INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2022
·Vol. 23
·期 23
·14903
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IF 6.208
Henan Shi,Zhuqing Wang,Fujie Xu,Jialin Li,Jing Li,Manyuan Wang
In 1972, Nobel laureate Youyou Tu’s research team conducted clinical trials on the dried material ofArtemisia annuaL. from Beijing extracted by ether and then treated with alkali (called “ether neutral dry”), which showed that artemisinin was not the only antimalarial component contained. The biosynthesis of sesquiterpenoids inA. annuahas increased exponentially after unremitting cultivation efforts, and the plant resources are now quite different from those in the 1970s. In consideration of emerging artemisinin resistance, it is of great theoretical and practical value to further study the antimalarial activity ofA. annuaand explore its causes. The purpose of this study is to clarify scientific questions, such as “What ingredients are synergistic with artemisinin inA. annua?”, and “Are there non-artemisinin antimalarial ingredients inA. annua?”. In this paper, Beijing wildA. annuawas used as a control and two representative cultivation species ofA. annuawere selected to evaluate the antimalarial activity of the herbal medicine. The antimalarial activity of different extracts on mice was studied using the Peters’ four-day suppressive test. UPLC-Q-TOF-MS was used to obtain mass spectrum data for all samples, and a UNIFI platform was used for identification. A multivariate statistical method was used to screen the different compounds with positive correlations. The antimalarial activity of different components from the ether extract and alkali treatments was determined and antimalarial components other than artemisinin were obtained. A total of 24 flavonoids, 68 sesquiterpenoids and 21 other compounds were identified. Compounds associated with differential antimalarial activity were identified. The material basis for the antimalarial activity ofA. annuawas clarified. The antimalarial components ofA. annuainclude two categories: first, artemisinin and non-artemisinin antimalarial active components, of which the non-artemisinin antimalarial active components may include 5α-hydroperoxy-eudesma-4(15),11-diene; second, several antimalarial synergistic ingredients inA. annua, including arteanniun B, arteanniun B analogues and polymethoxy flavonoids.Keywords:Artemisia annuaL.;synergistic effect;antimalarial;UPLC-Q-TOF-MS;OPLS-DA
研究领域:
药理学
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代谢组学
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药物化学
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植物科学
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DOI
PubMed
高影响因子
TALANTA
·
2025
·
IF 6.1
Tiantian Chen,Qian Xiang,Xuemei Sang,Daxiu Li,Wenjiao zhou,Fengfeng Xu
Malaria remains a significant threat to global health, especially with the emergence of drug-resistant strains. Therefore, precise monitoring of antimalarial drug levels is crucial for assessing and managing drug resistance. Here, we report a multiplex aptasensor that enables simultaneous fluorescence detection of two antimalarial drugs (MQ and PQ) via split dsT7 promoter-mediated transcription of two-color light-up RNA aptamers. The detection mechanism relies on specific binding of target antimalarial drugs (MQ/PQ) to their aptamers, each triggering formation of intact dsT7 promoter to induce amplified transcription of its cognate RNA aptamer. The generated RNA aptamers bind their corresponding organic dyes (TO1-Biotin and MG) with high affinity, yielding 7.7-/25-fold fluorescence enhancement to enable ultrasensitive detection of MQ and PQ with limits of 0.71 ng/mL and 0.069 ng/mL, respectively. The method also exhibits high selectivity and low background signal. Furthermore, this label-free system achieves multiplexed detection of antimalarial drugs in 10-fold diluted human serum (recovery: 98.67–106.84 % for PQ and 99.89–106.19 % for MQ), demonstrating its real utility. This label-free system is adaptable to other biomarkers through aptamer replacement.
研究领域:
生物化学
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分子生物学
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医学诊断
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产品关联
DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2021
·
IF 4.539
Yilin Wu,Rongxin Lin,Faguang Ma,Zhongyi Jiang
Development of membrane-based molecularly imprinted material with rapid rebinding and high-permselectivity performance has become an urgent need in chemical separation and industrial production. Herein, the high-quality membrane-based designs were proposed for the preparation of SiO 2 @polydopamine blended nanocomposite imprinted membranes with hierarchical structure. The high-efficiency antimalarial drug , artemisinin, was used as template molecule during the newly-developed sol-gel artemisinin-imprinted strategy. Importantly in this work, instead of the direct construction of imprinting layers on membranes, the artemisinin-imprinted SiO 2 @polydopamine particles were initially synthesized followed by a phase conversion process to obtain the SPIMs. The SiO 2 -based artemisinin-imprinted polymers on PDA nanospheres would played imprinted-triggered roles for achieving specific artemisinin-imprinted sites. Meanwhile, amount of artemisinin-imprinted cavities and permselectivity were both optimized, high-permselectivity coefficients (more than 11.5), fast adsorption kinetics and enhanced rebinding capacity (45.89 mg g −1 ) could be obtained. That is to say, this new direction of the membrane’s design would become the further design and guide for selective separation membrane materials.
研究领域:
材料科学
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化学工程
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药学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2021
·
IF 5.875
Wei He,Yawei Du,Chuncao Li,Ji Wang,Yang Wang,Con Dogovski,Rui Hu,Zhiyong Tao,Chen Yao,Xinsong Li
Artesunate (ARS) is the only artemisinin-based intravenous drug approved for treatment of malaria in the clinic. ARS is rapidly metabolized in vivo to short lived (∼30–45 min) but fast acting, dihydroartemisinin (DHA). The short half-life of DHA necessitates multiple dose administration to circumvent the risk of recrudescence and development of artemisinin resistance. In this work, we report a stable, safe and potent alternative artemisinin-based injectable nanocomplex consisting of dimeric artesunate-choline conjugate (dACC) micelles coated with hyaluronic acid (HA). Firstly, dACC was synthesized by one-step esterification of two artesunate molecules with 3-(dimethylamino)-1,2-propanediol followed by quaternization. After that, dACC was self-assembled into cationic nanomicelles and further coated with anionic small molecular weight HA. The HA-coated dACC nanocomplex (dACC/HA nanocomplex) has a narrow size distribution of about 30 nm. Hemolytic toxicity and cytotoxicity studies revealed a favorable bio-safety profile. Finally, in vitro and in vivo studies showed the dACC/HA nanocomplex possess superior safety and antimalarial efficacy compared to ARS. Taken together, the dACC/HA nanocomplex is a promising injectable alternative to the traditional clinically used artesunate.
研究领域:
药剂学
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传染病学
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纳米医学
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2022
·
IF 3.841
Yuan-Yuan Feng,Chang-E Dong,Rui Li,Xiao-Qing Zhang,Wei Wang,Xing-Rui Zhang,Wei-Wei Liu,Da-Hua Shi
Summary A series of new hybrids of 1,2,4-triazine-quinoline were designed, synthesized and assessed as antimalarial agents. The structures of the 1,2,4-triazine-quinoline hybrids were confirmed by IR, NMR, HRMS and single-crystal X-ray diffraction studies. Compound 5f had the crystal system of monoclinic and Cc space group. Compound 5j possessed the monoclinic crystal system and C2/c space group. Compound 5n showed the monoclinic crystal system and P21 space group. Compounds 5a - 5m all exhibited good inhibitory activities associated with β -hematin formation. Compound 5c had the best inhibitory activity of β -hemotin formation with IC 50 values of 4.54 ± 0.16 µM.
研究领域:
药理学
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有机化学
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寄生虫学
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DOI
高影响因子
Journal of Fungi
·
2024
·Vol. 10
·期 11
·736
·
IF 4.2
Guo-Jun Zhou,Wei-Jia Xiong,Wei Xu,Zheng-Rong Dou,Bo-Chao Liu,Xue-Li Li,Hao Du,Hai-Feng Li,Yong-Zeng Zhang,Bei Jiang,Kai-Ling Wang
Astragalus, a group of legume plants, has a pronounced rhizosphere effect. Many species ofAstragaluswith limited resource reserves are distributed in the high-altitude area of northern Yunnan, China. Although some of these plants have high medicinal value, the recognition of them is still at a low level. The aim of this research is to explore the species diversity of cultivable rhizofungi derived fromAstragalus acaulis,A. forrestiiandA. ernestiigrowing in a special high–cold environment of northwest Yunnan and discover anti-infective components from these fungi. A total of 93 fungal strains belonging to 38 species in 18 genera were isolated and identified. Antibacterial and antimalarial screening yielded 10 target strains. Among them, the ethyl acetate crude extract of the fermented substrate of the rhizofungusAspergillus calidoustusAA12 derived from the plantA. acaulisshowed broad-spectrum antibacterial activity and the best antimalarial activity. Further chemical investigation led to the first discovery of seven compounds from the speciesA. calidoustus, including sesterterpine 6-epi-ophiobolin G; three sesquiterpenes, penicisochroman A, pergillin and 7-methyl-2-(1-methylethylethlidene)-furo [3,2-H]isoquinoline-3-one; and three polyketides, trypacidin, 1,2-seco-trypacidin and questin. Among them, the compound 6-epi-ophiobolin G exhibited moderate to strong antibacterial activity against six Gram-positive pathogens with the minimum inhibitory concentration (MIC) ranging from 25 to 6.25 μg/mL and a prominent inhibitory effect on the biofilm ofStreptococcus agalactiaeat an MIC value of 3.125 μg/mL. This compound also displayed potent antimalarial activity againstPlasmodium falciparumstrains 3D7 and chloroquine-resistant Dd2 at the half-maximal inhibitory concentration (IC50) values of 3.319 and 4.340 µmol/L at 72 h, respectively. This study contributed to our understanding of the cultivable rhizofungi from characteristicAstragalusplants in special high–cold environments and further increased the library of fungi available for natural anti-infectious product screening.
研究领域:
微生物学
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药理学
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植物科学
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天然产物化学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Hengtong Zuo,Jihong Qiang,Yidan Wang,Rongrong Wang,Geng Wang,Liqing Chai,Guolian Ren,Yongdan Zhao,Guoshun Zhang,Shuqiu Zhang
Targeting delivery and prolonging action duration of artemisinin drugs are effective strategies for improving antimalarial treatment outcomes. Here, dihydroartemisinin (DHA) loaded poly (lactic- co -glycolic acid) (PLGA) nanoparticles (PDNs) were prepared and further cloaked with red blood cell (RBC) membranes via electrostatic interactions to yield RBC membrane-cloaked PDNs (RPDNs). The prepared RPDNs displayed a notable “core-shell” structure, with a negative surface charge of −29.2 ± 4.19 mV, a relatively uniform size distribution (86.4 ± 2.54 nm , polydispersity index of 0.179 ± 0.011), an average encapsulation efficiency (70.1 ± 0.79%), and a 24-h sustained-release behavior in vitro . Compared with PDNs, RPDNs showed markedly decreased phagocytic activity by RAW 264.7 cells and had prolonged blood circulation duration. The Pearson correlation coefficient of RPDNs distribution in infected red blood cells (iRBCs) was 0.7173, suggesting that RPDNs could effectively target Plasmodium -iRBCs. In Py By265-infected mice, RPDNs showed a higher inhibition ratio (88.39 ± 2.69%) than PDNs (83.13 ± 2.12%) or DHA (58.74 ± 3.78%), at the same dose of 8.8 μmol/kg. The ED 90 of RPDNs (8.13 ± 0.18 μmol/kg) was substantially lower than that of PDNs (14.48 ± 0.23 μmol/kg) and DHA (17.67 ± 3.38 μmol/kg). Furthermore, no apparent abnormalities were detected in routine blood examination, liver function indexes, and pathological analysis of tissue sections of Py By265-infected mice following RPDNs treatment. In conclusion, the prepared RPDNs exhibited enhanced antimalarial efficacy, prolonged circulation, targeted delivery to Plasmodium -iRBCs, and satisfactory biocompatibility .
研究领域:
药学
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纳米技术
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疟疾研究
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药物递送系统
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生物医学工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）