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Possible therapeutic targets and promising drugs based on unsymmetrical hetaryl-substituted porphyrins to combat SARS-CoV-2

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Journal of Pharmaceutical Analysis 2021年第6期11卷 691-698页

作者： Yury A.Gubarev Natalya Sh.Lebedeva Elena S.Yurina Sergey A.Syrbu Aleksey N.Kiselev Mikhail A.Lebedev G.A.Krestov Institute of Solution Chemistry of the Russian Academy of Sciences 153045IvanovoRussia Ivanovo State University of Chemistry and Technology 153000IvanovoRussia

Coronavirus disease 2019 is a serious disease that causes acute respiratory syndrome and negatively affects the central nervous *** acute respiratory syndrome coronavirus 2(SARS-CoV-2)crosses the blood-brain barrier due to the spike(S) protein on the surface of the viral ***,it is important to develop compounds that not only have an inhibitory effect but are also capable of completely deactivating the S protein *** study describes the purposeful modification of porphyrins and proposes compounds,asymmetrically hetaryl-substituted porphyrins with benzothiazole,benzoxazole,and N-methylbenzimidazole residues,to deactivate the S protein *** docking of SARS-CoV-2 proteins with hetaryl-substituted porphyrins showed that the viral S protein,nucleocapsid(N) protein,and non-structural protein 13(nsp13) exhibited the highest binding ***-substituted porphyrins form strong complexes(13-14 kcal/mol) with the receptor-binding domain of the S protein,while the distance from the porphyrins to the receptor-binding motif(RBM)does not exceed 20 ?;therefore,RBM can be oxidized by ^(1)O_(2),which is generated by *** porphyrins interact with the N protein in the serine/arginine-rich region,and a number of vulnerable amino acid residues are located in the photooxidation *** damage complicates the packaging of viral RNA into new ***-energy binding of hetaryl-substituted porphyrins with the N-and C-terminal domains of nsp13 was *** binding blocks the action of nsp13 as an enzyme of exoribonuclease and methyltransferase,thereby preventing RNA replication and processing.A procedure for the synthesis of hetaryl-substituted porphyrins was developed,new compounds were obtained,their structures were identified,and their photocatalytic properties were studied.

关键词： Porphyrins SARS-CoV-2 Molecular docking photoinactivation

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Reduced salinity interacts with ultraviolet radiation to alter photosystem Ⅱ function in diatom Skeletonema costatum

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Journal of Oceanology and Limnology 2022年第4期40卷 1615-1627页

作者： Shasha ZANG Fang YAN Daode YU Jingjing SONG Lei WANG Zhiguang XU Hongyan WU College of Life Science Ludong UniversityYantai 264025China Marine Science Research Institute of Shandong Province Qingdao 266104China Key Laboratory of Marine Biotechnology in Universities of Shandong(Ludong University) Yantai 264025China

To investigate the effect of reduced salinity on diatoms’ capacity to cope with changing ultraviolet radiation(U VR) and photosynthetically active radiation(PAR),Skeletonema costatum was grown in a range of salinity(15,25,and 35).The photo system Ⅱ(PSⅡ) function was analyzed by increasing PAR and UVR to mimic a mixing event in turbulent *** re sults show that high UVR exposure significantly reduced PSII activity,especially in cells grown at low ***,but not salinity,stimulated the ’removal’ rate of PSII protein *** alone,in the range of 15 to 35,did not regulate PSⅡ acceptor region;however,the low salinity+UVR treatment decreased the energy flux for electron transport per PSⅡ reaction center in *** showed that low salinity exacerbated the damaging effect of UVR on PSⅡ function in *** by suppressing Psb A protein synthe sis and modifying the photochemistry of PSⅡ.Although higher catalase(CAT) activity and NPQs were induced,they were unable to prevent the combined damage effect of low salinity+*** findings indicate that reduced salinity and increased UVR potentially affect the abundance and distribution of *** with the escalation of climate disturbances.

关键词： diatom ultraviolet radiation(UVR) photoinactivation photosystem II

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Separation and identification of the major components of Photocarcinorin and their tumor-photobiological activities

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Journal of Medical Colleges of PLA(China) 1991年第4期6卷 309-318页

作者：陈文晖段祥生许德余 Division of Medicinal Chemistry Laboratory for Antimalarial Drug ResearchSecond Military Medical UniversityShanghai 200433

It has been shown by the results-of HPLC analysis in combination with spectrographicdeterminations that PsD-007 is composed of 7 different porphyrins,In order of the proportion inPsD-007,they are:3 （or 8）-（l-methoxyethyl）-8 （or 3）-（l-hydroxyethyl）-deuteroporphyrin Ⅸ（MHD）;3,8-di-（l-methoxyethyl）-deuteroporphyrin Ⅸ（DMD）;3（or 8）-（l-methoxyethyl）-8 （or3）-vinyl-deuteroporphyrin Ⅸ（MVD）;3（or 8）-（l-hydroxyethyl）-8（or 3）-vinyl-deuteroporphyrin Ⅸ（HVD）;hernatoporphyrin Ⅸ （Hp）;protoporphyrin Ⅸ （Pp） and 3（or 8）-（O-aceylethyl）-8（or 3）-（l-hydroxyethyl）-deuteroporphrin Ⅸ （AHD）,which presented only in crude PsD-007 and hasbeen transformed into MHD and Hp,respectively during the separation and preparing the clinicalpreparation of *** of these porphyrins were further eonfirmed by the corre-sponding anthentic samples obtained by synthetic *** was found on the basis of the experi-mental data of photosensitizing ability in cell-free systems and photoinactivation of human cancercells in vitro as well as efficacy of photodynamic therapy for sarcoma.S180 in mice of the ma-jor components MILD,DMD and MVD composed of which more over 85% of the totalamount of PsD-007,that they all exhibited comparatively high photosensitizing ability andphotodynamic effects on cancer cells and tram-planted animal tumor.

关键词： photocarcinorin neoplasms photodynamic therapy photolocalization photochemodiagnosis and photochemotherapy photosensitizing ability photoinactivation photobiological activity separation and identificatio

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Photodynamic Inactivation of Antibiotic Resistant Bacteria by Phthalocyanin Compounds as Photosensitizers

Photodynamic Inactivation of Antibiotic Resistant Bacteria b...

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第八届全国化学生物学学术会议

作者： Yang Xiang Kewu Yang Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials Science Northwest University

＜正＞With the occurrence of the vancomycin-resistant staphylococcus,the last defense line of bacterial diseases is on the verge of *** an effort to develop novel antibacterial agents against the antibiotic resistant ... 详细信息

关键词： Superbugs Phthalocyanine Singlet oxygen photoinactivation

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