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| 1 | Artesunate synergizes with sorafenib to induce ferroptosis in hepatocellular carcinoma显示文摘Sorafenib is the first-line medication for advanced hepatocellular carcinoma(HCC),but it can only extend limited survival.It is imperative to find a combination strategy to increase sorafenib efficacy.Artesunate is such a preferred candidate,because artesunate is clinically well-tolerated and more importantly both drugs can induce ferroptosis through different mechanisms.In this study we investigated the combined effect of sorafenib and artesunate in inducing ferroptosis of HCC and elucidated the involved molecular mechanisms.We showed that artesunate greatly enhanced the anticancer effects of low dose of sorafenib against Huh7,SNU-449,and SNU-182 HCC cell lines in vitro and against Huh7 cell xenograft model in Balb/c nude mice.The combination index method confirmed that the combined effect of sorafenib and artesunate was synergistic.Compared with the treatment with artesunate or sorafenib alone,combined treatment induced significantly exacerbated lipid peroxidation and ferroptosis,which was blocked by N-acetyl cysteine and ferroptosis inhibitors liproxstatin-1 and deferoxamine mesylate,but not by inhibitors of other types of cell death(z-VAD,necrostatin-1 and belnacasan).In Huh7 cells,we demonstrated that the combined treatment induced oxidative stress and lysosome-mediated ferritinophagy,two essential aspects of ferroptosis.Sorafenib at low dose mainly caused oxidative stress through mitochondrial impairments and SLC7A11-invovled glutathione depletion.Artesunate-induced lysosome activation synergized with sorafenib-mediated pro-oxidative effects by promoting sequential reactions including lysosomal cathepsin B/L activation,ferritin degradation,lipid peroxidation,and consequent ferroptosis.Taken together,artesunate could be repurposed to sensitize sorafenib in HCC treatment.The combined treatment can be easily translated into clinical applications. | Zhong-jie Li Hui-qi Dai Xiao-wei Huang Ji Feng Jing-huan Deng Zi-xuan Wang Xiao-mei Yang Yu-jia Liu Yong Wu Pan-hong Chen Huan Shi Ji-gang Wang Jing Zhou Guo-dong Lu | 2021 | Acta Pharmacologica Sinica2021，42，2： | 31 |
| 2 | A Pilot Study of the Therapeutic Efficacy and Mechanism of Artesunate in the MRL/lpr Murine Model of Systemic Lupus Erythematosus显示文摘Recent evidence indicates that artesunate has immunomodulatory properties that might be useful for treating autoimmune disease.In this study,we conducted a pilot study and explored the effect and mechanism of artesunate on the treatment of systemic lupus erythematosus using an MRL/lpr murine model.MRL/lpr mice were divided into control,cyclophosphamide(CTX)and artesunate treatment groups.Blood was collected to measure serum levels of creatinine,antinuclear antibody(ANA)and anti-double-stranded DNA(anti-dsDNA)antibody.Twenty-four-hour urine was collected to measure levels of proteinuria.The concentration of monocyte chemotactic protein-1(MCP-1)in serum and urine was measured.The expression of MCP-1 in kidney was detected by Western blot and immunohistochemistry assay,respectively.The expression of B cell activating factor(BAFF)in spleen was determined by real time-PCR and immunoblotting.We found that artesunate significantly increased the survival rate,body weight and blood leukocyte counts,and reduced the serum levels of ANA and anti-dsDNA antibody titer,24 h urinary protein,and serum creatinine.Our results indicated that artesunate could decrease MCP-1,major pro-inflammation cytokine,in serum,urine and kidney.We also found that the level of BAFF,the major B cell activation factor,was decreased in artesunate treated MRL/lpr mice.Its efficacy was comparable with that of CTX in this study.Taken together,we have demonstrated that artesunate can inhibit the progression of disease and reverse the pathologic lesion of lupus nephritis. | Ouyang Jin Huayong Zhang Zhifeng Gu Shengnan Zhao Ting Xu Kangxing Zhou Bo Jiang Jie Wang Xiaofeng Zeng Lingyun Sun | 2009 | Cellular & Molecular Immunology2009，6，6： | 20 |
| 3 | Artesunate inhibits growth and induces apoptosis in human osteosarcoma HOS cell line in vitro and in vivo显示文摘This paper aims to investigate the effects of artesunate (ART) on growth and apoptosis in human osteosarcoma HOS cell line in vitro and in vivo and to explore the possible underlying mechanisms.Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.The induction of apoptosis was detected by light and transmission electron microscopy and flow cytometry.Western blot analysis was used to investigate the related mechanisms.Nude mice were further employed to investigate the antitumour activity of ART in vivo.MTT assay results demonstrated that ART selectively inhibits the growth of HOS cells in a dose-and time-dependent manner.Based on the findings of light and transmission electron microscopy,Hoechst 33258 staining,and fluorescein isothiocyanate (FITC)-annexin V staining,the cytotoxicity of ART in HOS cells occurs through apoptosis.With ART treatment,cytosolic cytochrome c was increased,Bax expression was gradually upregulated,Bcl-2 expression was downregulated,and caspase-9 and caspase-3 were activated.Thus,the intrinsic apoptotic pathway may be involved in ART-induced apoptosis.Cell cycle analysis by flow cytometry indicated that ART may induce cell cycle arrest at G2 /M phase.In nude mice bearing HOS xenograft tumours,ART inhibited tumour growth and regulated the expressions of cleaved caspase-3 and survivin,in agreement with in vitro observations.ART has a selective antitumour activity against human osteosarcoma HOS cells,which may be related to its effects on induction of apoptosis via the intrinsic pathway.The results suggest that ART is a promising candidate for the treatment of osteosarcoma. | Qiang xu Zhao-xu LI Hui-qin PENG Zheng-wang SUN Rui-lin CHENG Zhao-ming YE Wei-xu | 2011 | Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)2011，12，4： | 14 |
| 4 | Artesunate attenuates LPS-induced osteoclastogenesis by suppressing TLR4/TRAF6 and PLCγ1-Ca^(2+)-NFATc1 signaling pathway显示文摘In chronic infectious diseases caused by gram-negative bacteria,such as osteomyelitis,septic arthritis,and periodontitis,osteoclastic activity is enhanced with elevated inflammation,which disturbs the bone homeostasis and results in osteolysis.Lipopolysaccharide(LPS),as a bacteria product,plays an important role in this process.Recent evidence shows that an antimalarial drug artesunate attenuates LPS-induced osteolysis independent of RANKL.In this study we evaluated the effects of artesunate on LPS-induced osteoclastogenesis in vitro and femur osteolysis in vivo,and explored the mechanisms underlying the effects of artesunate on LPS-induced osteoclast differentiation independent of RANKL.In preosteoclastic RAW264.7 cells,we found that artesunate(1.56?12.5μM)dose dependently inhibited LPS-induced osteoclast formation accompanied by suppressing LPS-stimulated osteoclast-related gene expression(Fra-2,TRAP,Cathepsin K,β3-integrin,DC-STAMP,and Atp6v0d2).We showed that artesunate(3.125?12.5μM)inhibited LPS-stimulated nuclear factor of activated T cells c1(NFATc1)but not NF-κB transcriptional activity;artesunate(6.25,12.5μM)significantly inhibited LPS-stimulated NFATc1 protein expression.Furthermore,artesunate treatment markedly suppressed LPS-induced Ca2+influx,and decreased the expression of PP2B-Aα(calcineurin)and pPLCγ1 in the cells.In addition,artesunate treatment significantly decreased the expression of upstream signals TLR4 and TRAF6 during LPS-induced osteoclastogenesis.Administration of artesunate(10 mg/kg,ip)for 8 days effectively inhibited serum TNF-αlevels and ameliorated LPS(5 mg/kg,ip)-induced inflammatory bone loss in vivo.Taken together,artesunate attenuates LPS-induced inflammatory osteoclastogenesis by inhibiting the expression of TLR4/TRAF6 and the downstream PLCγ1-Ca^2+-NFATc1 signaling pathway.Artesunate is a valuable choice to treat bone loss induced by gram-negative bacteria infection or inflammation in RANKL-independent pathway. | Xiang-zhou Zeng Yue-yang Zhang Qin Yang Song Wang Bin-hua Zou Yan-hui Tan Min Zou Shu-wen Liu Xiao-juan Li | 2020 | Acta Pharmacologica Sinica2020，41，2： | 12 |
| 5 | Artemisinin anti-malarial drugs in China显示文摘Discovered by Youyou Tu, one of the 2015 Nobel Prize winners in Physiology or Medicine,together with many other Chinese scientists, artemisinin, artemether and artesunate, as well as other artemisinins, have brought the global anti-malarial treatment to a new era, saving millions of lives all around the world for the past 40 years. The discoveries of artemisinins were carried out beginning from the 1970 s, a special period in China, by hundreds of scientists all together under the 'whole nation'system. This article focusing on medicinal chemistry research, briefly introduced the discovery and invention course of the scientists according to the published papers, and highlighted their academic contribution and achievements. | Zongru Guo | 2016 | Acta Pharmaceutica Sinica B2016，6，2： | 11 |
| 6 | Effect of artesunate supplementation on bacterial translocation and dysbiosis of gut microbiota in rats with liver cirrhosis显示文摘AIM: To evaluate the effect of artesunate(AS) supplementation on bacterial translocation(BT) and gut microbiota in a rat model of liver cirrhosis. METHODS: Fifty-four male Sprague-Dawley rats were randomly divided into a normal control group(N), a liver cirrhosis group(M) and a liver cirrhosis group intervened with AS(MA). Each group was sampled at 4, 6 and 8 wk. Liver cirrhosis was induced by injection of carbon tetrachloride(CCl4), intragastric administration of 10% ethanol, and feeding a high fat diet. Rats in the MA group were intragastrically administered with AS(25 mg/kg body weight, once daily). Injuries of the liver and intestinal mucosa were assessed by hematoxylineosin or Masson's trichrome staining. Liver index was calculated as a ratio of the organ weight(g) to body weight(g). The gut microbiota was examined by automated ribosomal intergenic-spacer analysis of fecal DNA. BT was assessed by standard microbiological techniques in the blood, mesenteric lymph nodes(MLNs), liver, spleen, and kidney. RESULTS: Compared to group N, the body weight was reduced significantly in groups M and MA due to the development of liver cirrhosis over the period of 8 wk. The body weight was higher in group MA than in group M. The liver indices were significantly elevated at 4, 6 and 8 wk in groups M and MA compared to group N. AS supplementation partially decreased the liver indices in group MA. Marked histopathologic changes in the liver and small intestinal mucosa in group M were observed, which were alleviated in group MA. Levels of pro-inflammatory interleukin-6 and tumor necrosis factor-α were significantly elevated at 8 wk in ileal homogenates in group M compared to group N, which were decreased after AS supplementation in group MA. The dysbiosis of gut microbiota indicated by the mean diversity(Shannon index) and mean similarity(Sorenson index) was severe as the liver cirrhosis developed, and AS supplementation had an apparent intervention effect on the dysbiosis of gut microbiota at 4 wk. The occurrence of BT was increased in the liver of group M compared to that of group N. AS supplementation reduced BT in group MA at 8 wk. BT also occurred in the MLNs, spleen, and kidney, which was reduced by AS supplementation. BT was not detected in the blood in any group.CONCLUSION: Dysbiosis of gut microbiota, injury of intestinal mucosal barrier and BT occurred as liver cirrhosis progressed, which might enhance inflammation and aggravate liver injury. AS may have other nonantimalarial effects that modulate gut microbiota,inhibit BT and alleviate inflammation, resulting in a reduction in CCl4, alcohol and high fat-caused damages to the liver and intestine. | Yun-Xia Chen Li-Na Lai Hui-Ying Zhang Yang-Hui Bi Li Meng Xu-Jiong Li Xiao-Xia Tian Li-Min Wang Yi-Min Fan Zhong-Fu Zhao De-Wu Han Cheng Ji | 2016 | World Journal of Gastroenterology2016，22，10： | 10 |
| 7 | 甘草甜素治疗慢性乙型肝炎疗效观察 | 宋星宏 | 1997 | 中国中西医结合杂志1997，17，8： | 5 |
| 8 | Synergistic antitumor activity of artesunate and HDAC inhibitors through elevating heme synthesis via synergistic upregulation of ALAS1 expression显示文摘Artemisinin and its derivatives(ARTs) were reported to display heme-dependent antitumor activity. On the other hand, histone deacetylase inhibitors(HDACi) were known to be able to promote heme synthesis in erythroid cells. Nevertheless, the effect of HDACi on heme homeostasis in nonerythrocytes remains unknown. We envisioned that the combination of HDACi and artesunate(ARS)might have synergistic antitumor activity through modulating heme synthesis. In vitro studies revealed that combination of ARS and HDACi exerted synergistic tumor inhibition by inducing cell death. Moreover, this combination exhibited more effective antitumor activity than either ARS or HDACi monotherapy in xenograft models without apparent toxicity. Importantly, mechanistic studies revealed that HDACi coordinated with ARS to increase 5-aminolevulinate synthase(ALAS1) expression, and subsequent heme production, leading to enhanced cytotoxicity of ARS. Notably, knocking down ALAS1 significantly blunted the synergistic effect of ARS and HDACi on tumor inhibition, indicating a critical role of ALAS1 upregulation in mediating ARS cytotoxicity. Collectively, our study revealed the mechanism of synergistic antitumor action of ARS and HDACi. This finding indicates that modulation of heme synthesis pathway by the combination based on ARTs and other heme synthesis modulators represents a promising therapeutic approach to solid tumors. | Cai-Ping Chen Kun Chen Zhiqi Feng Xiaoan Wen Hongbin Sun | 2019 | Acta Pharmaceutica Sinica B2019，9，5： | 4 |
| 9 | Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway显示文摘AIM:To study the braking effectiveness of artesunate on transforming growth factor(TGF)-β2 mediated epithelial-mesenchymal transition(EMT)in retinal pigment epithelium(RPE)in vitro.METHODS:The fostered ARPE-19 cells were processed with artesunate alone or combined with the TGF-β2.The CCK-8 examination was utilized to test the cell propagation.Cell migration was detected by scratch as well as the Transwell examination.The EMT characters and activation of PI3K/Akt signal channel were estimated by Western blotting and immunofluorescence.The Western blotting was utilized in order to confirm the vitreous of controls as well as patients with proliferative vitreoretinopathy(PVR)were collected and the levels of PI3K,phospho-PI3K,Akt.RESULTS:Disposal of ARPE-19 cells with artesunate(50-150μmol/L)obviously suppressed their propagation and immigration,which dependent on the concentration and time.Artesunate suppressed the EMT which was induced by TGF-β2 in ARPE-19 cells through sustaining the expression of vimentin andα-SMA through the suppression of PI3K,phospho-PI3K,phospho-Akt and Akt.Levels of PI3K,phospho-PI3K,AKT and phospho-Akt was increased in the vitreous in PVR(P<0.05).CONCLUSION:Such findings indicate that PI3K/Akt signal channel is highly activated in vitreous of PVR.Artesuante is an operative depressor of the propagation,immigration and TGF-β2-mediated EMT of ARPE-19 cells by reduced the expression of PI3K/Akt channel. | Zi-Yi Wang Yu Zhang Ling-Dan Wu Jie Chen Mei-Ling Chen Ci-Min Chen Qi-Hua Xu | 2022 | International Journal of Ophthalmology(English edition)2022，15，2： | 4 |
| 10 | Research Progress on Artemisinin and Its Derivatives against Hematological Malignancies显示文摘Although current therapeutic methods against hematological malignancies are effective in the early stage,they usually lose their effectiveness because of the development of drug resistances.Seeking new drugs with significant therapeutic effects is one of the current research hotspots.Artemisinin,an extract from the plant Artemisia annua Linne,and its derivatives have excellent antimalarial effects in clinical applications as well as excellent safety.Recent studies have documented that artemisinin and its derivatives(ARTs)also have significant effects against multiple types of tumours,including hematological malignancies.This review focuses on the latest research achievements of ARTs in the treatment of hematological malignancies as well as its mechanisms and future applications.The mechanisms of ARTs against different types of hematological malignancies mainly include cell cycle arrest,induction autophagy and apoptosis,inhibition of angiogenesis,production of reactive oxygen species,and induction of differentiation.Additionally,the review also summarizes the anticancer effects of ARTs in many drug-resistant hematological malignancies and its synergistic effects with other drugs. | LI Ying SHAN Ning-ning SUI Xiao-hui | 2020 | Chinese Journal of Integrative Medicine2020，26，12： | 1 |
| 11 | Anti-malaria drug artesunate protects bronchial epithelium from DNA damage induced by asthma显示文摘OBJECTIVE To investigate the genome protective effects of anti-malaria drug,artesunate in an experimental allergic asthma model.METHODS Mice were sensitized on day 0 and 7 and challenged on day 14 with 100μg house dust mite(HDM)via intratracheal administration.Artesunate(30mg·kg-1)was administered intra-peritoneally on day 6,7,8,13,14 and 15.Samples were collected on day 1,3 and 5 post last HDM-challenge for analysis of air way inflammation and DNA damage.Lung sections were immunofluorescence(IF)-stained for DNA double strand breaks(DSBs)markers,γH2AX and 53BP1.Levels of DNA repair proteins Ku70 and Rad51,which are involved in non-homologous end joining(NHEJ)and homologous recombination(HR)DNA DSB repair pathways respectively,were measured.To quantify cell death in asthmatic lung,TUNEL staining was performed.Comet assay,a single cell gel electrophoresis was employed to detect DNA damage induced by HDM in BEAS-2Bhuman bronchial epithelial cell line,in vitro.RESULTS Artesunate treatment significantly reduces immune cells infiltration in BAL fluid of asthmatic mice,collected on day 3 and 5 post-challenge.Importantly,artesuante is able to protect bronchial epithelium from DNA DSBs induced by asthma,as detected by the reduced level of γH2AX and 53BP1 foci formation in the nucleus.This genome protective effect is evident even on day 1 post-challenge,when immune cells infiltration remained high.This indicates that artesunate confers protection on bronchial epithelium in the presence of inflammation.Additionally,artesunate is also able to reduce cell death in asthmatic lung revealed by TUNEL assay and cleaved caspase 3 level.Interestingly,the levels of DNA repair proteins in artesuante-treated asthmatic mice are unchanged as compared to HDM-only mice,suggesting that artesunate treatment does not augment the level of DNA repair proteins.When human bronchial epithelial BEAS-2 Bcells were exposed to HDMin vitro,we observed an increase in the levels of DNA damage.Artesunate(60μmol·L-1)co-incubated with HDM is not able to prevent direct DNA damage induced by the allergen.Together,these studies suggest that the genome protective effect of artesunate in vivo may be attributed to physiological effects(such as its anti-inflammatory effects)rather than serving to directly prevent DNA damage.CONCULSION This study highlights a novel role for artesunate in protecting bronchial epithelial cells from asthma-induced DNA damage. | TzeKheeCHAN WNFeliciaTAN BevinPENGELWARD WSFredWONG | 2015 | 中国药理学与毒理学杂志2015，29，S1： | 1 |
| 12 | Single-cell transcriptome analysis reveals the regulatory effects of artesunate on splenic immune cells in polymicrobial sepsis显示文摘Sepsis is characterized by a severe and life-threatening host immune response to polymicrobial infection accompanied by organ dysfunction.Studies on the therapeutic effect and mechanism of immunomodulatory drugs on the sepsis-induced hyperinflammatory or immunosuppression states of various immune cells remain limited.This study aimed to investigate the protective effects and underlying mechanism of artesunate(ART)on the splenic microenvironment of cecal ligation and puncture-induced sepsis model mice using single-cell RNA sequencing(scRNA-seq)and experimental validations.The scRNA-seq analysis revealed that ART inhibited the activation of pro-inflammatory macrophages recruited during sepsis.ART could restore neutrophils’chemotaxis and immune function in the septic spleen.It inhibited the activation of T regulatory cells but promoted the cytotoxic function of natural killer cells during sepsis.ART also promoted the differentiation and activity of splenic B cells in mice with sepsis.These results indicated that ART could alleviate the inflammatory and/or immunosuppressive states of various immune cells involved in sepsis to balance the immune homeostasis within the host.Overall,this study provided a comprehensive investigation of the regulatory effect of ART on the splenic microenvironment in sepsis,thus contributing to the application of ART as adjunctive therapy for the clinical treatment of sepsis. | Jiayun Chen Xueling He Yunmeng Bai Jing Liu Yin Kwan Wong Lulin Xie Qian Zhang Piao Luo Peng Gao Liwei Gu Qiuyan Guo Guangqing Cheng Chen Wang Jigang Wang | 2023 | Journal of Pharmaceutical Analysis2023，13，7： | 1 |
| 13 | 青蒿琥酯对肺癌A549细胞生物学行为的影响显示文摘目前,作为肺癌的常见治疗方法之一的化疗,由于其治疗过程中产生的耐药、化疗药物本身的毒副作用等原因,使得其效果已远不如从前,促使寻找更加安全有效的治疗药物成为当务之急。中药是我国医药文化的精粹,中药制剂抗肿瘤效应也越来越引发人们关注。 | 王静 韩福才 贺莉 师如意 杨斌 | 2016 | 中国药物与临床2016，16，7： | 1 |
| 14 | Enhanced lysosomal function is critical for paclitaxel resistance in cancer cells: reversed by artesunate显示文摘The mechanism underlying the resistance of cancer cells to chemotherapeutic drug varies with different cancer cells.Recent evidence shows that lysosomal function is associated with drug resistance of cancer cells.Artesunate,a derivative of artemisinin,displays broad antitumor activity and direct cytotoxicity on various tumor cells.Our previous study shows that artesunate increases autophagosome accumulation,while significantly decreases autolysosome number in cancer cells,suggesting that artesunate might impair the lysosomal function.In this study,we investigated the effects of artesunate on lysosomal function and its relationship with chemotherapeutic drug resistance in cancer cells.We found that the lysosomal function was significantly enhanced in two drug-resistant(A549/TAX and A549/DDP)cells.Furthermore,we showed that the enhanced lysosomal function by overexpression of transcription factor EB(TFEB)significantly increased MCF-7 cells resistance to doxorubicin(DOX),whereas the decreased lysosomal function by TFEB-knockdown or lysosome inhibitor chloroquine increased MCF-7 cells sensitivity to DOX.Treatment of A549/TAX cells with artesunate(2.5–50μM)dose-dependently inhibited lysosomal function and the clearance of dysfunctional mitochondria,and induced cell apoptosis.Moreover,we demonstrated that artesunate exerted more potent inhibition on the resistant(A549/TAX and MCF-7/ADR)cells with higher activity of lysosomal function.Our results suggest that artesunate or other inhibitors of lysosomal function would be potential in the treatment of cancer cells with drug resistance caused by the enhanced lysosomal function. | Zhe Li Yu-ting Zhu Min Xiang Jun-lan Qiu Shou-qing Luo Fang Lin | 2021 | Acta Pharmacologica Sinica2021，42，4： | 1 |
| 15 | Publication process involving the discovery of artemisinin (qinghaosu) before 1985显示文摘All the original references were provided by the Nobel Laureate Youyou Tu. The publication process involving the discovery of artemisinin was collected and sorted by her first Ph D student, Associate Professor Man-Yuan Wang. Through the publication of this article, the journal expects to provide a reference to the scientists who dedicated to the research of artemisinin, especially those who are interested in the discovery process of artemisinin. | Man-Yuan Wang | 2016 | Asian Pacific Journal of Tropical Biomedicine2016，6，6： | 1 |
| 16 | Phosphate imbalance conducting by BPs-based cancer-targeting phosphate anions carrier induces necrosis显示文摘As a vital nutrient closely related to the cance r-cells proliferation,phosphate anions have been paid great attention as a promising anticancer agent.Generally,the transport of phosphate anions depends on a protein transport system which is regulated by ion homeostasis regulations.Herein,we designed a reactive anionic nanocarrier based on black phosphorus nanosheets(BPs)and artesunate(ART),which could enter cells through endocytosis to generate phosphate anions,avoiding the regulation of cell homeostasis.The ionic nanocarrier was coated by polydopamine to defend BPs and ART and functionalized by folate(FA)and hyaluronic acid(HA)for targeting factor.With the anchoring groups FA/HA targeted the carrier into cells,polydopamine coating decomposed to expose ART for further generating reactive oxygen species(ROS)in cancer cell microenvironment,providing oxidation conditions.Next,ROS generated by ART makes BPs decompose to phosphate anions with effectively speed,giving rise to the destruction of ion homeostasis to induce necro sis and inhibit the proliferation for cancer cells.In consequence,this research provides novel idea and direction for the ionic carriers and tumor therapeutics. | Chunmeng Ma Jinlong Zhang Yuan Zhang Chen Ma Minrui Ma Fanpeng Ran Xiaoyan Liu Haixia Zhang | 2021 | Chinese Chemical Letters2021，32，4： | 1 |
| 17 | Single-cell RNA sequencing deciphers the mechanism of sepsis-induced liver injury and the therapeutic effects of artesunate显示文摘Liver,as an immune and detoxification organ,represents an important line of defense against bacteria and infection and a vulnerable organ that is easily injured during sepsis.Artesunate(ART)is an anti-malaria agent,that also exhibits broad pharmacological activities including anti-inflammatory,immune-regulation and liver protection.In this study,we investigated the cellular responses in liver to sepsis infection and ART hepatic-protective mechanisms against sepsis.Cecal ligation and puncture(CLP)-induced sepsis model was established in mice.The mice were administered ART(10 mg/kg,i.p.)at 4 h,and sacrificed at 12 h after the surgery.Liver samples were collected for preparing single-cell RNA transcriptome sequencing(scRNA-seq).The scRNA-seq analysis revealed that sepsis-induced a dramatic reduction of hepatic endothelial cells,especially the subtypes characterized with proliferation and differentiation.Macrophages were recruited during sepsis and released inflammatory cytokines(Tnf,Il1b,Il6),chemokines(Ccl6,Cd14),and transcription factor(Nfkb1),resulting in liver inflammatory responses.Massive apoptosis of lymphocytes and abnormal recruitment of neutrophils caused immune dysfunction.ART treatment significantly improved the survival of CLP mice within 96 h,and partially relieved or reversed the above-mentioned pathological features,mitigating the impact of sepsis on liver injury,inflammation,and dysfunction.This study provides comprehensive fundamental proof for the liver protective efficacy of ART against sepsis infection,which would potentially contribute to its clinical translation for sepsis therapy. | Xue-ling He Jia-yun Chen Yu-lin Feng Ping Song Yin Kwan Wong Lu-lin Xie Chen Wang Qian Zhang Yun-meng Bai Peng Gao Piao Luo Qiang Liu Fu-long Liao Zhi-jie Li Yong Jiang Ji-gang Wang | 2023 | Acta Pharmacologica Sinica2023，44，9： | 1 |
| 18 | Antiplasmodial and antiulcer activities of Melanthera scadens显示文摘Objective:To evaluate the antimalarial and antiulcerogenic activities ofleaf exlracl and fractions of Melanthera scandens(M.scandens).Methods:The crude leaf extract(37-111 mg/kg)and fractions(chloroform,ethylacetale and methanol;78 mg/kg)of M.scadens were investigated for antiplasmodial activity against chloroquine-sensitive Plasmodium berghei infections in mice and for antiulcer activity against experimentally-induced ulcers.The antimalarial activity during early and established infections as well as prophylactic was investigated.Artesunate(5 mg/kg)and pyrimethamine(1.2 mg/kg)were used as positive controls.Thin films made from tail blood of each mouse were used to assess the level of parasitaemia of the mice.Antiulcer activity of the crude extract was also evaluated against indomethacin,ethanol and histamine induced ulcers.Results:The extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine-sensitive Plasmodium berghei infection in prophylactic,suppressive and curative models in mice.These reductions were statistically significant(P<0.00l),They also improved the mean survival time(MST)from 9.28 to 17.73 days as compared with the control(P<0.0l-0.001).The activities of extract/fractions were incomparable to that of the standard drugs ie.artesunate and pyrimethamine.On experimentally-induced ulcers,the extract inhibited indomethacin,ethanol and histamine induced ulcers.These inhibitions were statistically significant(P<0.001)and in a dose-dependent fashion.Conclusions:The antiplasmodial and antiulcerogenic effects of this plant may in part be mediated through the chemical constituents of the plant. | Jude E Okokon Ette O Etebong John A Udobang Jackson Obot | 2012 | Asian Pacific Journal of Tropical Biomedicine2012，2，1： | 1 |
| 19 | SYNTHESIS OF 11 α-HYDROXY-AND 11β-CHLORO-ARTEMISININ显示文摘11α-Hydroxy-and 11β-chloro-artemisinin have been prepared from | Ying Li~* De Wen LU | 1993 | Chinese Chemical Letters1993，4，2： | 0 |
| 20 | Artesunate attenuate chronic graft-versushost disease by regulating Th17/Treg balance显示文摘Objective To investigate the effects of artesunatetreatment on chronic graft-versus-host disease(cGVHD). Methods Recipient BALB /c mice received8 × 106 bone marrow cells with 8 × 106 spleen cells fromB10D2 mice. Artesunate solubilized in acetone was injectedintraperitoneally every day at a dose of 1 mg /kg onDay 28 after BMT. The clinical scores,survival and histopathologicaldamage were analyzed. The frequency ofTh17 and Tregs in PB and spleens from the mice wereevaluated by flow cytometry. In addition,CD4 + T cellsfrom the spleens of mice were cultured in vitro,thenstimulated with artesunate,the frequency of Th17 andTregs in these splenocytes were evaluated by flow cytometry. | 陈晓梅 | 2019 | China Medical Abstracts(Internal Medicine)2019，36，2： | 0 |
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