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1.
Molecules ; 26(5)2021 Feb 24.
Artigo em Inglês | MEDLINE | ID: mdl-33668340

RESUMO

Sigma-1 (σ-1) receptor agonists are considered as potential treatment for stroke. TS-157 is an alkoxyisoxazole-based σ-1 receptor agonist previously discovered in our group. The present study describes TS-157 profile in a battery of tests for cerebral ischemia. Initial evaluation demonstrated the compound's safety profile and blood-brain barrier permeability, as well as its ability to induce neurite outgrowth in vitro. The neurite outgrowth was shown to be mediated via σ-1 receptor agonism and involves upregulation of ERK phosphorylation (pERK). In particular, TS-157 also significantly accelerated the recovery of motor function in rats with transient middle cerebral artery occlusion (tMCAO). Overall, the results herein support the notion that σ-1 receptor agonists are potential therapeutics for stroke and further animal efficacy studies are warranted.


Assuntos
MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Infarto da Artéria Cerebral Média/tratamento farmacológico , Atividade Motora/efeitos dos fármacos , Crescimento Neuronal/efeitos dos fármacos , Oxazóis/farmacologia , Receptores sigma/agonistas , Recuperação de Função Fisiológica/efeitos dos fármacos , Animais , Infarto da Artéria Cerebral Média/metabolismo , Masculino , Estrutura Molecular , Oxazóis/síntese química , Oxazóis/química , Fosforilação/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Receptor Sigma-1
2.
Zhen Ci Yan Jiu ; 42(1): 62-6, 2017 Feb 25.
Artigo em Chinês | MEDLINE | ID: mdl-29072000

RESUMO

OBJECTIVE: To observe the effect of acupuncture stimulation of different acupoints or acupoint groups on intestinal locomotor in slow transit constipation (STC) mice, so as to provide experimental evidence for demonstrating the synergic function of acupoint combination. METHODS: A total of 190 Kunming mice were randomized into 19 groups:normal control, model, uni-"Quchi" (LI 11), uni-"Shangjuxu" (ST 37), uni-"Tianshu"(ST 25), and uni-"Dachangshu"(BL 25) groups, for analyzing the effect of single acupoint; normal control, model, uni-ST 25+uni-BL 25, uni-LI 11+uni-ST 37, bi-ST 25, bi-BL 25, bi-LI 11, and bi-ST 37 groups, for comparing the effect between single acupoint and two acupoints combination; normal control, model, bi-ST 25+bi-BL 25, bi-LI 11+bi-ST 37, and uni-LI 11+uni-ST 37+uni-ST 25 +uni-BL 25 groups, for comparing the effect between four acupoints and two acupoints combinations (10 mice/group). The STC model was established by intragastric administration of compound diphenoxylate suspension (1 mg/100 g), once daily for 2 days. Manual acupuncture needle stimulation (200 twirling times/min for 1 min) was applied to the abovementioned unilateral or bilateral acupoints twice daily for 7 times. The first defecation time, the defecation grain number in 12 h and the intestinal propulsion rate were determined using activated carbon gavage. RESULTS: Compared with the normal group, the first defecation time was significantly increased in the STC model group (P<0.01), while the 12 h defecation grain number and the intestinal propulsion rate were considerably decreased in the model group (P<0.01). After manual acupuncture intervention, the first defecation time was notably shortened in the uni-LI 11, uni-ST 37, uni-ST 25, uni-BL 25, bi-ST 25, bi-BL 25, bi-LI 11, bi-ST 37, uni-ST 25+uni-BL 25, uni-LI 11+uni-ST 37, bi-ST 25+bi-BL 25, bi-LI 11+bi-ST 37 and the uni-ST 25+uni-BL 25+uni-LI 11+uni-ST 37 groups compared with the model group (P<0.05), while both the 12 h defecation grain number and intestinal propulsion rate were considerably increased in the abovementioned 13 acupuncture groups (P<0.05, P<0.01). The effects of uni-ST 25+uni-BL 25 and uni-LI 11+uni-ST 37 were significantly superior to those of bi-ST 25, bi-BL 25, bi-LI 11 and bi-ST 37 groups, and those of the uni-ST 25+uni-BL 25+uni-LI 11+uni-ST 37 group were markedly superior to those of bi-ST 25+bi-BL 25 and bi-LI 11+bi-ST 37 groups in shortening the first defecation time and in increasing the 12 h defecation grain number and intestinal propulsion rate (P<0.05). CONCLUSIONS: Acupuncture stimulation of LI 11, ST 37, ST 25 and BL 25 can improve constipation in STC mice, and the effect of two acupoints combination is significantly superior to that of the corresponding bilateral single acupoint, and that of the 4 unilateral single acupoint combination is obviously superior to that of two bilateral acupoints combination, suggesting a synergistic action of acupuncture stimulation.


Assuntos
Pontos de Acupuntura , Terapia por Acupuntura , Constipação Intestinal/fisiopatologia , Constipação Intestinal/terapia , Animais , Defecação , Feminino , Motilidade Gastrointestinal , Humanos , Masculino , Camundongos
3.
Nanoscale Res Lett ; 11(1): 453, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27726121

RESUMO

Fill factors (FFs) of ~0.87 have been obtained for crystalline Si (c-Si) solar cells based on Ag front contacts after rapid thermal annealing. The usual single PN junction model fails to explain the high FF result. A metal/oxide/semiconductor (MOS) junction at the emitter is found to be inversely connected to the PN one, and when its barrier height/e is close to the open-circuit voltage of the solar cell, very high FF is obtainable. In this work, although the open-circuit voltage (<580 mV) is not high here, the efficiency of c-Si solar cell still reaches the state-of-the-art value (>20 %) due to the high FF achieved.

4.
Zhen Ci Yan Jiu ; 38(2): 87-92, 2013 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-23819208

RESUMO

OBJECTIVE: To observe the effect of electroacupuncture (EA) on the expression of myocardial 1-phosphatidylinositol 3-kinase (PI 3 K), hypoxia-inducible factor-1alpha (HIF-1alpha) and vascular endothelial growth factor (VEGF) in rats with cerebral-cardiac syndrome (CCS), so as to reveal its mechanism underlying reducing ischemic myocardial injury. METHODS: Forty SD rats were randomly and equally divided into sham-operation, model, EA and non-acupoint (the lateral-superior side of the hip) groups (10 rats/group). CCS model was established by injection of collagenase (1 U/microL) and heparin (7 U/microL) into the right caudate nucleus. Following modeling, EA (1.5 mA, 2 Hz, 20 min) was applied to "Shuigou" (GV 26), "Fengfu" (GV 16), "Neiguan" (PC 6) and "Xinshu" (BL 15) acupoints, once daily for three consecutive days. The expression levels of PI 3 K,HIF-1alpha and VEGF in the myocardium were detected by immunohistochemistry. RESULTS: Compared with the sham-operation group, the expression levels of myocardial PI 3 K, HIF-1a and VEGF proteins were significantly increased in the model group (P<0.01). While in comparison with the model group, there were little increase in the non-acupoint group (P>0.05) and considerable increase in the expression levels of the 3 myocardial proteins in the EA group (P<0.05). CONCLUSION: EA intervention has a function in upregulating the expression of myocardial VEGF, HIF-1alpha and PI 3 K proteins in CCS rats, which maybe contribute to its protective effect on ischaemic myocardial injury.


Assuntos
Doenças Cerebelares/genética , Doenças Cerebelares/terapia , Eletroacupuntura , Cardiopatias/genética , Cardiopatias/terapia , Subunidade alfa do Fator 1 Induzível por Hipóxia/genética , Fosfatidilinositol 3-Quinase/genética , Fator A de Crescimento do Endotélio Vascular/genética , Pontos de Acupuntura , Animais , Doenças Cerebelares/metabolismo , Feminino , Cardiopatias/metabolismo , Humanos , Subunidade alfa do Fator 1 Induzível por Hipóxia/metabolismo , Masculino , Fosfatidilinositol 3-Quinase/metabolismo , Ratos , Ratos Sprague-Dawley , Fator A de Crescimento do Endotélio Vascular/metabolismo
5.
Zhen Ci Yan Jiu ; 38(1): 78-82, 2013 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-23650806

RESUMO

Exterior-interior relationship of meridians and zangfu organs is an important component of the theory of acupuncturology in Chinese medicine. According to the descriptions in classic works of Chinese medicine and findings of modern experimental researches, in the present paper, the authors analyzed the close association between the "Heart" and "Small Intestine", exterior-interior correlation between the Heart Meridian and Small Intestine Meridian, and between the "Heart" and body surface (acupoints), limbs, five sensory organs, etc. In addition, the authors also summarized the underlying mechanisms of the above-mentioned exterior-interior relationship of the "Heart" and put forward some proposals for the future researches.


Assuntos
Pontos de Acupuntura , Coração/fisiologia , Intestino Delgado/fisiologia , Meridianos , Terapia por Acupuntura , Experimentação Animal , Animais , Humanos
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