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821.
Fang Liu Lihong Ye Wei Wei Gaoyi Yang Yang Ye Jun Meng Xueyan Din Songjia Zhao 《Saudi Journal of Biological Sciences》2019,26(3):589-594
Objective
To determine the effect of laser needle-knife on PI-3K, AKT and VEGF mRNA expression of vertebral arteries in a rabbit model of cervical spondylotic arteriopathy (CSA) and the mechanism of action involved.Methods
Forty healthy general-grade rabbits were divided into a normal control group, model group, acupuncture group, and laser needle-knife group (n?=?10 rabbits per group), and the CSA rabbit model was established in all but groups but the normal control group. CSA model rabbits in the acupuncture group were treated by acupuncture at the Fengchi (GB 20) and Cervical Jiaji (EX-B 2) points, whereas rabbits in the laser needle-knife group were treated with laser needle-knife targeting the Jiaji points near the C5 spinous process. Rabbits in the normal control and model groups were fixed using similar methods. Behavioral characteristics of all rabbits were evaluated before and after treatment. Peak systolic velocity (PSV) of the right carotid and vertebral arteries in each group were examined using beside B ultrasound, and PI-3K, AKT, VEGF mRNA expression in vertebral arteries were determined by real-time PCR.Results
The behavioral signs of rabbits were improved after treatment in both the acupuncture and laser needle-knife groups. In comparison with control group, PSV of right carotid arteries in acupuncture group and laser needle-knife group were enhanced significantly (P?<?0.05 and P?<?0.01), PSV of right vertebral arteries in acupuncture group and laser needle-knife group were enhanced significantly too (P?<?0.01 and P?<?0.05). PI-3K mRNA expression in laser needle-knife and acupuncture group was significantly higher than that in control group (P?<?0.01, P?<?0.05). AKT mRNA expression in laser needle-knife and acupuncture group was significantly higher than that in control group (P?<?0.01). VEGF mRNA expression in laser needle-knife and acupuncture group was significantly higher than that in control group too (P?<?0.01, P?<?0.05). No significant differences were found in PI-3K, AKT and VEGF mRNA expression levels among acupuncture and laser needle-knife groups (P?>?0.05).Conclusion
Laser needle-knife could effectively intervene the mRNA expression of PI-3K, AKT and VEGF, this may be one of the mechanisms of the effect of laser needle-knife in treating CSA in rabbits. 相似文献822.
Birong Zhang James R. Kiefer Robert A. Blake Jae H. Chang Steven Hartman Ellen Rei Ingalla Tracy Kleinheinz Vidhi Mody Michelle Nannini Daniel F. Ortwine Yingqing Ran Amy Sambrone Deepak Sampath Maia Vinogradova Yu Zhong Jerome C. Nwachukwu Kendall W. Nettles Tommy Lai Jun Liang 《Bioorganic & medicinal chemistry letters》2019,29(7):905-911
Despite tremendous progress made in the understanding of the ERα signaling pathway and the approval of many therapeutic agents, ER+?breast cancer continues to be a leading cause of cancer death in women. We set out to discover compounds with a dual mechanism of action in which they not only compete with estradiol for binding with ERα, but also can induce the degradation of the ERα protein itself. We were attracted to the constrained chromenes containing a tetracyclic benzopyranobenzoxepine scaffold, which were reported as potent selective estrogen receptor modulators (SERMs). Incorporation of a fluoromethyl azetidine side chain yielded highly potent and efficacious selective estrogen receptor degraders (SERDs), such as 16aa and surprisingly, also its enantiomeric pair 16ab. Co-crystal structures of the enantiomeric pair 16aa and 16ab in complex with ERα revealed default (mimics the A-D rings of endogenous ligand estradiol) and core-flipped binding modes, rationalizing the equivalent potency observed for these enantiomers in the ERα degradation and MCF-7 anti-proliferation assays. 相似文献
823.
Yi‐zhou Tan Dong‐dong Fei Xiao‐ning He Ji‐min Dai Rong‐chen Xu Xin‐yue Xu Jun‐jie Wu Bei Li 《Cell proliferation》2019,52(4)
L‐type voltage‐gated calcium ion channels (L‐VGCCs) have been demonstrated to be the mediator of several significant intracellular activities in excitable cells, such as neurons, chromaffin cells and myocytes. Recently, an increasing number of studies have investigated the function of L‐VGCCs in non‐excitable cells, particularly stem cells. However, there appear to be no systematic reviews of the relationship between L‐VGCCs and stem cells, and filling this gap is prescient considering the contribution of L‐VGCCs to the proliferation and differentiation of several types of stem cells. This review will discuss the possible involvement of L‐VGCCs in stem cells, mainly focusing on osteogenesis mediated by mesenchymal stem cells (MSCs) from different tissues and neurogenesis mediated by neural stem/progenitor cells (NSCs). Additionally, advanced applications that use these channels as the target for tissue engineering, which may offer the hope of tissue regeneration in the future, will also be explored. 相似文献
824.
Zhenbo Guo Yiming Xu Yujie Peng Wei Quan Peng Xie Lichuan Wu Jun Jiang Lisheng Wang Xu Liu 《Bioorganic & medicinal chemistry letters》2019,29(9):1133-1137
A series of (S)-tryptamine derivatives containing an allyl group and an aryl sulfonamide unit were designed, synthesized and evaluated for their potential application as anticancer agents. The structures of the synthesized compounds were characterized by 1H NMR, 13C NMR and ESI-MS spectral analyses. The target compounds were evaluated for their in vitro cytotoxicity against HepG2, HeLa, CNE1 and A549 human cancer cell lines. Some of the synthesized compounds showed moderate to good anticancer activities against four selected cancer cell lines, among of which 6ag was found to be the most active analogue possessing IC50 values 16.5–18.7?μM. Further mechanism studies revealed that compound 6ag could significantly induce HepG2 cell cycle arrest at G1 phase, promote cell apoptosis, and inhibit the colony formation as well. 相似文献
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