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Preparation of aripiprazole-poly(methyl vinyl ether-co-maleic anhydride)nanocomposites via supercritical antisolvent process for improved antidepression therapy

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Regenerative Biomaterials 2022年第1期9卷 917-927页

作者： Lin-Fei Chen Ying Chen You-Yu Duan Man-Man Zhang Pei-Yao Xu Ranjith Kumar Kankala Shi-Bin Wang Ai-Zheng Chen College of Chemical Engineering Huaqiao UniversityXiamen 361021PR China Institute of Biomaterials and Tisszue Engineering Huaqiao UniversityXiamen 361021PR China Fujian Provincial Key Laboratory of Biochemical Technology Huaqiao UniversityXiamen 361021PR China

Aripiprazole(ARI),a second-generation atypical antipsychotic drug approved for schizophrenia treatment,shows good efficacy against ***,the poorly aqueous solubility of ARI leads to low bioavailability and increased dose-related side effects,seriously limiting its application in ***,we demonstrated the fabrication of ARI and poly(methyl vinyl etherco-maleic anhydride)(PVMMA)composite nanoparticles(PA NPs)using the supercritical antisolvent(SAS)process for enhancing its water-solubility and curative anti-depressant ***,the optimal experimental conditions(ARI/PVMMA mass ratio of 1:6,pressure of 10MPa,and solution flow rate of 0.75ml min^(-1))were determined by a 23 factorial experimental design,resulting in the PA NPs with an excellent particle *** vitro cell experiments showed that PA NPs significantly inhibited the inflammatory response caused by the microglia activation induced by lipopolysaccharide(LPS).Similarly,mice behavioral tests demonstrated that PA NPs significantly improved LPS-induced depression-like ***,compared with free ARI,the LPS-induced activation of microglia in the mouse brain and the expression of inflammatory factors in serum were significantly reduced after treatment with PA ***,the innovative PA NPs designed by SAS processmight provide a candidate for developing new ARI-based nano-formulations.

关键词： aripiprazole supercritical fluid technology antidepression new nano-formulation

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Identification of antidepression constituents from Angelica Sinensis Radix contrubuting to Xiaoyaosan

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中国药理学通报 2015年第B11期31卷 120-121页

作者： GONGWen-xia ZHOUYu-zhi LIXiao QINGXue-mei ModernResarchVenterforTraditionalChineseMedicine ShanxiUniversityTaiyuan030006 CollegeofChemistryandChemicalEngineering ShanxiUniversityTaiyuan030006

Aim The study focused on identification and antidepression active verification of constituents from An- gelica Sinensis Radix contrubuting to Xiaoyaosan based on UPLC-PDA guided isolation technique. Methods The UPLC-PDA chromatogram of Xiaoyaosan was compared with that of Angelica Sinensis Radix. The relative retention time of each peak and the Uhraviolet spectra providing by PDA were used in the analyses. Constituents were isola- ted from Angelica Sinensis Radix under the guidance of UPLC-PDA investigation. Structures of the isolates were elu- cidated by NMR techniques. Anti-depression effect was evaluated on glutamate-induced neurons. Results Five marker peaks of Xiaoyaosan fingerprint were belong to Angelica Sinensis Radix, and they were determined as conife- ryl ferulate（ I）, E-butylidenephthalide （ II）, ligustilide （III）, Z-butylidenephthalide （ IV ）, 14-Acetoxy-12-sene- cioyloxytetradeca-2E,8E,10E-trien-4,6-diyn-l-ol（V）. Compound V was isolated from the plants of Umbelliferae for the first time. Treatment with compound I, III, IV can protect PC12 and SH-SY5Y cell from glutamate-induced cytotoxicity. antidepression bioactivity of compound I was first investigated. Conclusion UPLC-PDA guided iso-lation technique was confirmed to be a rapid and accurate method to identify the main active constituents from An- gelica Sinensis Radix contrubuting to Xiaoyaosan.

关键词： Xiaoyaosan Angelica Sinensis Radix guided isolation antidepression UPLC-PDA active constitu-ents

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Antidepressive Effects and Possible Therapeutic Basis of Xiaochaihutang

Antidepressive Effects and Possible Therapeutic Basis of Xia...

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第十四届全国中药和天然药物学术研讨会

作者： Kuo Zhang Fang Wang Yingxu Dong Lljuan Wang Huanhuan Pang Guangyue Su Jie Ma Zhili Xiong Jingyu Yang Chunfu Wu Shenyang Pharmaceutical University

Aim Xiaochaihutang（XCHT）,a famous Chinese herbal formula,has been used clinically in depressive *** previous study has demonstrated that XCHT has therapeutic actions on depressive-like behavior induced by chronic unpredictable mild stress in rats,which is mediated by increasing the monoamine neurotransmitter concentration and neurotrophin ***,the therapeutic basis of XCHT on treating depression is *** aim of present study is to provide deeper insights into therapeutic mechanisms of antidepressive effects of XCHT and its main *** The core in compatibility of XCHT on antidepressive effect was evaluated by using orthogonal array *** effects of XCHT and its core in compatibility were comparatively evaluated by tail suspension test（TST） and forced swim test（FST）.Levels of monoamine neurotransmitter were detected by HPLE-ECD and serum corticosterone was also measured by Elisa *** In orthogonal array design,taking immobility time as index,one-way ANOVA indicated that Radix Scutellariae,Ginseng and Radix glycyrrhizae,which were named HRG,might be the core in compatibility of *** administration of both XCHT and HRG for 15 days significantly reduced the immobility time in TST and *** addition,XCHT and HRG significantly increased levels of 5-HT,DA and DOPAC in hypothalamus and reduced the level of serum corticosterone in mice exposed to ***:HRG is the core in compatibility of XCHT on *** and HRG exert antidepressivet effects via regulating monoamine neurotransmitter and neuroendocrine HPA axis system.

关键词： Xiaochaihutang antidepression compatibility monoamine neurotransmitter HPA axis.

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Research progress on antidepressive active ingredients and mechanism of Xiaoyaosan

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中国药理学通报 2015年第B11期31卷 123-123页

作者： LIXiao GONGWen-xia ZHOUYu-zhi QINXue-mei ModernResearchCenterforTraditionalChineseMedicine ShanxiUniversityTaiyuan030006

The antidepressive effect of Xiaoyaosan is doubtless by researches while the potential antidepressive ac- tive ingredients and their mechanisms remain unclear. In order to explain the antidepressive effect of Xiaoyaosan, all of the recent reports were sought out on the current situation of the antidepressive monomer compositions of Xi- aoyaosan and their mechanism. By exploring the relationship between the effects and the active ingredients, the mechanism and the active ingredients, the antidepressive active ingredients such as quercetin, isorhamnetin, isoliquiritigenin, saikosaponinA, saikosaponinD, glycyrrhiz- kaempferol, liquiritin, isoliquiritin, liquiritigenin, inate, paeoniflorin, albiflorin, ferulic acid, curcumin and their mechanism of antidepressive such as regulating the monoamine neurotransmitter systems, regulating the neuroendocrine system, affecting the neural plasticity and neu- affecting the cytokines level, anti-oxidative stress were rotrophic, affecting the cellular and molecular mechanisms , summarized. By the overview in the level of monomer rather than formulae, we uncovered the antidepressive mech- anism of Xiaoyaosan and further confirmed that Xiaoyaosan, as a classic antidepressive Chinese prescription, had many characteristics, such as multi-level , multi-channel, multi-target and so on .

关键词： Xiaoyaosan monomer antidepression active ingredients mechanism research progress

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Antidepressant effects of SiniSan on LPS-induced depression in mice model and the regulation mechanism of SiniSan on Indoleamine2, 3-dioxygenase

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中国药理学通报 2015年第B11期31卷 66-66页

作者： CHANGHong-sehng LIHai-na ZHANGJing SchoolofChinesePharmacy BeijingUniversityofChineseMedicineBeijing100102

Aim To study the influence of SiniSan on the Tryptophan- kynurenine（TRP-KYN）pathway, the activity and content of the key metabolism enzyme indoleamine2, 3-dioxygenase （IDO）. Methods The mice model was established by intraperitoneal injection LPS （ 1 mg · kg^-1 ）. Using ELISA to detect the contents of IFN-γin serum. The content of Tryptophan and kynurenine in brain tissue were detected by using HPLC-MS/MS technique. The mRNA expression level of IDO in brain tissue was detected by using real-time PCR. Results 4 hours after the LPS injection, the immobility time of model group mice prolonged. The content of IFN-~/in serum increased significantly （P 〈 0.05）. Meanwhile, the activity of IDO in brain tissue and the mRNA expression level of IDO increased. SiniSan could short the immobility time of mice, reduced the content of IFN-γin serum （P 〈 0.05）. It could also inhibit the activity of IDO and the expression of mRNA（P 〈 0.01 ）. Conclusion SiniSan blocks the pathway of IDO activation, inhibit the activity of IDO and reduce the content of it. SiniSan produces antidepressant effect by adjusting the TRP-KYN metabolism.

关键词： SiniSan LPS mice antidepression IDO

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Pharmacological Effects and Molecular Mechanism of Synephrine Hydrochloride

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Asian Agricultural Research 2023年第4期15卷 34-36页

作者： Quan QUAN Jingchao WANG Mingxinzhi WANG Hai CHEN Anqi WANG Chenghao JIN College of Life Science and Biotechnology Heilongjiang Bayi Agricultural UniversityDaqing 163319China

Synephrine hydrochloride,an alkaloid compound extracted from immature bitter orange,has many pharmacological effects such as anticancer effect,antioxidant effect and antidepression *** this paper,the pharmacological effects and mechanism of synephrine hydrochloride were reviewed in order to provide a theoretical basis for the development and application of synephrine hydrochloride.

关键词： Synephrine hydrochloride Pharmacological effects Anticancer Antioxidation antidepression

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