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1Reactive capillary hemangiomas: a novel dermatologic toxicity following anti-PD-1 treatment with SHR-1210显示文摘Objective: SHR-1210 is a new and promising anti-PD-1 agent for solid tumors. During the phase I study of SHR-1210, we encountered a novel but prevalent immune-related dermatologic toxicity: reactive capillary hemangiomas(RCHs). Thus we tried to summarize the features of RCHs and estimate their relationship with tumor response.Methods: This prospective observational study systematically enrolled 98 patients with advanced solid tumors from April 27th,2016 to June 8th, 2017 in the context of the phase I clinical study of SHR-1210. This report focused on the skin toxicities. Patients underwent entire skin inspection every two weeks while taking medication. The clinical course of RCHs was recorded and their association with tumor response was estimated. The data cut-off date was November 15th, 2017.Results: After a median follow-up of 242(range, 29–567) days, RCHs were observed in 85.7%(84/98) of patients on cutaneous/mucosal surfaces; 84.5%(71/84) of the RCHs were evaluated as grade 1 adverse events. No grade 3 or 4 RCHs were observed. The time of onset of RCHs was dose dependent and shortest in the 400 mg-dose cohort(P < 0.001). Spontaneous and complete regression of RCHs was observed both during and after treatment. The objective response rate of tumors for patients with RCHs was 28.9%(24/83). However, no responders were observed among the patients without RCHs.Conclusions: RCHs were prevalent but manageable during treatment with SHR-1210. It might add to the expanding literature regarding immune-related dermatologic adverse events.Xuelian Chen Lanying Ma Xi Wang Hongnan Mo Dawei Wu Bo Lan Dong Qu Hongtu Zhang Jing Huang Binghe Xu 2019Cancer Biology & Medicine2019,16,1:53
2Antimony speciation in the environment:Recent advances in understanding the biogeochemical processes and ecological effects显示文摘Antimony(Sb) is a toxic metalloid, and its pollution has become a global environmental problem as a result of its extensive use and corresponding Sb-mining activities. The toxicity and mobility of Sb strongly depend on its chemical speciation. In this review, we summarize the current knowledge on the biogeochemical processes(including emission, distribution,speciation, redox, metabolism and toxicity) that trigger the mobilization and transformation of Sb from pollution sources to the surrounding environment. Natural phenomena such as weathering, biological activity and volcanic activity, together with anthropogenic inputs, are responsible for the emission of Sb into the environment. Sb emitted in the environment can adsorb and undergo redox reactions on organic or inorganic environmental media, thus changing its existing form and exerting toxic effects on the ecosystem. This review is based on a careful and systematic collection of the latest papers during 2010–2017 and our research results, and it illustrates the fate and ecological effects of Sb in the environment.Mengchang He Ningning Wang Xiaojing Long Chengjun Zhang Congli Ma Qianyun Zhong Aihua Wang Ying Wang Aneesa Pervaiz Jun Shan 2019Journal of Environmental Sciences2019,31,1:40
3Variation of Cd concentration in various rice cultivars and derivation of cadmium toxicity thresholds for paddy soil by species-sensitivity distribution显示文摘It is imperative to derive an appropriate cadmium(Cd) health risk toxicity threshold for paddy soils to ensure the Cd concentration of rice grains meet the food safety standard. In this study, 20 rice cultivars from the main rice producing areas in China were selected, and a pot-experiment was conducted to investigate transformation of Cd in paddy soil-rice system with 0(CK), 0.3 mg kg–1(T1) and 0.6 mg kg–1(T2) Cd treatments in greenhouse. The results showed that Cd concentrations of rice grains existed significant difference(P<0.05) in 20 rice cultivars under the same Cd level in soil. The Cd concentrations of rice grains of the CK, T1 and T2 treatments were in the range of 0.143–0.202, 0.128–0.458 and 0.332–0.806 mg kg–1, respectively. Marked differences of the ratios of Cd concentration for soil to rice grain(BCFs) and transfer factors(TFs, root to grain and straw to grain) among the tested cultivars were observed in this study. The bioconcentration factors(BCFgrain) and TFs of the 20 rice cultivars were 0.300–1.112 and 0.342–0.817, respectively. The TFs of Cd from straw to grain ranged from 0.366 to 1.71, with significant differences among these 20 rice cultivars. The bioconcentration factors(BCFgrain) and TFs among the 20 rice cultivars ranged from 0.300–1.112 and 0.342–0.817, respectively. The species-sensitivity distribution(SSD) of Cd sensitivity of the rice species could be fitted well with Burr-III(R2=0.987) based on the data of BCFs. The toxicity threshold of Cd derived from SSD for the paddy soil was 0.507 mg kg–1 in the present study.SONG Wen-en CHEN Shi-bao LIU Ji-fang CHEN Li SONG Ning-ning LI Ning LIU Bin 2015Journal of Integrative Agriculture2015,14,9:33
4The pharmacology, toxicology and therapeutic potential of anthraquinone derivative emodin显示文摘Emodin(1, 3, 8-trihydroxy-6-methylanthraquinone) is a derived anthraquinone compound extracted from roots and barks of pharmaceutical plants, including Rheum palmatum, Aloe vera, Giant knotweed, Polygonum multiflorum and Polygonum cuspidatum. The review aims to provide a scientific summary of emodin in pharmacological activities and toxicity in order to identify the therapeutic potential for its use in human specific organs as a new medicine. Based on the fundamental properties, such as anticancer, anti-inflammatory, antioxidant, antibacterial, antivirs, anti-diabetes, immunosuppressive and osteogenesis promotion, emodin is expected to become an effective preventive and therapeutic drug of cancer, myocardial infarction, atherosclerosis, diabetes, acute pancreatitis, asthma, periodontitis, fatty livers and neurodegenerative diseases. This article intends to provide a novel insight for further development of emodin, hoping to reveal the potential of emodin and necessity of further studies in this field.CUI Ya CHEN Liu-Jing HUANG Tu YING Jian-Qiong LI Juan 2020Chinese Journal of Natural Medicines2020,18,6:23
5Toxicity of cadmium and its competition with mineral nutrients for uptake by plants:A review显示文摘Cadmium(Cd)is a toxic heavy metal occurring in the environment naturally and is also generated through various anthropogenic sources and acts as a pollutant.Human health is affected by Cd pollution in farmland soils because food is the main source of Cd intake in the non-smoking population.For crops,Cd toxicity may result from a disturbance in uptake and translocation of mineral nutrients and disturbance in plant metabolism,inhibiting plant growth and development.However,plants have Cd tolerance mechanisms,including restricted Cd uptake,decreased Cd root-to-shoot translocation,enhanced antioxidant enzyme activities,and increased production of phytochelatins.Furthermore,optimal supply of mineral nutrients is one of the strategies to alleviate the damaging effects of Cd on plants and to avoid its entry into the food chain.The emerging molecular knowledge contributes to understanding Cd uptake,translocation,and remobilization in plants.In this review,Cd toxicity and tolerance mechanisms,agricultural practices to minimize Cd accumulation,Cd competition with essential elements(calcium,copper,iron,zinc,and manganese),and genes associated with Cd uptake are discussed in detail,especially regarding how these mineral nutrients and genes play a role in decreasing Cd uptake and accumulation in crop plants.Shiyu QIN Hongen LIU Zhaojun NIE Zed RENGEL Wei GAO Chang LI Peng ZHAO 2020Pedosphere2020,30,2:20
6Safety Research in Traditional Chinese Medicine: Methods, Applications, and Outlook显示文摘Traditional Chinese medicine (TCM) is a medical system that has collected and summarized abundant clinical experience over its long history of more than 2000 years. However, the frequent occurrence of TCM-induced adverse reactions has hindered the modernization and internationalization of TCM, while attracting increasing attention from around the world. Unlike chemical drugs and biological agents, the difficulties involved in research on the toxicity and safety of TCM mainly include the complexity of its components and the unpredictability of drug–body interactions. Much of TCM, which has overall therapeutic effects, has the typical mechanisms of multiple components, multiple pathways, and multiple targets. While considering the gradualness and unpredictability of TCM toxicity, the ambiguity of toxicants and safe dosage, and individual differences during long-term TCM administration, we have systematically established key techniques for the toxicity assessment of TCM. These techniques mainly include TCM toxicity discovery in an early phase, based on a combination of drug toxicology genomics and metabolomics;methods to identify dose–toxicity relationships in TCM;and integrated techniques for the exploration of TCM interactions, such as fast-screening tests based on drug-metabolizing enzymes and receptor pathways. In particular, we have developed a new technical system for TCM safety evaluation using molecular toxicology, which has been validated well in research on TCM compatibility contraindication, quality control, and allergen discovery. The application of this key technical platform is introduced here in detail. This application includes model organisms, toxicant biomarkers, a magnetic suspension technique, and the application of network toxicology and computational toxicology in research on the toxicity of Fructus toosendan, Semen cassiae, Polygonum multiflorum, and Fructus psoraleae.Yue Gao Aihua Liang Xiaohui Fan Limin Hu Feiran Hao Yubo Li 2019Engineering2019,5,1:19
7Recent Advance in Studies on Angelica sinensis显示文摘Angelicae Sinensis Radix (ASR) is the root of Angelica sinensis which is a fragrant and perennial herb native to China, Japan, and Korea. In traditional Chinese medicine (TCM), the plant is useful for replenishing and invigorating blood, relieving pain, and moistening the intestines, resulting in its application for the treatment of menstrual disorders, and as an emollient and laxative for chronic constipation of the aged and debilitated. An in-depth review of the literature brings to light a great number of chemical constituents that have been isolated from ASR as well as both preclinical (in vivo and in vitro) and clinical studies, which over the years, have sought to investigate the medicinal relevance of some of these phytoconstituents and/or extract(s) prepared from ASR. The purpose of this review is therefore to present some major pharmacological and pharmacokinetic research findings on some selected phytoconstituents of ASR with emphasis on the current trends in terms of research techniques or design. This review would also provide a wealth of information for users/practitioners of TCM regarding the use of ASR or its products for maximum efficiency and minimal toxicity or side effects.Ling FANG Xue-feng XIAO Chang-xiao LIU Xin HE 2012Chinese Herbal Medicines2012,4,1:18
8Toxicities and risk assessment of heavy metals in sediments of Taihu Lake, China, based on sediment quality guidelines显示文摘The occurrence, toxicities, and ecological risks of five heavy metals(Pb, Cu, Cd, Zn and Ni) in the sediment of Taihu Lake were investigated in this study. To evaluate the toxicities caused by the heavy metals, the toxicities induced by organic contaminants and ammonia in the sediments were screened out with activated carbon and zeolite. The toxicities of heavy metals in sediments were tested with benthic invertebrates(tubificid and chironomid).The correlations between toxicity of sediment and the sediment quality guidelines(SQGs)derived previously were evaluated. There were significant correlations(p < 0.0001) between the observed toxicities and the total risk quotients of the heavy metals based on SQGs,indicating that threshold effect level(TEL) and probable effect level(PEL) were reliable to predict the toxicities of heavy metals in the sediments of Taihu Lake. By contrast, the method based on acid volatile sulfides(AVS) and simultaneously extracted metals(SEM),such as ∑SEM/AVS and ∑SEM-AVS, did not show correlations with the toxicities. Moreover,the predictive ability of SQGs was confirmed by a total predicting accuracy of 77%. Ecological risk assessment based on TELs and PELs showed that the contaminations of Pb, Cu, Cd and Zn in the sediments of Taihu Lake were at relatively low or medium levels. The risks caused by heavy metals in the sediments of northern bay of the lake, which received more wastewater discharge from upper stream, were higher than other area of the lake.Yanfeng Zhang Yuwei Han Jinxi Yang Lingyan Zhu Wenjue Zhong 2017Journal of Environmental Sciences2017,29,12:16
9Ferrostatin-1 protects HT-22 cells from oxidative toxicity显示文摘Ferroptosis is a type of programmed cell death dependent on iron.It is different from other forms of cell death such as apoptosis,classic necrosis and autophagy.Ferroptosis is involved in many neurodegenerative diseases.The role of ferroptosis in glutamate-induced neuronal toxicity is not fully understood.To test its toxicity,glutamate(1.25–20 mM)was applied to HT-22 cells for 12 to 48 hours.The optimal experimental conditions occurred at 12 hours after incubation with 5 mM glutamate.Cells were cultured with 3–12μM ferrostatin-1,an inhibitor of ferroptosis,for 12 hours before exposure to glutamate.The cell viability was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.Autophagy was determined by monodansylcadaverine staining and apoptosis by caspase 3 activity.Damage to cell structures was observed under light and by transmission electron microscopy.The release of lactate dehydrogenase was detected by the commercial kit.Reactive oxygen species were measured by flow cytometry.Glutathione peroxidase activity,superoxide dismutase activity and malondialdehyde level were detected by the appropriate commercial kit.Prostaglandin peroxidase synthase 2 and glutathione peroxidase 4 gene expression was detected by real-time quantitative polymerase chain reaction.Glutathione peroxidase 4 and nuclear factor erythroid-derived-like 2 protein expression was detected by western blot analysis.Results showed that ferrostatin-1 can significantly counter the effects of glutamate on HT-22 cells,improving the survival rate,reducing the release of lactate dehydrogenase and reducing the damage to mitochondrial ultrastructure.However,it did not affect the caspase-3 expression and monodansylcadaverine-positive staining in glutamate-injured HT-22 cells.Ferrostatin-1 reduced the levels of reactive oxygen species and malondialdehyde and enhanced superoxide dismutase activity.It decreased gene expression of prostaglandin peroxidase synthase 2 and increased gene expression of glutathione peroxidase 4 and protein expressions of glutathione peroxidase 4 and nuclear factor(erythroid-derived)-like 2 in glutamate-injured HT-22 cells.Treatment of cultured cells with the apoptosis inhibitor Z-Val-Ala-Asp(OMe)-fluoromethyl ketone(2–8μM),autophagy inhibitor 3-methyladenine(100–400μM)or necrosis inhibitor necrostatin-1(10–40μM)had no effect on glutamate induced cell damage.However,the iron chelator deferoxamine mesylate salt inhibited glutamate induced cell death.Thus,the results suggested that ferroptosis is caused by glutamate-induced toxicity and that ferrostatin-1 protects HT-22 cells from glutamate-induced oxidative toxicity by inhibiting the oxidative stress.Jun Chu Chen-Xu Liu Rui Song Qing-Lin Li 2020Neural Regeneration Research2020,15,3:16
10Severe irinotecan-induced toxicity in a patient with UGT1A1*28 and UGT1A1*6 polymorphisms显示文摘Many studies have demonstrated the impact of UGT1A1 on toxicity of irinotecan. In particular, patients bear-ing UGT1A1*28 (TA 7/7) have a higher risk of severe neutropenia and diarrhea. Based on this, prescribers of irinotecan are advised that patients with UGT1A1*28 (TA 7/7) should start with a reduced dose of irinotecan, although a particular dose is not specified. Research in Asian countries has shown a lower incidence of UG-T1A1*28 (TA 7/7), while UGT1A1*6 (A/A) is more often found and is associated with severe irinotecan-related neutropenia. We report here a case of a metastatic colorectal cancer patient who is heterozygous for the UGT1A1*28 polymorphism (TA 6/7) as well as the UG-T1A1*6 polymorphism (G/A). The patient was treated with FOLFIRI for 9 cycles and underwent two irinote-can dose reductions according to pharmacokinetic data regarding exposure to the active metabolite, SN-38. Simultaneous heterozygous UGT1A1*28 and UGT1A1*6 polymorphisms may produce higher exposure to SN-38 and a higher risk of adverse effects related to irinote-can. Additional studies will be necessary to determine the optimal starting dose of irinotecan for patients with both UGT1A1*28 and UGT1A1*6 polymorphisms.Jian-Ming Xu Yan Wang Fei-Jiao Ge Li Lin Ze-Yuan Liu Manish R Sharma 2013World Journal of Gastroenterology2013,19,24:14
11Understanding the biochar’s role in ameliorating soil acidity显示文摘Extensive acidic soils,which suffer from accelerated soil acidification,are found in southern China.Soil acidity,aluminum toxicity,and nutrient deficiencies severely limited crop productivity in acidic soils.It has been widely reported that crop residue biochars can ameliorate acidic soils and increase crop productivity.Here,we summarized the positive effects and mechanisms involved in the correction of soil acidity,the alleviation of aluminum toxicity and the increase of soil pH buffering capacity by crop residue biochars.The carbonate,oxygen-containing functional groups and silicates in biochars are the major components responsible for their efficacy in amending acidic soils and resisting soil re-acidification.We conclude that application of crop residue biochars may be a better option than traditional liming to ameliorate acidic soils.Nonetheless,further researches into soil acidification are still required to address some issues that are controversial and poorly understood.SHI Ren-yong LI Jiu-yu NI Ni XU Ren-kou 2019Journal of Integrative Agriculture2019,18,7:14
12Safety of menstrual blood-derived stromal cell transplantation in treatment of intrauterine adhesion显示文摘BACKGROUND Intrauterine adhesion(IUA)can cause serious damage to women’s reproductive health,yet current treatment methods are difficult to achieve satisfactory results.In our previous studies,we demonstrated that menstrual-derived stromal stem cells(MenSCs),with high proliferative capacity and self-renewal ability,have a powerful therapeutic effect in patients with severe IUA.However,safety assessment of MenSCs transplantation is essential for its further application.AIM To evaluate the short-,medium-,and long-term biosafety of MenSCs via intrauterine transplantation in a rat model of IUA,with a focus on toxicity and tumorigenicity.METHODS MenSCs were injected into the sub-serosal layer of the uterus in an IUA rat model,for 3 d,3 mo,and 6 mo separately,to monitor the corresponding acute,sub-chronic,and chronic effects.Healthy rats of the same age served as negative controls.Toxicity effects were evaluated by body weight,organ weight,histopathology,hematology,and biochemistry tests.Tumorigenicity of MenSCs was investigated in Balb/c-nu mice in vivo and by colony formation assays in vitro.RESULTS Compared with the same week-old control group,all of the IUA rats receiving MenSC transplantation demonstrated no obvious changes in body weight,mainorgan weight,or blood cell composition during the acute,sub-chronic,and chronic observation periods.At the same time,serum biochemical tests showed no adverse effects on metabolism or liver and kidney function.After 4 wk of subcutaneous injection of Men SCs in Balb/c-nu nude mice,no tumor formation or cell metastasis was observed.Moreover,there was no tumor colony formation of Men SCs during soft agar culture in vitro.CONCLUSION There is no acute,sub-chronic,or chronic poisoning,infection,tumorigenesis,or endometriosis in rats with IUA after Men SC transplantation.The above results suggest that intrauterine transplantation of Men SCs is safe for endometrial treatment.Qi-Yuan Chang Si-Wen Zhang Ping-Ping Li Zheng-Wei Yuan Ji-Chun Tan 2020World Journal of Stem Cells2020,12,5:14
13Visualizing the emerging trends of biochar research and applications in 2019:a scientometric analysis and review显示文摘Biochar,derived from thermal pyrolysis of biomass,has been regarded as a low-cost,sustainable and beneficial material and widely applied in agriculture,environment and energy during the last two decades.To elucidate the research status timely and future trends in biochar field,CiteSpace is used to systematically analyze the related literature retrieved from the Web of Science core collection in 2019.Based on the keywords clustering analysis,it was found that“biochar production”,“organic pollutants removal”,“heavy metals immobilization”,“bioremediation”were the main hotspots in research covering biochar.“Bioremediation”is an emerging topic and deserves extensive attention due to its highly effective and environmentally friendly treatment of pollutants.Improving the phytoremediation effect,immobilizing functional microorganisms on biochar,and using microorganisms as raw materials to produce biochar were the common methods of biochar-assisted bioremediation.While studies focused on“soil quality and plant growth”and“biochar and global climate change”decreased,investigations concentrated in the toxicity of biochar to soil biota and ruminants are sustainably growing.Research on direct and catalytic thermal pyrolysis of green waste(mainly microalgae)for biofuels(bio-oil,biodiesel,syngas,etc.)and biochar production is increasing.Converting municipal wastes(e.g.,sewage sludge,fallen leaves)into biochar through pyrolysis was a suitable treatment for municipal waste and became a popular topic in recent time.Moreover,the biochar produced from these municipal wastes exhibited excellent performance in the removal of pollutants from wastewater and soil.This review may help to identify future directions in biochar research and applications.Ping Wu Zeyu Wang Hailong Wang Nanthi S.Bolan Yujun Wang Wenfu Chen 2020Biochar2020,2,2:14
14Role of Microtubule-associated Protein Tau Phosphorylation in Alzheimer's Disease显示文摘As a major microtubule-associated protein, tau plays an important role in promoting microtubule assembly and stabilizing microtubules. In Alzheimer's disease(AD) and other tauopathies, the abnormally hyperphosphorylated tau proteins are aggregated into paired helical filaments and accumulated in the neurons with the form of neurofibrillary tangles. An imbalanced regulation in protein kinases and protein phosphatases is the direct cause of tau hyperphosphorylation. Among various kinases and phosphatases, glycogen synthase kinase-3β(GSK-3β) and protein phosphatase 2A(PP2A) are the most implicated. Accumulation of the hyperphosphorylated tau induces synaptic toxicity and cognitive impairments. Here, we review the upstream factors or pathways that can regulate GSK-3β or PP2A activity mainly based on our recent findings. We will also discuss the mechanisms that may underlie tau-induced synaptic toxicity.马荣红 张瑶 洪小月 张俊菲 王建枝 刘恭平 2017Journal of Huazhong University of Science and Technology(Medical Sciences)2017,37,3:14
15Study on the anticarcinogenic effect and acutetoxicity of liver-targeting mitoxantrone-nanoparticles显示文摘AIM To study the anticarcinogenic effect and acute toxicity of liver targeting mitoxantrone nanospheres. METHODS The anticarcinogenic effect of mitoxantrone polybutylcyanoacrylate nanoparticles (DHAQ PBCA NP) was investigated by using heterotopic and orthotopic transplantation models of human hepatocellular carcinoma (HCC) in nude mice and was compared with mitoxantrone (DHAQ) and doxorubicin (ADR). The acute toxicity of DHAQ PBCA NP lyophilized injection in mice was also studied. RESULTS The tumor inhibition rates of ADR, DHAQ, DHAQ PBCA NP to orthotopically transplanted HCC were 60 07%, 67 49% and 99 44%, respectively, but regard to heterotopically transplanted HCC, these were 80 03%, 86 18% and 92 90%, which were concordant with the results acquired by mitosis counting and proliferating cell nuclear antigen (PCNA). After iv administration to mice with DHAQ PBCA NP, the LD 50 was 16 9*!mg/*!kg ± 3 9*!mg/*!kg , no obvious local irritation was observed and there was no significant damage to the structure of liver cells, and that of the heart, spleen and kidneys. CONCLUSION The effect of DHAQ PBCA NP was significantly higher than that of DHAQ and ADR in the anti orthotopically transplanted HCC and the acute toxicity was relatively low.ZHANG Zhi Rong, HE Qin, LIAO Gong Tie and BAI Shao Huai 1999World Journal of Gastroenterology1999,5,6:13
16Adverse reactions of Amiodarone显示文摘Adverse drug reaction is defined by the World Health Organization as any response to a drug that is noxious and unintended and occurs at a dose normally used in man.Older people are at elevated risk of adverse drug reactions—because of changes in pharmacodynamics,concurrent use of multiple medications and the related drug interactions.However,adverse drug reactions are significantly underestimated in the elderly population that is also exposed to inappropriate drugs.Amiodarone is an antiarrhythmic drug used commonly for the treatment of atrial fibrillation and is increasingly prescribed in older people.While amiodarone is an efficient drug for rhythm control,it’s a carrier of different adverse reactions,and pro and cons must be carefully evaluated before its use especially in older people.Ruben ML Colunga Biancatelli Viviana Congedo Leonardo Calvosa Marco Ciacciarelli Alessandro Polidoro Luigi Iuliano 2019Journal of Geriatric Cardiology2019,16,7:11
17Structural Characterization and Acute Toxicity Simulation for Nitroaromatic Compounds显示文摘The three-dimensional holographic vector of atomic interaction field(3D-Ho VAIF) is used to characterize the molecular structures of 45 nitroaromatic compounds.Two quantitative structure-toxicity relationship(QSAR) models are built up by stepwise regression(SMR),multiple linear regression(MLR) and partial least-squares regression(PLS).The correlation coefficients(R) of the models are 0.960 and 0.961,respectively.Then the models are evaluated by performing the cross-validation with the leave-one-out(LOO) procedure and the correlation coefficients(RCV) are 0.949 and 0.941,respectively.The results show that the descriptors can successfully describe the structures of organic compounds.The stability and predictability of the model are satisfactory.廖立敏 黄茜 李建凤 2016Chinese Journal of Structural Chemistry2016,35,3:10
18Tagetes erecta Linn.and its mosquitocidal potency against Culex quinquefasciatus显示文摘Objective:To investigate mosquitocidal effects of ethanolic extract of(lowers of Tagetes erecta(T.erecta) and its chloroform and petroleum ether soluble fractions against the larvae of Culex quinquefasciatus(Cx.quinquefasciatus).Methods:The fresh flowers of T.erecta were extracted in cold with ethanol(5.0 L) and after concentration,the ethanol extract was fractionated with chloroform and petroleum ether to afford a brownish syrupy suspension of ethanol extract(50.0 g),petroleum ether soluble fraction(18.6 g) and chloroform soluble fraction(23.8 g).The larvicidal effect of ethanol extract and their solvent fractions were determined by the standard procedure of WHO against different instars of Cx.quinquefasciatus.Results:Among the tested samples the chloroform soluble fractions showed the highest toxicity and consequently,the lowest LC_(50) values(14.14 μ g/mL,17.06 μ g/mL.36.88 μ g/mL and 75.48 μ g/mL) for all the instars larvae of Cx.quinquefasciatus.The larvae showed comparative tolerance in the course of increasing age and time.Conclusions:It can be concluded that the flowers of T.erecta are very effective natural larvicide and could be useful against Cx.quinquefasciatus.Farjana Nikkon M Rowshanul Habib Zahangir Alam Saud M Rezaul Karim 2011Asian Pacific Journal of Tropical Biomedicine2011,1,3:10
19Stems and leaves of Aconitum carmichaelii Debx.as potential herbal resources for treating rheumatoid arthritis: Chemical analysis,toxicity and activity evaluation显示文摘According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloids in mother roots, fibrous roots, stems, and leaves of Aconitum carmichaelii Debx. were measured by HPLC-MS/MS. And multivariate analysis methods, such as clustering analysis and principal component analysis, were applied to analyze the difference among various parts. In addition, the acute toxicity, analgesia, and anti-inflammatory tests were carried out. The results suggested that the contents of alkaloids in mother roots and fibrous roots were approximate, but those of leaves and stems were different from mother roots and fibrous roots. The results of the acute toxicity testing demonstrated the toxicity of fibrous root was strongest, and mother roots were slightly less toxic than fibrous roots. The stems and leaves were far less toxic than mother and fibrous roots. In addition, the analgesia and inflammatory tests showed the effects of the various tissues had no difference each other. These results provided a basis for developing new complementary and alternative treatments for rheumatoid arthritis patients. Simultaneously, the approach may also turn wastes into treasure and promote the development of circular economy.HE Ya-Nan OU Shui-Ping XIONG Xi PAN Yuan PEI Jin XU Run-Chun GENG Fu-Neng HAN Li ZHANG Ding-Kun YANG Ming 2018Chinese Journal of Natural Medicines2018,16,9:10
20Drug metabolism in drug discovery and development显示文摘Drug metabolism as a discipline plays an important role in drug discovery and development and the effects of drug metabolism on pharmacokinetics(PK), pharmacodynamics(PD), and safety should be carefully considered. This communication provides an overview of common strategies in the area of drug metabolism for improving PK/PD and safety profiles of drug candidates; these include, but are not limited to, collaboration with medicinal chemists on structure–activity relationships(SAR) to overcome high clearance, using deuterium replacement to further optimize a lead, prodrug approaches to circumvent formulation and delivery difficulties, and addressing issues such as species differences in metabolism,drug–drug interactions(DDI) and formation of reactive metabolites.Zhoupeng Zhang Wei Tang 2018Acta Pharmaceutica Sinica B2018,8,5:9
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