CHEMICAL ENGINEERING JOURNAL
·
2023
·
IF 15.1
Minjia Meng,Yi Li,Hui Peng,Binrong Li,Chuanxun Zhang,Jiajia Ren,Qingluola Ren,Yan Liu,Jianming Pan
The selective separation and purification of ART and ARE using molecularly imprinted membrane (MIM) has attracted considerable attention, but most of conventional blending MIM face low adsorption capacity and poor selectivity due to the blockage of imprinting sites. Herein, an alternative ART imprinted MnO 2 nanowires “coating” membrane (MINM) with hydrophilicity was fabricated by vacuum filtration of imprinted MnO 2 nanowires and graphene oxide nanosheets on PVDF membrane surface for selective ART separation. For the MINM, the imprinted MnO 2 nanowires coating offers more available exposed imprinting sites on the MINM surface compared to that of the blending MIM, while the introduction of graphene oxide improves the hydrophilicity of MINM, significantly reducing the non-specific absorption. Consequently, the MINM exhibits ultrahigh ART adsorption capacity and selectivity, with the ART adsorption amount of 335 mg g −1 at 5 min using dynamic cross-flow separation system, about 12.18 times higher than that of ARE (27.5 mg g −1 ), and the separation factor ( a ) value of 12.39. Moreover, the ATR FT-IR dynamic spectrum discloses the in-situ formation of H-bond between ART and MINM, playing a key role in the selective adsorption process. This work provides an alternative strategy to prepare “coating” MIM for high-efficient and selective separation of complex analogue systems.
研究领域:
材料科学
·
药物化学
·
分离技术
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF AOAC INTERNATIONAL
·
2021
·Vol. 104
·期 4
·1206-1212
·
IF 1.913
You Cong,Yu Jun,Qin Guangjiong,Yang JinPeng,Yang Chunlei,Hu Guoyuan
BackgroundArtemisia hedinii is a well-known traditional Chinese medicine. It can be used to extract dihydroartemisinin (DHA).ObjectiveThe purpose of this study was to explore the optimal conditions for the homogenate extraction of DHA from A. hedinii and the antifungal activity of DHA.MethodsIn this study, single-factor experiments and the response surface method were used to determine the optimal extraction conditions of crude extract and DHA. The method of spore germination was used to study the antifungal activity of DHA on Alternaria alternata.ResultsThe optimal conditions were found as follows: ratio of liquid to material 22 mL/g; extraction time 60 s; and soaking time 34 min. Under these conditions, extraction yield of DHA was (1.76 ± 0.04%). When the concentrations of crude extract were 0.5 and 8 mg/mL, the spore germination inhibition rates of A. alternata were (17.00 ± 2.05%) and (92.56 ± 2.01%), which were 3.34 and 1.15 times that of the DHA standard, respectively.ConclusionsHomogenate extraction technology is a fast and efficient method for extracting DHA from A. hedinii. The crude extract has significant antifungal activity against A. alternata and is inexpensive, providing possible DHA usage in the prevention and treatment of plant pathogenic fungi.HighlightsThe optimum conditions of the extraction of DHA from A. hedinii by homogenate extraction were obtained. DHA has antifungal activity against A. alternata. Compared with pure DHA, the crude extract has stronger antifungal activity against A. alternata.
研究领域:
中药学
·
植物化学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
AICHE JOURNAL
·
2022
·Vol. 68
·期 8
·e17711
·
IF 4.167
Yingying Cao,Xin Tan,Guoxiong Zhan,Qiongguang Li,Hui Wang,Zengxi Li
One of the challenges to obtain high-quality natural active substances is the selective separation of the target compound from its analogues. In this study, ionic liquids (ILs), with design flexibility, were proposed to separate artemisitene and artemisinin, typical examples of natural analogues. Based on COSMO-RS calculation, several ILs were selected to separate artemisitene/artemisinin by experiment. It was demonstrated that the aqueous solution of N -allyl- N,N,N -trimethylammonium chloride ([AA][Cl]) exhibited excellent capability for selective separation of the two compounds. Under the optimal conditions (40°C, 1 h), the separation selectivity of artemisitene/artemisinin could reach 12.23 when the initial impurity content was only 0.8 wt%. Spectroscopic analysis and molecular dynamics indicated that π – π complexation between artemisitene and [AA][Cl] plays a major role in this separation process. Moreover, the process of multistage cross-flow extraction was compared with counter-flow extraction, and the latter one exhibited advantages in energy consumption and product yield.
研究领域:
化学工程
·
天然产物化学
·
药物化学
✓ 已验证
DOI
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
·
2022
·
IF 5.518
Minjia Meng,Suao Wang,Jingyi Dai,Yi Li,Yonghai Feng,Yu Zhu,Hongbo Zhang,Yan Liu
In this work, a simple metal-organic framework (MOF) material, UiO-66-NH 2 , was prepared for the highly efficient separation of artemisinin (Art) and artesunate (Aru). Selective adsorption tests showed that UiO-66-NH 2 presented a much higher selectivity toward Aru than Art ( α Aru/Art = 40.74). The N 2 adsorption-desorption isotherm results of UiO-66-NH 2 indicated a suitable pore size to enable the free entry of Art and Aru. Contact angle analysis indicated that UiO-66-NH 2 is hydrophilic with the -NH 2 group, and can interact with the hydrophobic Aru through hydrogen bonding between the -NH 2 and -COOH groups, which is not possible with the hydrophobic Art. The selective adsorption of Aru onto UiO-66-NH 2 may be attributed to three factors: pore size, functional groups, and difference in hydrophobic/hydrophilic characteristics between the adsorbent and adsorbate. Molecularly imprinted polymers (MIPs) were prepared using Aru as a template for selective adsorption experiments to verify the excellent selectivity of UiO-66-NH 2 . The adsorption amount (65.24 mg g −1 ) and selectivity factor ( α Aru/Art = 40.74) of UiO-66-NH 2 toward Aru were significantly better than those of the MIPs (2.039 mg g −1 and 3.072, respectively). The binding capacity and better selectivity of UiO-66-NH 2 provide evidence supporting the potential of MOF adsorbents for the separation of various analogous molecules.
研究领域:
药学
·
材料科学
·
分离技术
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF ADHESION AND ADHESIVES
·
2023
·
IF 3.4
Yashuang Ding,Qiongfang Li,Wenya Tang,Yahui Pan,Rongrong Nie,Xiangfeng Meng
Objectives This study aims to investigate the potential effect of a primer containing Artemisinin (ART) or its derivative—dihydroartemisinin (DHA) on the dentin endogenous MMPs activity and resin bonding durability under etch-and-rinse mode. Materials and methods Molecular docking was applied for evaluating the potential interactions of MMP-2 and MMP-9 with ART and DHA. Then human third molars were randomly assigned to six groups, after etch-and-rinse treatment, pretreated with the primers containing 0.25, 0.5 mg/mL ART, 0.25, 0.5 mg/mL DHA and 2% chlorhexidine (CHX) for 2 min, respectively, while one untreated group was served as the control group. The endogenous MMPs activity of demineralized dentin was tested with in situ zymography test and zymographic assay. Following the etch-and-rinse bonding process with a universal resin bond , the specimens of the microtensile bond strength (μTBS) and nanoleakage were tested with or without 10,000 °C thermocycling and 6-month storage in artificial saliva at 37 °C. Results Molecular docking showed that ART and DHA combined with MMP-2 and MMP-9 through forming covalent bonds with the zinc ion of MMPs. Compared with the control group, the ART, DHA and CHX groups showed less endogenous MMPs activity, and the MMPs activity of 0.5 mg/mL DHA group had no significant difference from that of 2% CHX group. Ageing condition reduced the μTBS values dramatically and also aggravated the nanoleakage of all the groups, specifically, the control group showed lower μTBS value and a broader, thicker and more consecutive silver deposition than other groups. Conclusions The primer containing ART or DHA could preserve bond durability and slow down the nanoleakage of resin-dentin interface over time through inhibiting the endogenous MMPs activity.
研究领域:
牙科学
·
分子生物学
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
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
·
传染病学
·
纳米医学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
·
2020
·
IF 2.997
Liqing Chai,Rongrong Wang,Yan Wang,Wenju Guo,Ning Li,Hengtong Zuo,Yidan Wang,Danyu Duan,Guolian Ren,Bin Zheng,Ruili Wang,Shuqiu Zhang
Artemisinin (ART) drugs showed declining plasma concentrations after repeated oral dosing, known as time-dependent pharmacokinetics (PK). ART and dihydroartemisinin (DHA) were adopted as representatives to evaluate the roles of first-pass effects and systemic metabolism in time-dependent PK by comparison of oral versus intravenous administration and 1 dose versus 5 consecutive doses PK in rats and dogs, respectively. The hepatic extraction ratio ( ER h ) and the intestinal elimination changes were further investigated in rats to distinguish the roles of hepatic first-pass effect or intestinal first-pass effect. The induction capacities of ARTs to cytochrome P450 ( CYP450 ) in rats and human cells were evaluated as well. For ART, only the oral groups showed time-dependent PK. A fairly high ER h that obtained for ART was not sensitive to multiple oral doses. An increased elimination and CYP450 expression have also been found in the intestine. For DHA, though a significant CYP450 induction was observed, neither time-dependent PK nor changes in the first-pass effects was found. In conclusion, time-dependent PK of ART was mainly caused by the increased intestinal first-pass effect rather than hepatic first-pass effect or systemic metabolism. DHA was not involved in auto-induction elimination, thus showing no time-dependent PK.
研究领域:
药理学
·
药物代谢
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Oncology
·
2020
·
IF 4.848
Chen Ying,Li Rui,Zhu Yuqi,Zhong Sixia,Qian Jinjun,Yang Dongqing,Jurczyszyn Artur,Beksac Meral,Gu Chunyan,Yang Ye
The discovery of artemisinin (ART) for malaria treatment won the 2015 Nobel Prize in Medicine, which inspired the rediscovery and development of ART for the treatment of other diseases including cancer. In this study, we investigated the potential therapeutic effect of ART and dihydroartemisinin (DHA) on multiple myeloma (MM) cells including primary MM cells and in 5TMM3VT mouse model. Both in vitro and in vivo experiments showed that DHA might be a more promising anti-MM agent with significantly improved efficacy compared to ART. Mechanistic analyses suggested that DHA activated the mitochondrial apoptotic pathway by interacting with ferrous (Fe2+) ions and oxygen to produce reactive oxygen species (ROS). Intriguingly, DHA could reverse the upregulated expression of B-cell lymphoma 2 (Bcl-2) protein, a typical mitochondrial apoptotic marker, induced by dexamethasone (Dexa) in MM. We further demonstrated that DHA treatment could overcome Dexa resistance and enhance Dexa efficacy in MM. Additionally, DHA combined with Dexa resulted in increased ROS production and cytochrome C translocation from the mitochondria to the cytoplasm, resulting in alterations to the mitochondrial membrane potential and caspase-mediated apoptosis. In summary, our study demonstrated that DHA was superior to ART in MM treatment and overcame Dexa resistance both in vitro and in vivo, providing a promising therapeutic strategy for MM therapy.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Yaru Zhang,Wei He,Yawei Du,Ying Du,Chao Zhao,Ying Zhang,Hu Zhang,Lihong Yin,Xinsong Li
Objective The dimeric artesunate phospholipid conjugate (Di-ART-GPC) is a novel amphipathic artemisinin derivative, which can be assembled into liposomes. Di-ART-GPC liposomes were prepared and evaluated as potential anti-inflammatory agents for rheumatic arthritis (RA). Methods Di-ART-GPC was assembled into liposomes utilizing thin film dispersion-high pressure homogenization. Dynamic light scattering (DLS), transmission electron microscopy (TEM), and electron cryo microscopy (cryo-EM) were employed to characterize the liposomal size and morphology. The in vitro cytotoxicity of the Di-ART-GPC liposomes was assessed using Cell Counting Kit-8 (CCK8). The anti-inflammatory effects were studied utilizing the inflammatory cell model. Finally, the in vivo efficacy of the Di-ART-GPC-conjugated liposomes was investigated using the arthritis rat model. Results The particle size of the Di-ART-GPC liposomes decreased to a narrow range of approximately 70 nm following high-pressure homogenization. The in vitro studies revealed low cytotoxicity and good anti-inflammatory effects of the Di-ART-GPC liposomes, which exhibited significantly higher inhibition of the cell secretion of pro-inflammatory cytokines than ART . The in vivo evaluation confirmed that treatment with Di-ART-GPC resulted in a decline in the ankle swelling rate and a low inflammatory response compared with the model control and ART. Conclusion Di-ART-GPC liposomes demonstrate remarkable potential as novel ART-based anti-inflammatory agents for RA.
研究领域:
药理学
·
免疫学
·
风湿病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULES
·
2021
·Vol. 26
·期 18
·5698
·
IF 4.412
Sennan Qiao,Hansi Zhang,Fei Sun,Zhenyan Jiang
Artemisinin (also known as Qinghaosu), an active component of the Qinghao extract, is widely used as antimalarial drug. Previous studies reveal that artemisinin and its derivatives also have effective anti-inflammatory and immunomodulatory properties, but the direct molecular target remains unknown. Recently, several reports mentioned that myeloid differentiation factor 2 (MD-2, also known as lymphocyte antigen 96) may be the endogenous target of artemisinin in the inhibition of lipopolysaccharide signaling. However, the exact interaction between artemisinin and MD-2 is still not fully understood. Here, experimental and computational methods were employed to elucidate the relationship between the artemisinin and its inhibition mechanism. Experimental results showed that artemether exhibit higher anti-inflammatory activity performance than artemisinin and artesunate. Molecular docking results showed that artemisinin, artesunate, and artemether had similar binding poses, and all complexes remained stable throughout the whole molecular dynamics simulations, whereas the binding of artemisinin and its derivatives to MD-2 decreased the TLR4(Toll-Like Receptor 4)/MD-2 stability. Moreover, artemether exhibited lower binding energy as compared to artemisinin and artesunate, which is in good agreement with the experimental results. Leu61, Leu78, and Ile117 are indeed key residues that contribute to the binding free energy. Binding free energy analysis further confirmed that hydrophobic interactions were critical to maintain the binding mode of artemisinin and its derivatives with MD-2.Keywords:molecular dynamics simulation;myeloid differentiation factor 2;artemisinin;anti-inflammatory;binding free energy
研究领域:
药理学
·
免疫学
·
分子生物学
·
计算化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2020
·
IF 7.182
Yingying Cao,Yongqiang Zhang,Ying Zhang,Ling Wang,Lunchao Lv,Xifei Ma,Shaojuan Zeng,Hui Wang
Artemisinin is mainly derived from Artemisia annua L. Since the leaves composition is complex, artemisinin purification faces great challenges. In this work, functional chitosan membranes were fabricated by a one-step hydrolysis method through grafting long-chain alkyl group on the surface of chitosan to increase its hydrophobicity. The as-prepared membranes were used to adsorb wax oil ( i.e. , the impurity components) in Artemisia annua L. and to avoid co-precipitation of wax oil along with artemisinin using the crystallization technique for purification. Octyl-trimethoxysilane modified chitosan membrane (FCM-C 8 ) showed excellent capability to intensify this purification process. The product purity could reach more than 98 % using one crystallization step under the optimal conditions, and in this case, adsorption capacity of FCM-C 8 for wax oil was 478.9 mg/g. In addition, the adsorption kinetics and mechanism of wax oil on FCM-C 8 were studied. The membrane can simultaneously adsorb multiple components in wax oil through interactions like electrostatic forces, hydrogen bondings.
研究领域:
生物工程
·
制药工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
·
2018
·Vol. 37
·期 1
·1-14
·
IF 6.217
Yao Yuyuan,Guo Qinglong,Cao Yue,Qiu Yangmin,Tan Renxiang,Yu Zhou,Zhou Yuxin,Lu Na
Background Cancer-associated fibroblasts (CAFs) are activated fibroblasts associated with cancer. They have an important role in tumor growth and metastasis. Artemisinin (ART) is a sesquiterpene lactone extracted from Chinese herb qinghao, and artemether (ARM), artesunate (ARS) and dihydroartemisinin (DHA) were synthesized derivatives of artemisinin, which also have anti-malarial and anti-cancer effects such as artemisinin.Methods In this study, we investigated the in-vitro and in-vivo effects of artemisinin derivatives on inactivating cancer-associated fibroblasts and uncovered its underlying mechanism.Results We demonstrated that ARS and DHA could revert L-929-CAFs and CAFs from activated to inactivated state in vitro. Mechanically, ARS and DHA could suppress TGF-β signaling to inhibit activation of L-929-CAFs and CAFs, and decreased interaction between tumor and tumor microenvironment. The results showed that ARS and DHA could suppress CAFs-induced breast cancer growth and metastasis in the orthotopic model. Conformably, ARS and DHA suppressed TGF-β signaling to inactivate cancer-associated fibroblasts and inhibit cancer metastasis in vivo.Conclusion sArtemisinin derivatives are potential therapeutic agents for the treatment of breast cancer.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 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）