Pub Date : 2023-10-19DOI: 10.1177/09731296231203855
Xudong Qiu, Yang Dong, Bihan Wang, Shuo Yang, Jinghui Sun, He Li, Jianguang Chen, Xingxu Du, Chun Mei Wang
Background Schisandra chinensis (S. chinensis) is a drug commonly used in the clinical treatment of cardiovascular diseases in Traditional Chinese Medicine. However, the specific components and mechanisms of its action are still unclear. We screened six kinds of lignans from S. chinensis with high content and found that schisandrol A and schisantherin A had a strong vasorelaxant effect. The purpose of this study was to investigate the relaxation and underlying mechanism of schisandrol A in the isolated thoracic aorta of rats. Materials and Methods Isolated rat endothelium-intact and endothelium-removed thoracic aorta strips were pre-constricted with phenylephrine (PE), and the relaxation of schisandrol A on the strips was observed. Then, the mechanism was explored by pre-incubating the strips with nitric oxide synthetase inhibitor Nɷ-nitro-l-arginine methyl ester (L-NAME), cyclooxygenase inhibitor (indomethacin), potassium channel blockers 4-aminopyridine (4-AP), barium chloride (BaCl2), tetraethylamine (TEA), and glibenclamide, respectively, and changing the calcium concentration in the bath. In addition, expressions of endothelial nitric oxide synthetase (eNOS) mRNA and protein in rat thoracic aorta were detected. Results Schisandrol A induced both endothelium-dependent and endothelium-independent relaxation of isolated thoracic aorta strips of rats, and the mechanism might be related to promoting the synthesis of NO, inhibiting Ca 2+ release from the sarcoplasmic reticulum, and blocking the Ca 2+ channels. Conclusion These discoveries may provide a theoretical basis for the traditional application of S. chinensis to treat cardiovascular disease.
{"title":"Relaxation Effect of Schisandrol A on Isolated Thoracic Aorta and Its Mechanism in Rats","authors":"Xudong Qiu, Yang Dong, Bihan Wang, Shuo Yang, Jinghui Sun, He Li, Jianguang Chen, Xingxu Du, Chun Mei Wang","doi":"10.1177/09731296231203855","DOIUrl":"https://doi.org/10.1177/09731296231203855","url":null,"abstract":"Background Schisandra chinensis (S. chinensis) is a drug commonly used in the clinical treatment of cardiovascular diseases in Traditional Chinese Medicine. However, the specific components and mechanisms of its action are still unclear. We screened six kinds of lignans from S. chinensis with high content and found that schisandrol A and schisantherin A had a strong vasorelaxant effect. The purpose of this study was to investigate the relaxation and underlying mechanism of schisandrol A in the isolated thoracic aorta of rats. Materials and Methods Isolated rat endothelium-intact and endothelium-removed thoracic aorta strips were pre-constricted with phenylephrine (PE), and the relaxation of schisandrol A on the strips was observed. Then, the mechanism was explored by pre-incubating the strips with nitric oxide synthetase inhibitor Nɷ-nitro-l-arginine methyl ester (L-NAME), cyclooxygenase inhibitor (indomethacin), potassium channel blockers 4-aminopyridine (4-AP), barium chloride (BaCl2), tetraethylamine (TEA), and glibenclamide, respectively, and changing the calcium concentration in the bath. In addition, expressions of endothelial nitric oxide synthetase (eNOS) mRNA and protein in rat thoracic aorta were detected. Results Schisandrol A induced both endothelium-dependent and endothelium-independent relaxation of isolated thoracic aorta strips of rats, and the mechanism might be related to promoting the synthesis of NO, inhibiting Ca 2+ release from the sarcoplasmic reticulum, and blocking the Ca 2+ channels. Conclusion These discoveries may provide a theoretical basis for the traditional application of S. chinensis to treat cardiovascular disease.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"13 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135730522","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-17DOI: 10.1177/09731296231196189
Sivasakthi Paramasivam, Senthamil Selvan Perumal
Background Osteoporosis is a chronic metabolic bone disease caused due to the dysregulation in the functioning of osteoblast and osteoclast cells leading to increased bone resorption predominantly in postmenopausal women and the elderly, thereby affecting a significant global population. Purpose The present study aims to computationally screen the phytochemical constituents of Oldenlandia umbellata Linn against the unique molecular therapeutic targets of osteoporosis and validate the results using Molecular Dynamics (MD) Simulation. Methods The molecular docking analysis of the selected phytoconstituents against the molecular targets were performed using AutoDock 4.2.6 – AutoDock Tools 1.5.6. In addition, the drug likeliness, ADME, bioactivity, and toxicity were predicted using Molinspiration ADMELAB2.0, ProTox-II and Orisis DataWarrior online tools. Molecular Dynamic Simulation studies were performed using WebGRO macromolecular simulation server. Results Molecular docking results and data analysis revealed that deacetylasperuloside possesses good drug-likeness, ADME properties, and bioactive scores and did not indicate any toxicity compared to other phytochemicals exhibiting binding energies below –8.00 Kcal/mol against the targets. Together, the study emphasized that deacetylasperuloside could bind with the molecular targets of osteoporosis, and the lead is a potential therapeutic candidate for osteoporosis treatment. Further, molecular dynamic simulation analysis for 100 ns revealed that the ligand–protein complexes, including glycogen synthase kinase 3β (GSK3β)-deacetylasperuloside and cathepsin K (CTSK)-deacetylasperuloside complexes, were stable and highly compact assessed from their trajectories. Hence, it can be emphasized that deacetylasperuloside could be a potential therapeutic molecule that could inhibit the targets, including GSK3β and CTSK. Conclusion Oldenlandia umbellata L. is a potential candidate for identifying therapeutic leads for osteoporosis treatment. Further, in vitro and in vivo studies are needed as an output of this research to evaluate its therapeutic efficacy.
{"title":"<i>In Silico</i> Rationalization for Leads from <i>Oldenlandia umbellata</i> L. to Inhibit Multiple Molecular Targets Regulating Osteoporosis","authors":"Sivasakthi Paramasivam, Senthamil Selvan Perumal","doi":"10.1177/09731296231196189","DOIUrl":"https://doi.org/10.1177/09731296231196189","url":null,"abstract":"Background Osteoporosis is a chronic metabolic bone disease caused due to the dysregulation in the functioning of osteoblast and osteoclast cells leading to increased bone resorption predominantly in postmenopausal women and the elderly, thereby affecting a significant global population. Purpose The present study aims to computationally screen the phytochemical constituents of Oldenlandia umbellata Linn against the unique molecular therapeutic targets of osteoporosis and validate the results using Molecular Dynamics (MD) Simulation. Methods The molecular docking analysis of the selected phytoconstituents against the molecular targets were performed using AutoDock 4.2.6 – AutoDock Tools 1.5.6. In addition, the drug likeliness, ADME, bioactivity, and toxicity were predicted using Molinspiration ADMELAB2.0, ProTox-II and Orisis DataWarrior online tools. Molecular Dynamic Simulation studies were performed using WebGRO macromolecular simulation server. Results Molecular docking results and data analysis revealed that deacetylasperuloside possesses good drug-likeness, ADME properties, and bioactive scores and did not indicate any toxicity compared to other phytochemicals exhibiting binding energies below –8.00 Kcal/mol against the targets. Together, the study emphasized that deacetylasperuloside could bind with the molecular targets of osteoporosis, and the lead is a potential therapeutic candidate for osteoporosis treatment. Further, molecular dynamic simulation analysis for 100 ns revealed that the ligand–protein complexes, including glycogen synthase kinase 3β (GSK3β)-deacetylasperuloside and cathepsin K (CTSK)-deacetylasperuloside complexes, were stable and highly compact assessed from their trajectories. Hence, it can be emphasized that deacetylasperuloside could be a potential therapeutic molecule that could inhibit the targets, including GSK3β and CTSK. Conclusion Oldenlandia umbellata L. is a potential candidate for identifying therapeutic leads for osteoporosis treatment. Further, in vitro and in vivo studies are needed as an output of this research to evaluate its therapeutic efficacy.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"8 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135993569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Objectives Prolactinoma is a common intracranial tumor with a high incidence and serious harm to human health. At present, there is only one therapeutic drug in China, bromocriptine, and the Chinese herb Prunella vulgaris L.( P. vulgaris)(PV) has shown certain anti-prolactinoma effects in the early stage. We expect to develop a candidate drug against prolactinoma. Materials and Methods First, the extracts of P. vulgaris L.(PVE)were extracted with water, and the cell proliferation test of rat pituitary tumor cells MMQ was checked by the Cell Counting Kit-8 (CCK-8) assay. Then, core targets and correlative pathways were selected by the “protein–protein interaction” (PPI) network and the “PV–Target–Prolactinoma” network. The core targets and main components simulate the binding by molecular docking. Finally, the PVE and MMQ cells were used to verify the results. Results Through the CCK-8 assay, the PVE inhibited the proliferation of MMQ cells. From the network pharmacology, the 21 targets, 9 signaling pathways, and 20 gene ontology (GO) projects were attained ( p < .05). As a result the estrogen receptor α (ESR1), RAC-alpha serine/threonine-protein kinase(AKT1), and mitogen-activated protein kinase 3(MAPK3)were the core targets of protein against prolactinomas, which was in line with western blotting analysis. Conclusion Our findings demonstrate that the PVE was verified against prolactinomas through the ESR1, MAPK3 targets, and the phosphoinositide 3-kinase/protein kinase B pathway.
{"title":"Network Pharmacology to Explore the Mechanism of <i>Prunella vulgaris</i> L. Against Prolactinoma","authors":"Jun-Hua Meng, Ping Ni, Yu-Ling Cao, Yu Zhang, Xiong Wang, Hong Zhang, Yong-Gang Chen","doi":"10.1177/09731296231189329","DOIUrl":"https://doi.org/10.1177/09731296231189329","url":null,"abstract":"Objectives Prolactinoma is a common intracranial tumor with a high incidence and serious harm to human health. At present, there is only one therapeutic drug in China, bromocriptine, and the Chinese herb Prunella vulgaris L.( P. vulgaris)(PV) has shown certain anti-prolactinoma effects in the early stage. We expect to develop a candidate drug against prolactinoma. Materials and Methods First, the extracts of P. vulgaris L.(PVE)were extracted with water, and the cell proliferation test of rat pituitary tumor cells MMQ was checked by the Cell Counting Kit-8 (CCK-8) assay. Then, core targets and correlative pathways were selected by the “protein–protein interaction” (PPI) network and the “PV–Target–Prolactinoma” network. The core targets and main components simulate the binding by molecular docking. Finally, the PVE and MMQ cells were used to verify the results. Results Through the CCK-8 assay, the PVE inhibited the proliferation of MMQ cells. From the network pharmacology, the 21 targets, 9 signaling pathways, and 20 gene ontology (GO) projects were attained ( p < .05). As a result the estrogen receptor α (ESR1), RAC-alpha serine/threonine-protein kinase(AKT1), and mitogen-activated protein kinase 3(MAPK3)were the core targets of protein against prolactinomas, which was in line with western blotting analysis. Conclusion Our findings demonstrate that the PVE was verified against prolactinomas through the ESR1, MAPK3 targets, and the phosphoinositide 3-kinase/protein kinase B pathway.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135969239","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-12DOI: 10.1177/09731296231203454
Qianyu He, Hu Hao, Keke Zhao
Objectives Rutin protects and stabilizes hepatocytes and is used to treat hepatitis, liver cirrhosis, and other diseases. However, there is little evidence to suggest that Rutin is associated with CCl 4 -induced hepatotoxicity. In this study, we investigated the effects of Rutin on CCl 4 -induced liver inflammation and discussed in vivo and in vitro mechanisms. Materials and Methods CCl 4 was used to induce liver inflammation, and Rutin was used for intervention in mice. Then the body weight, liver weight, and liver inflammation of all mice were measured. Western blotting and RT-PCR were used to assess TLR4/MyD88/NFκB inflammation signaling pathways and inflammatory gene expression. Finally, TLR4 was activated in primary hepatocytes to verify the above signal pathways. Findings CCl 4 mice developed liver function damage and liver inflammation. Further investigations showed that the inhibitory effects of Si on inflammation were mediated by TLR4/MyD88/NFκB inflammation signaling pathways inhibition. Primary hepatocyte studies also confirmed the participation of these signaling pathways and proteins. Significance Rutin improved CCl 4 -induced liver inflammation. Such mechanisms may be related to TLR4/MyD88/NFκB inflammation signaling pathways.
{"title":"Investigating the Anti-inflammatory Effects of Rutin in Carbon Tetrachloride-induced Hepatotoxicity: Role of TLR4/MyD88/NFκB Signaling Pathway Modulation","authors":"Qianyu He, Hu Hao, Keke Zhao","doi":"10.1177/09731296231203454","DOIUrl":"https://doi.org/10.1177/09731296231203454","url":null,"abstract":"Objectives Rutin protects and stabilizes hepatocytes and is used to treat hepatitis, liver cirrhosis, and other diseases. However, there is little evidence to suggest that Rutin is associated with CCl 4 -induced hepatotoxicity. In this study, we investigated the effects of Rutin on CCl 4 -induced liver inflammation and discussed in vivo and in vitro mechanisms. Materials and Methods CCl 4 was used to induce liver inflammation, and Rutin was used for intervention in mice. Then the body weight, liver weight, and liver inflammation of all mice were measured. Western blotting and RT-PCR were used to assess TLR4/MyD88/NFκB inflammation signaling pathways and inflammatory gene expression. Finally, TLR4 was activated in primary hepatocytes to verify the above signal pathways. Findings CCl 4 mice developed liver function damage and liver inflammation. Further investigations showed that the inhibitory effects of Si on inflammation were mediated by TLR4/MyD88/NFκB inflammation signaling pathways inhibition. Primary hepatocyte studies also confirmed the participation of these signaling pathways and proteins. Significance Rutin improved CCl 4 -induced liver inflammation. Such mechanisms may be related to TLR4/MyD88/NFκB inflammation signaling pathways.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"120 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136012688","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-12DOI: 10.1177/09731296231204152
Hongling Zhao, Na Li, Xiaoyan Cui, Yongzhou Yu, Zi Liu, Jianhui Chen, Yuxuan Tian, Chunying Zhao, Hui Xiong
Background Sanqi Xueshangning Capsules (SXC) is a famous Chinese patent medicine with a good curative effect on various gynecological pain diseases in China. However, its chemical composition and potential active ingredients were clearly unrevealed, which hindered the elaboration of its material basis functional mechanism and clinical application. Materials and Methods In the study, we developed an integrative ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) method coupled with SCIEX OS software for characterizing the chemical composition in SXC. The data collection was conducted using a Waters UPLCTM HSS T3 (2.1 × 100 mm, 1.8 µm) in a binary elution system. The SCIEX OS software coupled with multivariable processing techniques was used to screen absorbed prototypes in serum after oral administration of SXC. The structural identification of the components was performed by MS/MS fragmentation mechanism. Results A total of 113 components from SXC were tentatively characterized, including 38 saponins, 13 flavonoids, 10 phenylpropanoids, 9 alkaloids, 20 organic acids, and 23 others. Based on the in vitro composition results, 21 absorbed prototypes in rat serum were identified, mainly including alkaloids, flavonoids, phenylpropanoids, and saponins. Conclusion It was concluded that an integrative UPLC-Q-TOF-MS method coupled with SCIEX OS software could be successfully applied for the components’ characterization of SXC in vitro and in vivo, which laid a reliable scientific basis for promoting the discovery of material basis and the improvement of quality control of SXC.
三七血痛宁胶囊是我国著名的中成药，对多种妇科疼痛疾病有较好的疗效。但其化学成分和潜在有效成分尚未明确，阻碍了其物质基础、作用机制和临床应用的阐述。在研究中，我们开发了一种集成超高效液相色谱四极杆飞行时间质谱(UPLC-Q-TOF-MS)方法，结合SCIEX OS软件对SXC的化学成分进行了表征。数据采集采用Waters UPLCTM HSS T3 (2.1 × 100 mm, 1.8µm)在二元洗脱系统中进行。采用SCIEX OS软件结合多变量处理技术筛选口服SXC后血清中吸收原型。采用MS/MS破碎机制对各组分进行结构鉴定。结果经初步鉴定，共鉴定出113种成分，其中皂苷38种，黄酮类化合物13种，苯丙素10种，生物碱9种，有机酸20种，其他23种。根据体外组成结果，鉴定出21种大鼠血清吸收原型，主要包括生物碱、黄酮类、苯丙素和皂苷。结论UPLC-Q-TOF-MS联用SCIEX OS软件可成功应用于SXC的体内体外组分表征，为促进SXC物质基础的发现和质量控制的提高奠定了可靠的科学依据。
{"title":"Systematic Characterization of the Chemical Components and Absorbed Prototypes in Sanqi Xueshangning Capsules Using UPLC-Q-TOF-MS with SCIEX OS Software","authors":"Hongling Zhao, Na Li, Xiaoyan Cui, Yongzhou Yu, Zi Liu, Jianhui Chen, Yuxuan Tian, Chunying Zhao, Hui Xiong","doi":"10.1177/09731296231204152","DOIUrl":"https://doi.org/10.1177/09731296231204152","url":null,"abstract":"Background Sanqi Xueshangning Capsules (SXC) is a famous Chinese patent medicine with a good curative effect on various gynecological pain diseases in China. However, its chemical composition and potential active ingredients were clearly unrevealed, which hindered the elaboration of its material basis functional mechanism and clinical application. Materials and Methods In the study, we developed an integrative ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) method coupled with SCIEX OS software for characterizing the chemical composition in SXC. The data collection was conducted using a Waters UPLCTM HSS T3 (2.1 × 100 mm, 1.8 µm) in a binary elution system. The SCIEX OS software coupled with multivariable processing techniques was used to screen absorbed prototypes in serum after oral administration of SXC. The structural identification of the components was performed by MS/MS fragmentation mechanism. Results A total of 113 components from SXC were tentatively characterized, including 38 saponins, 13 flavonoids, 10 phenylpropanoids, 9 alkaloids, 20 organic acids, and 23 others. Based on the in vitro composition results, 21 absorbed prototypes in rat serum were identified, mainly including alkaloids, flavonoids, phenylpropanoids, and saponins. Conclusion It was concluded that an integrative UPLC-Q-TOF-MS method coupled with SCIEX OS software could be successfully applied for the components’ characterization of SXC in vitro and in vivo, which laid a reliable scientific basis for promoting the discovery of material basis and the improvement of quality control of SXC.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"73 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135967914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-09DOI: 10.1177/09731296231201210
Fevziye Deniz Güler, Nurullah Ozdemir
Background There are many active substances in the composition of the Hypericum perforatum L. plant that have different and complex structures and show different pharmacological effects. It was accepted as a medicinal plant by the World Health Organization in 2002, and it is given a detailed place in the monographs under the name Hyperici herba. In these monographs, the antibacterial, antiviral, antidepressant, protein kinase-C inhibitor, and wound-healing effects of the plant were described. Objectives The aim of this study is to determine the essential oil components in the samples of the H. perforatum L. plant, which is widely grown in the Thrace region in Türkiye. Materials and Methods H. perforatum L. plant growing naturally in the provinces of the Thrace region was collected, and the essential oils of the plant were obtained by using the hydro distillation method after the collected herbs were dried. Chemical content analyses were performed on a gas chromatography-flame ionization detection (GC-FID). Results The main components of the essential oil of the plant are sesquiterpenes (ß-caryophyllene, caryophyllene oxide, β-selinene, α-selinene, β-farnesene, α-amorphene, spathulenol), alcohols (1-tetradecanol, 1-tridecanol, phytol, and alpha cadinol), and fatty acids (pentadecanoic acid, palmitic acid, and 9, 12 octadecadienoic acid). Conclusion This is the first study to determine the chemical composition of essential oil in H. perforatum L. samples collected from the Thrace region in Türkiye. The essential oil content of the plant can be affected by factors such as the developmental stages of the plant (preblooming, flowering stage, and fruiting time), use of fresh or dry plant material, extraction method, genetic parameters, and climate.
{"title":"Chemical Composition of Essential Oils of Medicinal Plants Grown in the Thrace Region in Türkiye, <i>Hypericum perforatum</i> L","authors":"Fevziye Deniz Güler, Nurullah Ozdemir","doi":"10.1177/09731296231201210","DOIUrl":"https://doi.org/10.1177/09731296231201210","url":null,"abstract":"Background There are many active substances in the composition of the Hypericum perforatum L. plant that have different and complex structures and show different pharmacological effects. It was accepted as a medicinal plant by the World Health Organization in 2002, and it is given a detailed place in the monographs under the name Hyperici herba. In these monographs, the antibacterial, antiviral, antidepressant, protein kinase-C inhibitor, and wound-healing effects of the plant were described. Objectives The aim of this study is to determine the essential oil components in the samples of the H. perforatum L. plant, which is widely grown in the Thrace region in Türkiye. Materials and Methods H. perforatum L. plant growing naturally in the provinces of the Thrace region was collected, and the essential oils of the plant were obtained by using the hydro distillation method after the collected herbs were dried. Chemical content analyses were performed on a gas chromatography-flame ionization detection (GC-FID). Results The main components of the essential oil of the plant are sesquiterpenes (ß-caryophyllene, caryophyllene oxide, β-selinene, α-selinene, β-farnesene, α-amorphene, spathulenol), alcohols (1-tetradecanol, 1-tridecanol, phytol, and alpha cadinol), and fatty acids (pentadecanoic acid, palmitic acid, and 9, 12 octadecadienoic acid). Conclusion This is the first study to determine the chemical composition of essential oil in H. perforatum L. samples collected from the Thrace region in Türkiye. The essential oil content of the plant can be affected by factors such as the developmental stages of the plant (preblooming, flowering stage, and fruiting time), use of fresh or dry plant material, extraction method, genetic parameters, and climate.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"69 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135093857","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-05DOI: 10.1177/09731296231190691
Jia-chen Shi, Ping Wu, Yong-mei Li, Xiao-rui Li
Objectives Psoriasis vulgaris is an immune-mediated inflammatory skin disease that is associated with depression. In this study, we investigated the effect of Xiegan–Liangxue–Jiedu (XGLXJD) decoction, a traditional Chinese medicine formula, on psoriasis based on network pharmacology, molecular docking, and animal experiments. Materials and Methods A protein–protein interaction (PPI) network was constructed using the overlapping targets of XGLXJD decoction and psoriasis. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed using Metascape database. High-performance liquid chromatography (HPLC) was used to investigate the main compounds of XGLXJD decoction. Molecular docking was performed to predict the potential interaction between the main compounds and proteins of interest. A C57 mouse model of psoriasis was established via continuous exposure to imiquimod. Seven days later, the XGLXJD decoction was orally administered at increasing doses for 6 days. The psoriasis area and severity index were calculated. Hematoxylin and eosin staining was used to examine skin morphology. Enzyme-linked immunosorbent assay (ELISA) was used to determine the serum levels of adenylyl cyclase (AC), cyclic adenosine monophosphate (cAMP), protein kinase A (PKA), interleukin-17 (IL-17), and tumor necrosis factor-α (TNF-α). Sucrose preference test and forced swimming test were used to assess depression-like behavior. Immunohistochemical (IHC) staining and immunofluorescence were used to investigate the cAMP-response element binding protein (CREB) signaling pathway. Results Overall, 162 overlapping targets were generated. A total of 398 biological processes, 84 molecular functions, and 47 cellular components were identified via GO analysis, whereas 140 pathways were identified via KEGG pathway analysis. The most notable signaling pathways were cAMP as well as downstream IL-17 and TNF-α signaling pathways. HPLC analysis revealed that the main compounds of XGLXJD decoction were paeoniflorin, isorhamnetin, quercetin, luteolin, kaempferol, and baicalein. The molecular docking assay indicated that the docking energies of the main compounds of XGLXJD decoction to the top hub genes were less than −5 kcal/mol. ELISA revealed that the administration of XGLXJD decoction decreased the levels of pro-inflammatory cytokines (TNF-α and IL-17). Furthermore, the AC, cAMP, and PKA levels were enhanced after its administration. IHC staining demonstrated that the administration of XGLXJD decoction activated the AC–cAMP–PKA–CREB signaling pathway in skin. In addition, it enhanced sucrose preference and forced swimming time percentage. It also enhanced the expression of cAMP and PKA in the hippocampus. Conclusion XGLXJD decoction alleviated psoriasis and depression-like behavior. The AC–cAMP–PKA–CREB signaling pathway may play a crucial role in mediating this effect.
{"title":"Xiegan-Liangxue-Jiedu Decoction Alleviated Psoriasis and Depressionlike Behavior in a Mouse Model: Role of the AC–cAMP–PKA–CREB Signaling Pathway","authors":"Jia-chen Shi, Ping Wu, Yong-mei Li, Xiao-rui Li","doi":"10.1177/09731296231190691","DOIUrl":"https://doi.org/10.1177/09731296231190691","url":null,"abstract":"Objectives Psoriasis vulgaris is an immune-mediated inflammatory skin disease that is associated with depression. In this study, we investigated the effect of Xiegan–Liangxue–Jiedu (XGLXJD) decoction, a traditional Chinese medicine formula, on psoriasis based on network pharmacology, molecular docking, and animal experiments. Materials and Methods A protein–protein interaction (PPI) network was constructed using the overlapping targets of XGLXJD decoction and psoriasis. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed using Metascape database. High-performance liquid chromatography (HPLC) was used to investigate the main compounds of XGLXJD decoction. Molecular docking was performed to predict the potential interaction between the main compounds and proteins of interest. A C57 mouse model of psoriasis was established via continuous exposure to imiquimod. Seven days later, the XGLXJD decoction was orally administered at increasing doses for 6 days. The psoriasis area and severity index were calculated. Hematoxylin and eosin staining was used to examine skin morphology. Enzyme-linked immunosorbent assay (ELISA) was used to determine the serum levels of adenylyl cyclase (AC), cyclic adenosine monophosphate (cAMP), protein kinase A (PKA), interleukin-17 (IL-17), and tumor necrosis factor-α (TNF-α). Sucrose preference test and forced swimming test were used to assess depression-like behavior. Immunohistochemical (IHC) staining and immunofluorescence were used to investigate the cAMP-response element binding protein (CREB) signaling pathway. Results Overall, 162 overlapping targets were generated. A total of 398 biological processes, 84 molecular functions, and 47 cellular components were identified via GO analysis, whereas 140 pathways were identified via KEGG pathway analysis. The most notable signaling pathways were cAMP as well as downstream IL-17 and TNF-α signaling pathways. HPLC analysis revealed that the main compounds of XGLXJD decoction were paeoniflorin, isorhamnetin, quercetin, luteolin, kaempferol, and baicalein. The molecular docking assay indicated that the docking energies of the main compounds of XGLXJD decoction to the top hub genes were less than −5 kcal/mol. ELISA revealed that the administration of XGLXJD decoction decreased the levels of pro-inflammatory cytokines (TNF-α and IL-17). Furthermore, the AC, cAMP, and PKA levels were enhanced after its administration. IHC staining demonstrated that the administration of XGLXJD decoction activated the AC–cAMP–PKA–CREB signaling pathway in skin. In addition, it enhanced sucrose preference and forced swimming time percentage. It also enhanced the expression of cAMP and PKA in the hippocampus. Conclusion XGLXJD decoction alleviated psoriasis and depression-like behavior. The AC–cAMP–PKA–CREB signaling pathway may play a crucial role in mediating this effect.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"34 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135480829","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-04DOI: 10.1177/09731296231190686
Gang Wang
Background Modern strategies to alleviate the harmful effects of organophosphate pesticide diazinon (DN) abnormalities were focused mainly on using natural compounds or their derivatives. DN is an organophosphate compound that causes many health abnormalities in humans due to its usage as an insecticide in agriculture. TQ is one of the beneficiary active principles derived from plant sources that has pharmacological benefits. Aim This research reveals the therapeutic potential of thymoquinone (TQ) on DN-induced myocardial infarction (MI) in rats. Materials and Methods Male Sprague–Dawley rats were procured, acclimatized, and divided into four groups of six animals each with feed and water ad libitum. MI was induced in rats with a dose of 25 mg/kg DN by oral gavage and TQ in a dose of 20 mg/kg p.o. for the treatment. After animal sacrifice at the end of the experimental period, serum and heart tissue samples were collected and processed appropriately for various analyses such as changes in the body weight, heart weight, marker enzymes, oxidative markers, non-enzymatic and enzymatic antioxidants, inflammatory cytokines, histopathological studies, and cardiac-specific markers. Results DN-induced toxicity depicted decreased body weight (167.83 ± 4.62), heart weight (0.9 ± 0.06), and heart-to-body weight ratio (0.54 ± 0.03). Also, elevated marker enzymes (147.33 ± 20.85, 407.5 ± 31.3, and 110.67 ± 9.65 for CK-MB, AST, and ALT, respectively), elevated oxidative markers (12.87 ± 1.34, 125.17 ± 9.95, and 80.17 ± 5.78 for serum MDA, heart MDA, and heart GSSG, respectively), decreased enzymatic- and nonenzymatic antioxidants (3.15 ± 0.42, 12.23 ± 1.02, 5.75 ± 0.46, 2.02 ± 0.26, 0.72 ± 0.07, 18.05 ± 1.04, 8.62 ± 0.65, and 45.8 ± 2.43 for SOD, CAT, GST, GPx, heart GSH, serum GSH, vit.E, and vit.C, respectively), damaged cellular architecture, elevated inflammatory cytokines, and cardiac-specific markers were noticed. Discussion TQ significantly reduced the toxicities produced by DN in almost all the above parameters. The beneficial effect of DN could be attributed to the influential effect of DN on cardiac-specific Nrf2/HO1-related pathways. Conclusion These results suggest that TQ exerts protection against MI and could serve as a promising candidate for drug development.
{"title":"Modulation of Nrf2/HO1 Pathway by Thymoquinone to Exert Protection Against Diazinon-induced Myocardial Infarction in Rats","authors":"Gang Wang","doi":"10.1177/09731296231190686","DOIUrl":"https://doi.org/10.1177/09731296231190686","url":null,"abstract":"Background Modern strategies to alleviate the harmful effects of organophosphate pesticide diazinon (DN) abnormalities were focused mainly on using natural compounds or their derivatives. DN is an organophosphate compound that causes many health abnormalities in humans due to its usage as an insecticide in agriculture. TQ is one of the beneficiary active principles derived from plant sources that has pharmacological benefits. Aim This research reveals the therapeutic potential of thymoquinone (TQ) on DN-induced myocardial infarction (MI) in rats. Materials and Methods Male Sprague–Dawley rats were procured, acclimatized, and divided into four groups of six animals each with feed and water ad libitum. MI was induced in rats with a dose of 25 mg/kg DN by oral gavage and TQ in a dose of 20 mg/kg p.o. for the treatment. After animal sacrifice at the end of the experimental period, serum and heart tissue samples were collected and processed appropriately for various analyses such as changes in the body weight, heart weight, marker enzymes, oxidative markers, non-enzymatic and enzymatic antioxidants, inflammatory cytokines, histopathological studies, and cardiac-specific markers. Results DN-induced toxicity depicted decreased body weight (167.83 ± 4.62), heart weight (0.9 ± 0.06), and heart-to-body weight ratio (0.54 ± 0.03). Also, elevated marker enzymes (147.33 ± 20.85, 407.5 ± 31.3, and 110.67 ± 9.65 for CK-MB, AST, and ALT, respectively), elevated oxidative markers (12.87 ± 1.34, 125.17 ± 9.95, and 80.17 ± 5.78 for serum MDA, heart MDA, and heart GSSG, respectively), decreased enzymatic- and nonenzymatic antioxidants (3.15 ± 0.42, 12.23 ± 1.02, 5.75 ± 0.46, 2.02 ± 0.26, 0.72 ± 0.07, 18.05 ± 1.04, 8.62 ± 0.65, and 45.8 ± 2.43 for SOD, CAT, GST, GPx, heart GSH, serum GSH, vit.E, and vit.C, respectively), damaged cellular architecture, elevated inflammatory cytokines, and cardiac-specific markers were noticed. Discussion TQ significantly reduced the toxicities produced by DN in almost all the above parameters. The beneficial effect of DN could be attributed to the influential effect of DN on cardiac-specific Nrf2/HO1-related pathways. Conclusion These results suggest that TQ exerts protection against MI and could serve as a promising candidate for drug development.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135591122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-10-03DOI: 10.1177/09731296231198931
Yongjie Lu, Lushi Cheng, Lu Ren, Dongqiu Chen, Shumin Guan, Siyang Zhu, Xian Xu, Bing Zhang, Minghui Tang, Chijian Zhang, Yong Ai, Lanyue Zhang, Tinggang He
Background Glabridin is one of the main components of the isoflavonoids in Glycyrrhiza glabra and possesses anti-inflammatory, antibacterial, and anticancer effects. Objectives Herein, the therapeutic effects and mechanisms of action of the glabridin liposome (GL) complex were studied in mice with imiquimod-induced psoriasis. Materials and Methods After treatment with GLs, their effectiveness was assessed using parameters, such as Psoriasis Area and Severity Index (PASI) score, histopathology, inflammatory cytokines, and psoriasis-associated proteins. Results The results demonstrated that GLs could significantly improve psoriatic symptoms, downregulate mast cell infiltration, and significantly reduce the PASI score of psoriatic mice. Quantitative reverse transcription polymerase chain reaction (RT-qPCR) results showed that GLs significantly decreased IL-23 and STAT3 mRNA expression. The results of immunohistochemistry and the enzyme-linked immunosorbent assay indicated that GLs decreased the expression of tumor necrosis factor-alpha (TNF-α), IL-17, and IL-22. Conclusion GLs can alleviate psoriasis by inhibiting the expression of keratinocyte-activating proteins. These results suggest that GLs have great potential for the clinical treatment of psoriasis.
{"title":"Therapeutic Effect and Mechanism of Glabridin Liposome on Imiquimod-induced Mice Psoriasis","authors":"Yongjie Lu, Lushi Cheng, Lu Ren, Dongqiu Chen, Shumin Guan, Siyang Zhu, Xian Xu, Bing Zhang, Minghui Tang, Chijian Zhang, Yong Ai, Lanyue Zhang, Tinggang He","doi":"10.1177/09731296231198931","DOIUrl":"https://doi.org/10.1177/09731296231198931","url":null,"abstract":"Background Glabridin is one of the main components of the isoflavonoids in Glycyrrhiza glabra and possesses anti-inflammatory, antibacterial, and anticancer effects. Objectives Herein, the therapeutic effects and mechanisms of action of the glabridin liposome (GL) complex were studied in mice with imiquimod-induced psoriasis. Materials and Methods After treatment with GLs, their effectiveness was assessed using parameters, such as Psoriasis Area and Severity Index (PASI) score, histopathology, inflammatory cytokines, and psoriasis-associated proteins. Results The results demonstrated that GLs could significantly improve psoriatic symptoms, downregulate mast cell infiltration, and significantly reduce the PASI score of psoriatic mice. Quantitative reverse transcription polymerase chain reaction (RT-qPCR) results showed that GLs significantly decreased IL-23 and STAT3 mRNA expression. The results of immunohistochemistry and the enzyme-linked immunosorbent assay indicated that GLs decreased the expression of tumor necrosis factor-alpha (TNF-α), IL-17, and IL-22. Conclusion GLs can alleviate psoriasis by inhibiting the expression of keratinocyte-activating proteins. These results suggest that GLs have great potential for the clinical treatment of psoriasis.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"98 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135697018","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-09-28DOI: 10.1177/09731296231189324
Hyeon Hwa Nam, Jun Ho Song, Jun Lee, Byeong Cheol Moon, Sumin Noh, Li Nan, Byung Kil Choo, Joong-Sun Kim
Objectives In the study, we investigated the effects of an Eriocheir sinensis water extract on a reflux esophagitis-induced rat model. Background The crab has been used as a traditional medicine and food source in many countries worldwide for a long time, and the crab contains various useful substances such as chitin, protein, calcium carbonate, etc. Materials and Methods All rats were fasted for 24 h and then orally pretreated with saline, Eriocheir sinensis (100 mg/kg), or ranitidine (40 mg/kg). Reflux esophagitis was induced by pylorus and forestomach ligation. Morphological changes in the mucosal damage in the esophagus were analyzed by the ImageJ program. Also, the expression of the inflammatory proteins and cytokine in the esophagus was measured by western blot assay to demonstrate the protective effects of Eriocheir sinensis in reflux esophagitis model. Histological analysis of esophagus was performed by hematoxylin & eosin (H&E) staining. Results In the reflux esophagitis induction group, the esophageal tissue damage caused by the induction of reflux was 60% of the whole. Eriocheir sinensis administration significantly ameliorated esophageal mucosal damage by 40%, also determined by histological evaluation of reflux esophagitis in rats. Eriocheir sinensis was also found to downregulate the expression levels of proteins such as cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and tight junction protein (claudin-5) compared to the reflux esophagitis induction group. In addition, Eriocheir sinensis markedly attenuated the activation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and the phosphorylation of the inhibitor of NF-κB (IκBα). Conclusion These results indicated that Eriocheir sinensis suppressed the development of esophagitis and modulated inflammation by regulating NF-κB activation. Based on these findings, we concluded that Eriocheir sinensis can protect the esophageal mucosa from reflux esophagitis.
{"title":"Functional Properties of the Water Extract from <i>Eriocheir sinensis</i> (Chinese mitten crab) Via Evaluation of Protective Effects on Reflux Esophagitis Model","authors":"Hyeon Hwa Nam, Jun Ho Song, Jun Lee, Byeong Cheol Moon, Sumin Noh, Li Nan, Byung Kil Choo, Joong-Sun Kim","doi":"10.1177/09731296231189324","DOIUrl":"https://doi.org/10.1177/09731296231189324","url":null,"abstract":"Objectives In the study, we investigated the effects of an Eriocheir sinensis water extract on a reflux esophagitis-induced rat model. Background The crab has been used as a traditional medicine and food source in many countries worldwide for a long time, and the crab contains various useful substances such as chitin, protein, calcium carbonate, etc. Materials and Methods All rats were fasted for 24 h and then orally pretreated with saline, Eriocheir sinensis (100 mg/kg), or ranitidine (40 mg/kg). Reflux esophagitis was induced by pylorus and forestomach ligation. Morphological changes in the mucosal damage in the esophagus were analyzed by the ImageJ program. Also, the expression of the inflammatory proteins and cytokine in the esophagus was measured by western blot assay to demonstrate the protective effects of Eriocheir sinensis in reflux esophagitis model. Histological analysis of esophagus was performed by hematoxylin & eosin (H&E) staining. Results In the reflux esophagitis induction group, the esophageal tissue damage caused by the induction of reflux was 60% of the whole. Eriocheir sinensis administration significantly ameliorated esophageal mucosal damage by 40%, also determined by histological evaluation of reflux esophagitis in rats. Eriocheir sinensis was also found to downregulate the expression levels of proteins such as cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and tight junction protein (claudin-5) compared to the reflux esophagitis induction group. In addition, Eriocheir sinensis markedly attenuated the activation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and the phosphorylation of the inhibitor of NF-κB (IκBα). Conclusion These results indicated that Eriocheir sinensis suppressed the development of esophagitis and modulated inflammation by regulating NF-κB activation. Based on these findings, we concluded that Eriocheir sinensis can protect the esophageal mucosa from reflux esophagitis.","PeriodicalId":19895,"journal":{"name":"Pharmacognosy Magazine","volume":"58 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135386636","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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