Synthesis and Protective Effect of New Ligustrazine-Benzoic Acid Derivatives against CoCl2-Induced Neurotoxicity in Differentiated PC12 Cells

Wang, Penglong; Zhang, Honggui; Chu, Fuxiang; Xu, Xin; Lin, Jinxuan; Chen, Chunxiao; Li, Guoliang; Cheng, Yatao; Wang, Lin; Li, Qiang; Zhang, Yu-Zhong; Lei, Haimin

doi:10.3390/molecules181013027

Cited by 24 publications

(31 citation statements)

References 26 publications

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“…Apostoli et al hypothesized that Co may have a specific neurotropism; therefore, CoCl 2 may have a neurotoxic effect ( 32 ). In addition, chronic occupational exposure to Co has been shown to induce sensory-motor polyneuropathy in humans ( 33 ), while in animal models, Co has been shown to have neurotoxic effects in vitro and in vivo ( 34 ).…”

Section: Discussionmentioning

confidence: 99%

Preconditioning with cobalt chloride modifies pain perception in mice

Alexa

Luca

Dondas

et al. 2015

Experimental and Therapeutic Medicine

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Cobalt chloride (CoCl2) modifies mitochondrial permeability and has a hypoxic-mimetic effect; thus, the compound induces tolerance to ischemia and increases resistance to a number of injury types. The aim of the present study was to investigate the effects of CoCl2 hypoxic preconditioning for three weeks on thermonociception, somatic and visceral inflammatory pain, locomotor activity and coordination in mice. A significant pronociceptive effect was observed in the hot plate and tail flick tests after one and two weeks of CoCl2 administration, respectively (P<0.001). Thermal hyperalgesia (Plantar test) was present in the first week, but recovered by the end of the experiment. Contrary to the hyperalgesic effect on thermonociception, CoCl2 hypoxic preconditioning decreased the time spent grooming the affected area in the second phase of the formalin test on the orofacial and paw models. The first phase of formalin-induced pain and the writhing test were not affected by CoCl2 preconditioning. Thus, the present study demonstrated that CoCl2 preconditioning has a dual effect on pain, and these effects should be taken into account along with the better-known neuro-, cardio- and renoprotective effects of CoCl2.

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Section: Discussionmentioning

confidence: 99%

Preconditioning with cobalt chloride modifies pain perception in mice

Alexa

Luca

Dondas

et al. 2015

Experimental and Therapeutic Medicine

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“…与蛇胆-川贝等复方中药对拼合研究相似, 中药川芎经典药对有效成分拼合开发已有较广泛且深入的研究, 如雷海民课题组 [22] 以川芎嗪和丹参中的活性成分酚酸类物质为前体原料进行拼合的先导化合物开发研究. 相关研究发现, 部分川芎嗪拼合产物具有增效、低毒和产生多重药理活性的特点, 以川芎嗪-齐墩果酸酯 (T-OA)为代表的拼合产物还具有一定的肝癌选择性 [23] .…”

Section: 配伍法则· 拼合原理: 川芎经典药对unclassified

Discovering leading compounds of new drugs in traditional Chinesemedicine from classic formula via combination principle

Bi¹,

Chu²,

Yan³

et al. 2016

Sci. Sin.-Vitae

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“…To further improve the neuroprotective property of TMP, we decided to undertake a study of a novel series of TMP derivatives based on the principles of hybridization and prodrug design in medicinal chemistry and acquired compounds with pharmacologically additive or synergetic e ects [12][13][14]. It has been demonstrated that T-VA ((4-((3,5,6-trimethylpyrazine-2-yl)methoxyl)-3-methoxybenzoic acid-3,5,6-trimethylpyrazin-2-methyl ester; see Results, Figure 1A) has a promising protective effect against CoCl 2 -induced neurotoxicity in differentiated PC12 cells (EC 50 = 4.249 µM) [15] and that the plasma concentration of T-VA reaches peak levels between 4 and 6 h post-intragastric administration [16].…”

Section: Introductionmentioning

confidence: 99%