inhibition of cell migration in MDA-MB-231/THP-1 co-cultured cells was observed. In summary, this study highlights the potential of Korean mistletoe as a prospective drug for the treatment of triple-negative breast cancer, particularly through its ability to regulate human immunity.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135888648","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 : 2023-10-10DOI: 10.3390/scipharm91040047
Dante Avilés-Montes, David Osvaldo Salinas-Sánchez, César Sotelo-Leyva, Alejandro Zamilpa, Franceli Itzel Batalla-Martinez, Rodolfo Abarca-Vargas, Juan Manuel Rivas-González, Óscar Dorado, Rodolfo Figueroa-Brito, Vera L. Petricevich, Dulce Lourdes Morales-Ferra, Manasés González-Cortazar
Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant effects of the acetonic extract (MmAE) of M. mexicana and its fractions (F3, F4-10, F14) using the forced swimming test (FST), elevated plus maze (EPM), open field test (OFT), pentobarbital-induced sleep test (PBTt), and pentylenetetrazol-induced seizure test (PTZt). MmAE, F3, F4-10, F14, and vehicle were administrated orally 24, 18, and 1 h prior to the evaluations. Imipramine (15 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the FST, while diazepam (1 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the EPM, OFT, PBTt, and PTZt. MmAE had an anxiolytic effect; MmAE and F3, F4-10, and F14 showed an antidepressant effect, sedative effect, hypnotic effect, and anticonvulsant effect. Using HPLC, we identified the compounds quercetin 3-O-rutinoside (1), kaempferol 3-O-glucoside (2), luteolin 7-O-glucoside (3), quercetin (4), and kaempferol (5) in MmAE and compounds (1), (2), and (3) in F14. Using GC-MS, we identified α-tocopherol, phytol, and β-amyrin in F3; β-tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10; and α- tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10. The neuropharmacological effects found in this work may be due to the presence of vitamins, phytosterols, terpenes, and flavonoids. This research requires further study to clarify the mechanisms of action of the identified compounds.
精神和神经障碍是影响思想、情绪、行为和人际关系的疾病。墨氏马氏菌。是墨西哥传统医学中用于治疗这类疾病的植物。采用强迫游泳试验(FST)、升高+迷宫试验(EPM)、野外试验(OFT)、戊巴比妥诱导睡眠试验(PBTt)和戊四氮唑诱导癫痫发作试验(PTZt)，探讨墨氏菌丙酮提取物(MmAE)及其组分(F3、F4-10、F14)的抗抑郁、抗焦虑、镇静、催眠和抗惊厥作用。MmAE、F3、F4-10、F14和vehicle分别在评估前24、18和1 h口服。在评估前1小时给予丙咪嗪(15 mg/kg, p.o)作为FST的阳性对照，而在评估前1小时给予地西泮(1 mg/kg, p.o)作为EPM、OFT、PBTt和PTZt的阳性对照。MmAE有抗焦虑作用;MmAE与F3、F4-10、F14具有抗抑郁、镇静、催眠、抗惊厥作用。利用高效液相色谱法鉴定了MmAE中的槲皮素3- o -芦丁苷(1)、山奈酚3- o -葡萄糖苷(2)、木犀草素7- o -葡萄糖苷(3)、槲皮素(4)、山奈酚(5)和F14中的化合物(1)、(2)、(3)。采用气相色谱-质谱法鉴定了F3中α-生育酚、叶绿醇和β-amyrin;F4-10中β-生育酚、叶绿醇、β-谷甾醇和β-amyrin;α-生育酚、叶绿醇、β-谷甾醇和β-amyrin。在这项工作中发现的神经药理作用可能是由于维生素、植物甾醇、萜烯和类黄酮的存在。本研究需要进一步研究以阐明所鉴定化合物的作用机制。
{"title":"Neuropharmacological Activity of the Acetonic Extract of Malpighia mexicana A. Juss. and Its Phytochemical Profile","authors":"Dante Avilés-Montes, David Osvaldo Salinas-Sánchez, César Sotelo-Leyva, Alejandro Zamilpa, Franceli Itzel Batalla-Martinez, Rodolfo Abarca-Vargas, Juan Manuel Rivas-González, Óscar Dorado, Rodolfo Figueroa-Brito, Vera L. Petricevich, Dulce Lourdes Morales-Ferra, Manasés González-Cortazar","doi":"10.3390/scipharm91040047","DOIUrl":"https://doi.org/10.3390/scipharm91040047","url":null,"abstract":"Mental and neurological disorders are conditions that affect thoughts, emotions, behavior, and relationships. Malpighia mexicana A. Juss. is a plant used in Mexican traditional medicine for the treatment of such disorders. This work aimed to investigate the antidepressant, anxiolytic, sedative, hypnotic, and anticonvulsant effects of the acetonic extract (MmAE) of M. mexicana and its fractions (F3, F4-10, F14) using the forced swimming test (FST), elevated plus maze (EPM), open field test (OFT), pentobarbital-induced sleep test (PBTt), and pentylenetetrazol-induced seizure test (PTZt). MmAE, F3, F4-10, F14, and vehicle were administrated orally 24, 18, and 1 h prior to the evaluations. Imipramine (15 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the FST, while diazepam (1 mg/kg, p.o.) was administrated 1 h prior to the evaluations as a positive control for the EPM, OFT, PBTt, and PTZt. MmAE had an anxiolytic effect; MmAE and F3, F4-10, and F14 showed an antidepressant effect, sedative effect, hypnotic effect, and anticonvulsant effect. Using HPLC, we identified the compounds quercetin 3-O-rutinoside (1), kaempferol 3-O-glucoside (2), luteolin 7-O-glucoside (3), quercetin (4), and kaempferol (5) in MmAE and compounds (1), (2), and (3) in F14. Using GC-MS, we identified α-tocopherol, phytol, and β-amyrin in F3; β-tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10; and α- tocopherol, phytol, β-sitosterol, and β-amyrin in F4-10. The neuropharmacological effects found in this work may be due to the presence of vitamins, phytosterols, terpenes, and flavonoids. This research requires further study to clarify the mechanisms of action of the identified compounds.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"57 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136353395","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}
Diabetes is one of the most prevalent diseases worldwide, and the search for therapeutic alternatives in developing countries has been focused on natural products, primarily from plants. This study evaluated the antihyperglycemic and hypoglycemic activities of the albedo (FA) and flavedo (FF) flavonoid fractions obtained from orange peels (often discarded) in normoglycemic Wistar rats. The flavonoid fractions were identified and quantified using HPLC-UV-DAD and compared with glibenclamide, repaglinide, saxagliptin, and acarbose. Additionally, both fractions were tested in a streptozotocin (65 mg/kg)/nicotinamide (100 mg/kg)-induced diabetic model. In normoglycemic rats, the highest glucose variation (%VG) occurred during the first hour after FA (112.8%) and FF (105.30%) administration at 100 mg/kg, indicating a hypoglycemic effect. In diabetic rats, FF at 100 mg/kg showed the highest %VG (140.41%) during the first hour after administration. HPLC-UV-DAD analysis revealed the presence of hesperidin (HSP) and naringenin (NGN), with the highest concentrations found in FA (HSP: 41.41%; NGN: 10.75%). These findings suggest potential antihyperglycemic effects of FA and FF fractions, possibly attributed to the presence of HSP and NGN. The results obtained in this work lay the foundations to explore the therapeutic applications of orange peels for controlling hyperglycemia in diabetes. In conclusion, our results suggest a reevaluation and revalorization of orange peels, as they contain pharmaceutically relevant flavonoids.
{"title":"Hypoglycemic and Antihyperglycemic Potential of Flavonoid Fraction from Citrus sinensis (L.) Osbeck in Normoglycemic and Diabetic Rats","authors":"Jesús Alfredo Araujo-León, Maira Rubi Segura-Campos, Rolffy Ortiz-Andrade, Priscila Vazquez-Garcia, Daniela Carvajal-Sánchez, Ángel Cabañas-Wuan, Avel Adolfo González-Sánchez, Jonatan Uuh-Narvaez, Juan Carlos Sánchez-Salgado, Inés Fuentes-Noriega, Zhelmy Martín-Quintal","doi":"10.3390/scipharm91040046","DOIUrl":"https://doi.org/10.3390/scipharm91040046","url":null,"abstract":"Diabetes is one of the most prevalent diseases worldwide, and the search for therapeutic alternatives in developing countries has been focused on natural products, primarily from plants. This study evaluated the antihyperglycemic and hypoglycemic activities of the albedo (FA) and flavedo (FF) flavonoid fractions obtained from orange peels (often discarded) in normoglycemic Wistar rats. The flavonoid fractions were identified and quantified using HPLC-UV-DAD and compared with glibenclamide, repaglinide, saxagliptin, and acarbose. Additionally, both fractions were tested in a streptozotocin (65 mg/kg)/nicotinamide (100 mg/kg)-induced diabetic model. In normoglycemic rats, the highest glucose variation (%VG) occurred during the first hour after FA (112.8%) and FF (105.30%) administration at 100 mg/kg, indicating a hypoglycemic effect. In diabetic rats, FF at 100 mg/kg showed the highest %VG (140.41%) during the first hour after administration. HPLC-UV-DAD analysis revealed the presence of hesperidin (HSP) and naringenin (NGN), with the highest concentrations found in FA (HSP: 41.41%; NGN: 10.75%). These findings suggest potential antihyperglycemic effects of FA and FF fractions, possibly attributed to the presence of HSP and NGN. The results obtained in this work lay the foundations to explore the therapeutic applications of orange peels for controlling hyperglycemia in diabetes. In conclusion, our results suggest a reevaluation and revalorization of orange peels, as they contain pharmaceutically relevant flavonoids.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"242 3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135580069","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 : 2023-09-26DOI: 10.3390/scipharm91040045
Maria A. Konnova, Alexander A. Volkov, Anna G. Solovyeva, Peter V. Peretyagin, Nina B. Melnikova
The formulation of the transdermal patch with fulvic acid (FA) on an emulsion basis using pluronic Kolliphor® p237 as a permeability enhancer was developed and studied for anti-inflammatory properties. FA was isolated from the peat in the Nizhny Novgorod region of Russia and characterized as a potential active pharmaceutical ingredient. In vitro studies of the release of FA from the transdermal patch, as well as the FA penetration through the acetyl cellulose membrane using the Franz diffusion cell, showed its high efficiency (56% and 90%, respectively, in 8 h). In the in vivo experiment, qualitative and quantitative features of the rat knee caused by complete Freund’s adjuvant-induced arthritis (morphological changes, the FA influence on the biochemical indexes) were studied. The inflammatory process that developed within 15 days was accompanied by the activation of antioxidant oxidoreductase enzymes (by 50–70%), the increase in the cross-sectional diameter of the cartilage, and the increase in the values of marker indicators of the process of rheumatoid arthritis. Within 7 days of treatment, under the influence of FA, the values of ESR, RF, leukocytes, C-reactive protein, as well as the biochemical parameters characterizing oxidative stress (SOD, catalase, glutathione reductase, LDH, G6PD) normalized, and the edema reduced. These results may be useful for arthritis treatment using the transdermal patch with FA.
{"title":"Anti-Inflammatory Property Establishment of Fulvic Acid Transdermal Patch in Animal Model","authors":"Maria A. Konnova, Alexander A. Volkov, Anna G. Solovyeva, Peter V. Peretyagin, Nina B. Melnikova","doi":"10.3390/scipharm91040045","DOIUrl":"https://doi.org/10.3390/scipharm91040045","url":null,"abstract":"The formulation of the transdermal patch with fulvic acid (FA) on an emulsion basis using pluronic Kolliphor® p237 as a permeability enhancer was developed and studied for anti-inflammatory properties. FA was isolated from the peat in the Nizhny Novgorod region of Russia and characterized as a potential active pharmaceutical ingredient. In vitro studies of the release of FA from the transdermal patch, as well as the FA penetration through the acetyl cellulose membrane using the Franz diffusion cell, showed its high efficiency (56% and 90%, respectively, in 8 h). In the in vivo experiment, qualitative and quantitative features of the rat knee caused by complete Freund’s adjuvant-induced arthritis (morphological changes, the FA influence on the biochemical indexes) were studied. The inflammatory process that developed within 15 days was accompanied by the activation of antioxidant oxidoreductase enzymes (by 50–70%), the increase in the cross-sectional diameter of the cartilage, and the increase in the values of marker indicators of the process of rheumatoid arthritis. Within 7 days of treatment, under the influence of FA, the values of ESR, RF, leukocytes, C-reactive protein, as well as the biochemical parameters characterizing oxidative stress (SOD, catalase, glutathione reductase, LDH, G6PD) normalized, and the edema reduced. These results may be useful for arthritis treatment using the transdermal patch with FA.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135719375","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 : 2023-09-19DOI: 10.3390/scipharm91030044
Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Rainer Schobert, Bernhard Biersack
Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities of 3-hydroxy-2-naphthoic carboxyl hydrazone (2a). In addition, sound activities against L. major promastigotes were observed for various analogs of 2a (2b and 2i) and pyrid-2-ylpyrazole-based imines (3g and 3h). Relatively low toxicities to kidney cells and macrophages indicate promising selectivity profiles for these compounds.
以5-硝基呋喃醛和5-亚硝基噻吩-2-甲醛为原料制备了杂亚胺和酰基腙。对其抗刚地弓形虫和利什曼原虫活性进行了评价。对某些酰基腙和亚胺具有良好的抗寄生虫作用和选择性。钴(II)和铜(II)配合物保留了3-羟基-2-萘羧基腙的高抗弓形虫活性(2a)。此外，对2a (2b和2i)和吡啶-2-酰基吡唑基亚胺(3g和3h)的各种类似物，观察到对L. major promastigotes的良好活性。对肾细胞和巨噬细胞的毒性相对较低，表明这些化合物具有良好的选择性。
{"title":"Old Dogs with New Tricks: Antiparasitic Potential of Structurally Diverse 5-Nitrofuran and 5-Nitrothiophene Imines and Acyl Hydrazones","authors":"Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Rainer Schobert, Bernhard Biersack","doi":"10.3390/scipharm91030044","DOIUrl":"https://doi.org/10.3390/scipharm91030044","url":null,"abstract":"Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities of 3-hydroxy-2-naphthoic carboxyl hydrazone (2a). In addition, sound activities against L. major promastigotes were observed for various analogs of 2a (2b and 2i) and pyrid-2-ylpyrazole-based imines (3g and 3h). Relatively low toxicities to kidney cells and macrophages indicate promising selectivity profiles for these compounds.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":"32 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135014346","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 : 2023-09-01DOI: 10.3390/scipharm91030043
S. Ferdosh
The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which are used for urinary tract health by local healers. Literature searches were performed using Google Scholar, ScienceDirect, PubMed, and SpringerLink, by using several keywords, including “medicinal plants in Guam”, “traditional uses”, “bioactive compounds”, “pharmacological properties”, and “urinary tract infections”. This review highlights the traditional uses, bioactive compounds, and pharmacological properties of five medicinal plant species, namely Euphorbia hirta, Phyllanthus amarus, Premna serratifolia, Psidium guajava, and Urena lobata. Phenolics, alkaloids, terpenoids, essential oils, and polypeptides are the leading secondary metabolites reported in different plant extracts, which have been found to have significant antimicrobial, antioxidant, anti-inflammatory, antidiabetic, and anticancer properties. The therapeutic claims made about medicinal plants in Guam are well supported by the literature, having similar applications and pharmacological properties in other regions of the world. These medicinal plants have a lot of unexplored potential that might be utilized to develop more potent drugs for the treatment of infectious diseases, as well as food and herbal supplements.
{"title":"Ethnobotanical Review of Selected Medicinal Plants in Guam for the Treatment of Urinary Tract Ailments and Their Pharmacological Properties","authors":"S. Ferdosh","doi":"10.3390/scipharm91030043","DOIUrl":"https://doi.org/10.3390/scipharm91030043","url":null,"abstract":"The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which are used for urinary tract health by local healers. Literature searches were performed using Google Scholar, ScienceDirect, PubMed, and SpringerLink, by using several keywords, including “medicinal plants in Guam”, “traditional uses”, “bioactive compounds”, “pharmacological properties”, and “urinary tract infections”. This review highlights the traditional uses, bioactive compounds, and pharmacological properties of five medicinal plant species, namely Euphorbia hirta, Phyllanthus amarus, Premna serratifolia, Psidium guajava, and Urena lobata. Phenolics, alkaloids, terpenoids, essential oils, and polypeptides are the leading secondary metabolites reported in different plant extracts, which have been found to have significant antimicrobial, antioxidant, anti-inflammatory, antidiabetic, and anticancer properties. The therapeutic claims made about medicinal plants in Guam are well supported by the literature, having similar applications and pharmacological properties in other regions of the world. These medicinal plants have a lot of unexplored potential that might be utilized to develop more potent drugs for the treatment of infectious diseases, as well as food and herbal supplements.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49337470","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：