COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY A-MOLECULAR & INTEGRATIVE PHYSIOLOGY
·
2019
·
IF 2.142
Rong Xiong,Wei Zhao,Xi Chen,Tian Li,Haiyin Li,Yan Li,Wangshang Shen,Ping Chen
Serotonin is involved in the regulation of many physiological and behavioral processes in vertebrates and invertebrates. The effects of serotonin are mediated through interactions of several 5-HT receptor types. The expression and pharmacological properties of 5-HT1 have received more attention than other serotonin receptors, but its functions at the individual level are little studied in arthropods. Silkworm , a Lepidoptera model, almost has no reports about serotonin receptors. To analyze the function of Bm5-HT1A receptor in vitro , the ORF of Bm5-HT1A was cloned into the pcDNA3.1 vector and expressed in HEK 293 cells . Serotonin activation of Bm5-HT1A -expressing cells decreased forskolin-stimulated cAMP synthesis and had the most potent effect compared to other biogenic amines. Serotonin reduced cAMP synthesis in a dose-dependent manner, and half-maximal activation (EC50) occurred at a concentration of 1.17 × 10 −7 M (117 nM). The pharmacological analysis demonstrated that the rank potency of agonists was pimozide >8-OH-DPAT >5-MeOT ~ αm-5-HT, and antagonists was WAY-100635 > prazosin > SB-269970 > methiothepin at the Bm5-HT1A receptor. Injecting the antagonist of Bm5-HT1A receptor into larvae caused slow or weak motility, and adults lowered courtship vitality or moving speed. Injecting dsRNA of Bm5-HT1A into adults also dropped locomotivity in courtship. These results show that the Bm5-HT1A receptor is related to locomotor activity. This study provides the first information of serotonin receptor on pharmacological in silkworm and on individual functions in arthropods.
研究领域:
神经生物学
·
药理学
·
昆虫生理学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2021
·Vol. 22
·期 14
·7610
·
IF 5.924
Zhenyu Chen,Xiaoning Zhang,Jianwei Liang,Yansong Ji,Yuqing Zhou,Hao Fang
At present, silk fibroin (SF) hydrogel can be prepared by means of electrodeposition at 25 V in direct current (DC) mode. Reducing the applied voltage would provide benefits, including lower fabrication costs, less risk of high voltage shocks, and better stability of devices. Here, a simple but uncommon strategy for SF-based hydrogel preparation using 4 V in DC mode is discussed. SF was mixed and cross-linked with carboxymethyl chitosan (CMCS) through hydrogen bonding, then co-deposited on the graphite electrode. The thickness, mass, and shape of the SF/CMCS hydrogel were easily controlled by adjusting the electrodeposition parameters. Morphological characterization of the prepared hydrogel via SEM revealed a porous network within the fabricated hydrogel. This structure was due to intermolecular hydrogen bonding between SF and CMCS, according to the results of thermogravimetric analysis and rheological measurements. As a potential wound dressing, SF/CMCS hydrogel maintained a suitable moisture environment for wound healing and demonstrated distinct properties in terms of promoting the proliferation of HEK-293 cells and antibacterial activity againstEscherichia coliandStaphylococcus aureus. Furthermore, histological studies were conducted on a full-thickness skin wound in rats covered with the SF/CMCS hydrogel, with results indicating that this hydrogel can promote wound re-epithelization and enhance granulation tissue formation. These results illustrate the feasibility of using the developed strategy for SF-based hydrogel fabrication in practice for wound dressing.Keywords:silk fibroin;carboxymethyl chitosan;electrodeposition;wound dressing
研究领域:
材料科学
·
生物医学工程
·
伤口愈合
·
组织工程
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2016
·
IF 2.326
Qin Tang,Fangling Ji,Jianli Guo,Jingyun Wang,Yachen Li,Yongming Bao
Chrysin , one of natural flavonoid compounds, has recently been found to possess anti-inflammatory, antiallergic and anticancer properties. To increase its anticancer effects, 5 chrysin derivates were synthesized on the base of DNA intercalator structure. The inhibiting effects of chrysin and its derivatives on cancer cells Hela, BGC823, MCF-7, HepG2, and normal cells HEK-293, were evaluated by MTT assays . 5-(2′-amino) phenyl-7-cyclohexanemethylchrysin (Ch-1), a unique chrysin derivate, killed all the cancer cells but kept above 60% survival rate in normal cells HEK-293 at 62.5 μM. Treated with chrysin from 250 μM to 500 μM, those cells were still maintained above 60% survival rate. The result of circular dichroism spectra showed that Ch-1 could intercalate DNA while chrysin had no effects on DNA. Interestingly, Hela cells survival rates were 95% and 10%, after treated with 20 μM and 30 μM of Ch-1, respectively. Both intrinsic and extrinsic apoptotic pathway were identified in regulating the cell death caused by Ch-1 in Hela cells. p53, the upstream regulator of apoptotic pathway were extremely significantly up-regulated in Hela cells treated with 25 μM Ch-1. Moreover, the inhibiting effects and apoptotic related proteins responses to Ch-1 on Hela cells were abolished after pre-treated with Pifithrin-α (Pft-α), a p53 inhibitor. So, p53-depedent apoptosis is the crucial factor governing the inhibiting effects of Ch-1 in Hela cells. Amazingly, Ch-1 at non-toxic concentration (2.5–10 μM) enhanced significantly anti-cancer effect of 10-hydroxy camptothecin (HCPT) on Hela, BGC823, and MCF-7 cells.
研究领域:
癌症研究
·
药理学
·
细胞生物学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
·
2017
·
IF 4.187
Shuang-Shuang Wang,Rong-Hao Mu,Cheng-Fu Li,Shu-Qi Dong,Di Geng,Qing Liu,Li-Tao Yi
Dysregulation of microRNA (miRNA) has been shown to be involved in early observations of depression. MicroRNA-124-3p (miR-124) is the most abundant microRNA in the brain . Previous studies have shown that miR-124 plays a major role in depression. Here we showed that miR-124 directly targeted glucocorticoid receptor (GR) in HEK 293 cells . In addition, inhibition of miR-124 by its antagomir (2 nmol/every two days) could reverse the decrease of sucrose preference and the increase of immobility time in mice exposed to chronic corticosterone (CORT, 40 mg/kg) injection. Moreover, these effects on behavioral improvement were coupled to the activation of brain-derived neurotrophic factor (BDNF), TrkB, ERK, and CREB, as well as the induction of synaptogenesis and neuronal proliferation. Altogether, our study suggests that miR-124 can be served as a biomarker for depression and a novel target for drug development , and demonstrates that inhibition of miR-124 may be a strategy for treating depression by activating BDNF-TrkB signaling pathway in the hippocampus .
研究领域:
神经科学
·
分子生物学
·
药理学
✓ 已验证
DOI
PubMed
高影响因子
BRAIN BEHAVIOR AND IMMUNITY
·
2021
·
IF 7.217
Yun Wang,Ce Gao,Tianyu Gao,Lu Zhao,Shiguang Zhu,Lin Guo
A growing body of studies indicated that exosomes are one of vital players in pathological process of neuropsychiatric diseases, but their role in major depressive disorder (MDD) remains poorly understood. Here we purified plasma exosomes from depression including lipopolysaccharide (LPS)-challenged depression, chronic restraint stress (CRS)-induced depression, MDD subjects, and from control mice or volunteers. The therapeutic effect of these exogenous exosomes was assessed utilizing behavioral tests and biochemical approaches in the LPS-caused depression or microglial BV2 cells. The expression of exosomal sigma-1 receptor (Sig-1R) was evaluated by western blotting. The role of Sig-1R in the biological function of exosomes was determined using Sig-1R knockout mice and HEK 293 cells. Our results revealed that injection of exosomes from depression models or patients rather than normal controls significantly ameliorated depressive-like behaviors, deficiency of BDNF expression and neuro-inflammation in LPS-challenged mice. In addition, co-culture with exosomes from depression models or patients instead of from controls prevented LPS-induced inflammation responses in microglial BV2 cells. Moreover, Sig-1R was demonstrated for the first time to significantly be enriched in exosomes from depression models or patients compared with that from normal controls. However, Sig-1R null exosomes no longer emerged antidepressant-like action in LPS-challenged mice. Thus, we demonstrated that plasma exosomes from depression exerted antidepressant-like effects in a Sig-1R dependent manner in the LPS-induced depression. This work improves our understanding of the exosomes in depression, suggesting a novel exosomes-based approach for MDD treatment.
研究领域:
神经科学
·
药理学
·
分子生物学
·
精神病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2025
·
IF 3.1
Wu Xinhua,Wu Lifang,Li Zhaoquan,Tian Wei,Li Tao
Three series of (dimethyl-, dibutyl-, and diphenyl-) new organotin(IV) complexes based on chlorine substituted aryl ligands were synthesized and characterized by UV, 1 H NMR, 13 C NMR, 119 Sn NMR, HRMS, and X-ray crystallography analysis. MTT results showed that chlorine substitution at different positions on the aryl group exhibited different anticancer activities. Among them, 5-chloro substituents > 3,5-dichloro substituents > 3-chloro substituents on the aryl ring of salicylaldehyde on Schiff base ligand. In addition, different substituents on the tin atom also demonstrated extreme differences in anticancer activities, where dibutyltin > diphenyltin > dimethyltin. Interestingly, the complex LTDB2 exhibited excellent anti-proliferative activity against breast cancer MDA-MB-231 cells (superior to cisplatin) and lower toxicity against human embryonic kidney HEK-293 cells in vitro. Flow cytometry showed that LTDB2 not only induced apoptosis, but also induced cell cycle arrest in G2 phase. These findings provide new insights for further research and development of novel organotin(IV) complexes as anticancer drugs. Complex LTDB2 exhibited excellent anti-proliferative activity against breast cancer MDA-MB-231 cells in vitro and was superior to cisplatin. Flow cytometry showed that LTDB2 not only induced apoptosis, but also induced cell cycle arrest in G2 phase.
研究领域:
化学
·
药理学
·
肿瘤学
·
材料科学
✓ 已验证
DOI
高影响因子
危险品化学品经营许可证（带存储）