Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences最新文献_第10页

In vitro chemotherapeutic and antiangiogenic properties of cardenolides from Acokanthera oblongifolia (Hochst.) Codd. 长叶石竹内酯的体外化疗和抗血管生成特性科德。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-06-01 Print Date: 2021-07-27 DOI: 10.1515/znc-2020-0302

Maha M Soltan, Howaida I Abd-Alla, Amal Z Hassan, Atef G Hanna

{"title":"In vitro chemotherapeutic and antiangiogenic properties of cardenolides from Acokanthera oblongifolia (Hochst.) Codd.","authors":"Maha M Soltan, Howaida I Abd-Alla, Amal Z Hassan, Atef G Hanna","doi":"10.1515/znc-2020-0302","DOIUrl":"https://doi.org/10.1515/znc-2020-0302","url":null,"abstract":"Acovenoside A (Acov-A) and acobioside A (Acob-A) were isolated from Acokanthera oblongifolia. Their anticancer properties were explored regarding, antiproliferative and antiangiogenic activities. The study included screening phase against six cancer cell lines followed by mechanistic investigation against HepG2 cancer cell line. The sulforhodamine-B (SRB) was used to determine their growth inhibitory power. In the other hand, flow cytometry techniques were recorded the cell death type and cell cycle analysis. The clonogenic (colony formation) and wound healing assays, enzyme-linked immunosorbent assay (ELISA) and molecular docking, were performed to evaluate the antiangiogenesis capability. Both compounds were strongly, inhibited four cancer cell lines at GI50 less than 100 nM. The in vitro mechanistic investigation against HepG2 resulted in cell accumulations at G2M phase and induction of apoptosis upon treating cells separately, with 400 nM Acov-A and 200 nM Acob-A. Interestingly, the same concentrations were able to activate caspase-3 by 7.2 and 4.8-fold, respectively. Suppressing the clonogenic capacity of HepG2 cells (20 and 40 nM) and inhibiting the migration of the colon Caco-2 cancer cells were provoke the results of vascular endothelial growth factor receptor2 (VEGFR2) kinase enzyme inactivation. The docked study was highly supportive, to the antiangiogenic approach of both cardenolides. The isolated cardenolides could orchestrate pivotal events in fighting cancer.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 7-8","pages":"337-346"},"PeriodicalIF":2.0,"publicationDate":"2021-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39037365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Cardioprotective effects of omega 3 fatty acids from fish oil and it enhances autoimmunity in porcine cardiac myosin-induced myocarditis in the rat model. 鱼油中omega - 3脂肪酸的心脏保护作用及其增强猪心肌球蛋白诱导的大鼠心肌炎模型的自身免疫。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-31 Print Date: 2021-09-27 DOI: 10.1515/znc-2021-0057

Ling-Yan Li, Xu Wang, Ting-Chuan Zhang, Zong-Jun Liu, Jun-Qing Gao

{"title":"Cardioprotective effects of omega 3 fatty acids from fish oil and it enhances autoimmunity in porcine cardiac myosin-induced myocarditis in the rat model.","authors":"Ling-Yan Li, Xu Wang, Ting-Chuan Zhang, Zong-Jun Liu, Jun-Qing Gao","doi":"10.1515/znc-2021-0057","DOIUrl":"https://doi.org/10.1515/znc-2021-0057","url":null,"abstract":"This experiment proposed to investigate the efficiency of omega 3 fatty acids from fish that improves autoimmune against myocarditis in the rat. Fish oil was extracted from fresh Tuna fish and performed FAME analysis and mice bioassay. The autoimmune myocarditis was induced by subcutaneous injection of porcine cardiac myosin (PCM) into the footpads of rats on the first and seventh day. Rats were dissected on the 21st day to analyze the histopathological, hemodynamic, echocardiographic factors, and immunohistochemistry expressions. In the study, 73.90% of total fatty acids were recorded. Histological analysis revealed that omega 3 fatty acids administrated groups showed tremendous development in the multifocal myocardia hyaline degeneration and necrosis with inflammatory changes. Moreover, omega 3 fatty acids inhabited the expressions of inflammatory cells (CD4, CD8 and CD11b) and suppressed the level of NF-κB. The echocardiographic factors such as heartbeat, SBP, DBP, levels of LVDs, LVDd, LVPW percentage of LVFS, EF, expression levels of inflammatory cytokines (TNF, IL-1β, IFN-ɤ, IL-2, and IL-6) also significantly suppressed by omega 3 fatty acids. Hence, the present study proved that consuming fatty acid-enriched fish might be a successful therapy for improving the inflammatory profile, regenerates the heart tissues, and controlled the production of inflammatory cells.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 9-10","pages":"407-415"},"PeriodicalIF":2.0,"publicationDate":"2021-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/znc-2021-0057","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39043904","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors. 新的含2-肼噻唑的茚衍生物作为潜在的乙酰胆碱酯酶和单胺氧化酶- b抑制剂。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-28 Print Date: 2021-09-27 DOI: 10.1515/znc-2021-0058

İsmail Okan Ateş, Asaf Evrim Evren, Begüm Nurpelin Sağlik, Leyla Yurttaş

{"title":"New indane derivatives containing 2-hydrazinothiazole as potential acetylcholinesterase and monoamine oxidase-B inhibitors.","authors":"İsmail Okan Ateş, Asaf Evrim Evren, Begüm Nurpelin Sağlik, Leyla Yurttaş","doi":"10.1515/znc-2021-0058","DOIUrl":"https://doi.org/10.1515/znc-2021-0058","url":null,"abstract":"Although radical treatment of Alzheimer's and Parkinson's disease is not possible yet, it is aimed to slow the course of the disease and increase the life quality of individuals with the drugs used in the clinic at the present time. Successful results have been achieved in the use of cholinesterase inhibitors and monoamine oxidase inhibitors together in these neurodegenerative diseases. In this study, indane ring which are in the structure of anticholinesterase effective molecules and 2-hydrazinothiazole structure whose inhibitory activities reported on monoamine oxidase-B (MAO-B) were combined; 4-(substituted phenyl)-2-[2-(3-phenyl-2,3-dihydro-1H-inden-1-ylidene) hydrazinyl]thiazole derivatives (3a-3i) were synthesized as dual inhibitors. The structures of the compounds were verified by IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. When enzyme inhibition activities were evaluated, it was determined that the compounds 3a (42.33%) and 3d (42.39%) on acetylcholinesterase (AChE) enzyme; compounds 3g (75.42%) and 3h (60.33%) showed inhibition on MAO-B enzyme at most, at 10-3 M concentration.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 9-10","pages":"417-424"},"PeriodicalIF":2.0,"publicationDate":"2021-05-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39027692","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 3

Preliminary assessment of an injectable extracellular matrix from decellularized bovine myocardial tissue. 可注射的脱细胞牛心肌组织细胞外基质的初步评估。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-27 Print Date: 2021-11-25 DOI: 10.1515/znc-2021-0039

Hatice Ercan, Ayşe Eser Elçin, Yaşar Murat Elçin

{"title":"Preliminary assessment of an injectable extracellular matrix from decellularized bovine myocardial tissue.","authors":"Hatice Ercan, Ayşe Eser Elçin, Yaşar Murat Elçin","doi":"10.1515/znc-2021-0039","DOIUrl":"https://doi.org/10.1515/znc-2021-0039","url":null,"abstract":"The goal of this study was to develop an injectable form of decellularized bovine myocardial tissue matrix which could retain high levels of functional ECM molecules, and could gel at physiological temperature. Dissected ventricular tissue was processed by a detergent-based protocol, lyophilized, enzymatically-digested, and neutralized to form the injectable myocardial matrix (IMM). Histochemical analysis, DNA quantification, and agarose gel electrophoresis demonstrated the efficiency of the applied protocol. Chemical, thermal, morphological, and rheological characterization; protein and sulfated glycosaminoglycan (sGAG) content analysis were performed, in vitro biological properties were evaluated. An in vivo histocompatibility and biodegradability study was performed. Histochemistry revealed complete removal of myocardial cells. DNA content analysis revealed a significant decrease (87%) in the nuclear material, while protein and sGAG contents were highly preserved following decellularization. Soluble IMM was capable of turning into gel form at ∼37 °C, indicating selfassembling property. In vitro findings showed the biomaterial was noncytotoxic, nonhemolytic, and supported the attachment and proliferation of mesenchymal stem cells. In vivo study demonstrated IMM was well-tolerated by rats receiving subcutaneous injection. This work demonstrates that the IMM from decellularized bovine myocardial tissue has the potential for use as a feasible regenerative biomaterial in prospective tissue engineering and regenerative medicine studies.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 11-12","pages":"491-501"},"PeriodicalIF":2.0,"publicationDate":"2021-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39038893","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Oxidative stress and cyto-genotoxicity induced by poly-d-glucosamine in human blood cells in vitro. 聚d-氨基葡萄糖对体外人血细胞氧化应激和细胞遗传毒性的影响。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-26 Print Date: 2022-01-27 DOI: 10.1515/znc-2021-0080

Salim Cerig, Fatime Geyikoglu

{"title":"Oxidative stress and cyto-genotoxicity induced by poly-d-glucosamine in human blood cells in vitro.","authors":"Salim Cerig, Fatime Geyikoglu","doi":"10.1515/znc-2021-0080","DOIUrl":"https://doi.org/10.1515/znc-2021-0080","url":null,"abstract":"Poly-N-acetyl-d-glucosamine (CH; chitin) is the main component of the insect skeleton, fungal cell wall, and many crustaceans, including crab and shrimp. CH is the most abundant in nature after cellulose, and it has a complex and hardly soluble structure. Poly-d-glucosamine (CHO; chitosan) is a soluble derivative of CH produced by deacetylation used in many fields, including human health. This study carried out the cytotoxic, genotoxic, and oxidative effects of CHO on human whole blood (hWB) and lymphocytes (LYMs) in dose ranges 6.25-2000 μg/mL, in vitro. Total antioxidant capacity (TAC) and total oxidant status (TOS) analyzes were performed on plasma to appreciate oxidative stress. 3-(4,5-Dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assays were applied to understand the cytotoxicity. Chromosomal aberration (CA) and micronucleus (MN) methods were practiced to evaluate genotoxicity. 6.25-150 μg/mL doses increased TAC and decreased TOS. A decreasing and increasing curve from 200 to 2000 μg/mL on TAC and TOS values were determined, respectively. 0-250 μg/mL doses did not provide any cytotoxic data. However, 500-2000 μg/mL doses showed increasing cytotoxicity and genotoxicity. The study results showed that CHO does not pose a toxic risk to human health at low doses but may pose a threat at high doses.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"77 1-2","pages":"43-55"},"PeriodicalIF":2.0,"publicationDate":"2021-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39033157","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Loading of capsaicin-in-cyclodextrin inclusion complexes into PEGylated liposomes and the inhibitory effect on IL-8 production by MDA-MB-231 and A549 cancer cell lines. 聚乙二醇脂质体中辣椒素-环糊精包合物的负载及对MDA-MB-231和A549癌细胞产生IL-8的抑制作用

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-26 Print Date: 2021-11-25 DOI: 10.1515/znc-2021-0018

Hiba Abdelnabi, Walhan Alshaer, Hanan Azzam, Dana Alqudah, Ali Al-Samydai, Talal Aburjai

{"title":"Loading of capsaicin-in-cyclodextrin inclusion complexes into PEGylated liposomes and the inhibitory effect on IL-8 production by MDA-MB-231 and A549 cancer cell lines.","authors":"Hiba Abdelnabi, Walhan Alshaer, Hanan Azzam, Dana Alqudah, Ali Al-Samydai, Talal Aburjai","doi":"10.1515/znc-2021-0018","DOIUrl":"https://doi.org/10.1515/znc-2021-0018","url":null,"abstract":"Capsaicin (CAP) is an active component in Capsicum annuum L. known to have anti inflammatory and anticancer activity. CAP is highly lipophilic and suffers low bioavailability. Therefore, developing delivery systems that enhance solubility and bioavailability can provide more promising therapeutic applications for CAP. In the current work, CAP was complexed with β-cyclodextrin (βCD) to form capsaicin-in-β-cyclodextrin (CAP-in-βCD) inclusion complexes. Then, the CAP-in-βCD inclusion complexes were characterized and loaded into PEGylated liposomes using the thin-film hydration extrusion method. The size, charge, and polydispersity index (PDI) of the PEGylated liposomes were characterized. The levels of IL-8 production were quantified after treatment using array beads. The results of this work showed that the successful formation of inclusion complexes at 1:5 M ratio of CAP to βCD respectively. PEGylated liposomes loaded with βCD/CAP inclusion complexes (CAP-in-βCD-in-liposomes) have a hydrodynamic diameter of (181 ± 36) nm, zeta potential of (-2.63 ± 4.00) mV, encapsulation efficiency (EE) of (38.65 ± 3.70)%, drug loading (DL) of (1.65 ± 0.16)%, and a stable release profile. Both free CAP and liposomal CAP showed a significant reduction in the IL-8 production by the MDA-MB-231 and A549 cancer cell lines after treatment. In conclusion, a liposomal-based drug delivery system for CAP was achieved.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 11-12","pages":"503-514"},"PeriodicalIF":2.0,"publicationDate":"2021-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39033158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Benzylisoquinoline alkaloids from Nelumbo nucifera Gaertn. petals with antiausterity activities against the HeLa human cervical cancer cell line. 莲子中苯基异喹啉类生物碱。花瓣对HeLa人宫颈癌细胞系具有抗紧缩作用。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-24 Print Date: 2021-09-27 DOI: 10.1515/znc-2020-0304

Juthamart Maneenet, Ashraf M Omar, Sijia Sun, Min Jo Kim, Supawadee Daodee, Orawon Monthakantirat, Chantana Boonyarat, Yaowared Chulikhit, Suresh Awale

{"title":"Benzylisoquinoline alkaloids from Nelumbo nucifera Gaertn. petals with antiausterity activities against the HeLa human cervical cancer cell line.","authors":"Juthamart Maneenet, Ashraf M Omar, Sijia Sun, Min Jo Kim, Supawadee Daodee, Orawon Monthakantirat, Chantana Boonyarat, Yaowared Chulikhit, Suresh Awale","doi":"10.1515/znc-2020-0304","DOIUrl":"https://doi.org/10.1515/znc-2020-0304","url":null,"abstract":"Ethanolic extract of Nelumbo nucifera petals showed preferential cytotoxic activity against HeLa human cervical cancer cell line with a PC50 value of 10.4 μg/mL. This active extract was subjected to a phytochemical investigation study which led to the isolation of nine benzylisoquinoline alkaloids (1-9). The isolated compounds exhibited potent antiausterity activities. Moreover, under nutrient-deprived conditions, (-)-lirinidine (8) induced remarkable alterations in HeLa cell morphology including cell shrinkage and plasma blebbing leading to total cell death within 10 h. Mechanistically, 8 was found to inhibit Akt/mTOR signaling pathway. It also induced apoptosis by promoting caspase-3 activation and inhibiting Bcl-2 expression. Therefore, benzylisoquinoline alkaloids skeleton can be considered as a promising scaffold for the anticancer drug development against cervical cancer.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 9-10","pages":"401-406"},"PeriodicalIF":2.0,"publicationDate":"2021-05-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38935349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Flavonolignan 2, 3-dehydroderivatives from Oenanthe javanica and their anti inflammatory activities. 黄酮木脂素2,3 -脱氢衍生物及其抗炎活性。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-05-18 Print Date: 2021-11-25 DOI: 10.1515/znc-2021-0001

Rong-Rui Wei, Qin-Ge Ma

引用次数: 1

Oregano essential oil inhibits Candida spp. biofilms. 牛至精油抑制念珠菌生物膜。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-04-29 Print Date: 2021-11-25 DOI: 10.1515/znc-2021-0002

Mayram Hacioglu, Ozlem Oyardi, Alpcan Kirinti

{"title":"Oregano essential oil inhibits Candida spp. biofilms.","authors":"Mayram Hacioglu, Ozlem Oyardi, Alpcan Kirinti","doi":"10.1515/znc-2021-0002","DOIUrl":"https://doi.org/10.1515/znc-2021-0002","url":null,"abstract":"Candida spp. can form biofilms on mucosal surfaces and epithelial cells as well as on devices implanted in the body such as catheters and dentures, which are thought to underlie the most recalcitrant infections. It was aimed to show antifungal and antibiofilm activities of oregano oil (Origanum onites). The antifungal activities of some essential oils were investigated against C. spp. and among them, oregano oil was found to be the most effective oil and further biofilm studies were conducted with it. Oregano oil inhibited biofilm adhesion and formation of C. spp. and mature biofilms and also displayed the ability to reduce biofilm formation when they were allowed to form on surfaces previously coated with oil (up to 50% inhibition rates). In addition, oregano oil was found to be effective against dual biofilms of Candida albicans + Staphyloccocus aureus at different concentrations. This study suggests that O. onites essential oil has useful antibiofilm effects against C. spp. The inhibitory effects of O. onites essential oil, against C. spp., were demonstrated for the first time. It also had antifungal effect on biofilm formation and established biofilm even at MIC level.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 11-12","pages":"443-450"},"PeriodicalIF":2.0,"publicationDate":"2021-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/znc-2021-0002","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38841452","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 8

Synthesis, antioxidant, antimicrobial and antiviral docking studies of ethyl 2-(2-(arylidene)hydrazinyl)thiazole-4-carboxylates. 2-(2-(芳基)肼基)噻唑-4-羧酸乙酯的合成、抗氧化、抗菌和抗病毒对接研究。

IF 2 4区生物学

Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences Pub Date : 2021-04-26 Print Date: 2021-11-25 DOI: 10.1515/znc-2021-0042

Muhammad Haroon, Tashfeen Akhtar, Muhammad Khalid, Shehbaz Ali, Saniya Zahra, Ihsan Ul Haq, Muhanad Alhujaily, Mabilly C H de B Dias, Ana Cristina Lima Leite, Shabbir Muhammad

{"title":"Synthesis, antioxidant, antimicrobial and antiviral docking studies of ethyl 2-(2-(arylidene)hydrazinyl)thiazole-4-carboxylates.","authors":"Muhammad Haroon, Tashfeen Akhtar, Muhammad Khalid, Shehbaz Ali, Saniya Zahra, Ihsan Ul Haq, Muhanad Alhujaily, Mabilly C H de B Dias, Ana Cristina Lima Leite, Shabbir Muhammad","doi":"10.1515/znc-2021-0042","DOIUrl":"https://doi.org/10.1515/znc-2021-0042","url":null,"abstract":"A series of ethyl 2-(2-(arylidene)hydrazinyl)thiazole-4-carboxylates (2a-r) was synthesized in two steps from thiosemicarbazones (1a-r), which were cyclized with ethyl bromopyruvate to ethyl 2-(2-(arylidene)hydrazinyl)thiazole-4-carboxylates (2a-r). The structures of compounds (2a-r) were established by FT-IR, 1H- and 13C-NMR. The structure of compound 2a was confirmed by HRMS. The compounds (2a-r) were then evaluated for their antimicrobial and antioxidant assays. The antioxidant studies revealed, ethyl 2-(2-(4-hydroxy-3-methoxybenzylidene)hydrazinyl)thiazole-4-carboxylate (2g) and ethyl 2-(2-(1-phenylethylidene)hydrazinyl)thiazole-4-carboxylate (2h) as promising antioxidant agents with %FRSA: 84.46 ± 0.13 and 74.50 ± 0.37, TAC: 269.08 ± 0.92 and 269.11 ± 0.61 and TRP: 272.34 ± 0.87 and 231.11 ± 0.67 μg AAE/mg dry weight of compound. Beside bioactivities, density functional theory (DFT) methods were used to study the electronic structure and properties of synthesized compounds (2a-m). The potential of synthesized compounds for possible antiviral targets is also predicted through molecular docking methods. The compounds 2e and 2h showed good binding affinities and inhibition constants to be considered as therapeutic target for Mpro protein of SARS-CoV-2 (COVID-19). The present in-depth analysis of synthesized compounds will put them under the spot light for practical applications as antioxidants and the modification in structural motif may open the way for COVID-19 drug.","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"76 11-12","pages":"467-480"},"PeriodicalIF":2.0,"publicationDate":"2021-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1515/znc-2021-0042","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38909864","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 13