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- 저자 : Sheng Yin (검색결과 80 건)
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Synthesis and Cytotoxicity of Novel 3-Amino-4-indolylmaleimide Derivatives
Sheng-Yin Zhao,Yan-Wu Yang,Hai-Quan Zhang,Yun Yue,Mei Fan 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.4
In an attempt to develop potent and selective antitumor agents, a series of novel 3-amino-4-indolylmaleimides were designed and synthesized. The reaction showed high regioselectivity. The structure of compound 7a was determined by an X-ray single crystal diffraction method. The cytotoxicities of the title compounds were evaluated against HeLa, SMMC 7721 and HL 60 cancer cell lines by a standard MTT assay in vitro. The pharmacological results showed that some of the title compounds displayed moderate or high cytotoxic activity against the tested cell lines. Compound 7d was the most promising compound against the tested cancer cell lines. Structure-activity relationships are discussed based on the experimental data obtained. A hydroxyethylamino group at the 3-position in the side chain of indolylmaleimide is associated with an increase in cytotoxicity.
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Starving Aphelinus asychis negatively affects host feeding and parasitism on Myzus persicae
Sheng-Yin Wang,Yi Feng,Ning-Ning Liang,Rui Tang,Yan-Hong Liu,Da Yu Zhang,Tong-Xian Liu 한국응용곤충학회 2018 Journal of Asia-Pacific Entomology Vol.21 No.2
Aphelinus asychis (Walker) is an effective biological control agent for many species of aphids found on various crops. To provide strategies for releasing these parasitoids into a crop ecosystem, the effects of a short-duration starvation experiment on A. asychis were measured under laboratory conditions using Myzus persicae (Sulzer) as the host on cabbage and chili pepper plants. The survival rate of starved A. asychis female adults decreased sharply as the starving time increased, and the longevity of the starved parasitoids also decreased significantly. The number of aphids killed by the parasitoids decreased gradually with the extended duration of starvation. In addition, the number of aphids on chili peppers and cabbages killed by starved A. asychis females over their lifespan was significantly lower than that in the control group. Our results indicated that a short period of starvation might not cause significantly negative effects on the parasitoids and may be beneficial for the control of M. persicae at low densities after 1 day; however, starvation for>1 day seriously affected the performance of A. asychis females over their entire lifespan. The parasitoids performed similarly when aphids were fed chili pepper or cabbage plants.
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Clerodane furanoditerpenoids from the stems of Tinospora sinensis
Jun-Sheng Zhang,De-Feng Xu,Yin-Yin Wang,Ren-Fen Ma,Hua Zhang 대한약학회 2022 Archives of Pharmacal Research Vol.45 No.5
One new clerodane-type furanoditerpenoidtinosinoid A ( 1 ) and nine new nor-clerodane analogs tinosinoids B–J ( 2 − 10 ) have been isolated from the stems ofTinospora sinensis . The structures of the new compoundswith absolute confi gurations have been elucidated by spectroscopicmeans, including MS, NMR and ECD techniques,as well as chemical correlation. Compound 1 is a rare sulfurcontainingclerodane diterpenoid incorporating a 2-mercaptoethanolunit via a thioether bond, while compounds 4 / 5and 9 represent two pairs of unusual equilibrium regioisomersthrough an interesting intramolecular transesterifi cation. Our bioassays established that 1 and 8 displayed moderateantiproliferative eff ects against two human tumor celllines, and 9 and 10 showed signifi cant α -glucosidase inhibitoryactivities. A kinetics study revealed that compound 10was a noncompetitive α -glucosidase inhibitor, and its possiblebinding mode to the enzyme was further probed bymolecular docking experiments.
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Li, Hong-Sheng,Chen, Jin-Hu,Zhang, Wei,Shang, Dong-Ping,Li, Bao-Sheng,Sun, Tao,Lin, Xiu-Tong,Yin, Yong Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.3
Objective: To evaluate the effect of intravenous contrast on dose calculation in radiation treatment planning for oesophageal cancer. Methods: A total of 22 intravein-contrasted patients with oesophageal cancer were included. The Hounsfield unit (HU) value of the enhanced blood stream in thoracic great vessels and heart was overridden with 45 HU to simulate the non-contrast CT image, and 145 HU, 245 HU, 345 HU, and 445 HU to model the different contrast-enhanced scenarios. 1000 HU and -1000 HU were used to evaluate two non-physiologic extreme scenarios. Variation in dose distribution of the different scenarios was calculated to quantify the effect of contrast enhancement. Results: In the contrast-enhanced scenarios, the mean variation in dose for planning target volume (PTV) was less than 1.0%, and those for the total lung and spinal cord were less than 0.5%. When the HU value of the blood stream exceeded 245 the average variation exceeded 1.0% for the heart V40. In the non-physiologic extreme scenarios, the dose variation of PTV was less than 1.0%, while the dose calculations of the organs at risk were greater than 2.0%. Conclusions: The use of contrast agent does not significantly influence dose calculation of PTV, lung and spinal cord. However, it does have influence on dose accuracy for heart.
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Li, Hong-Sheng,Kong, Ling-Ling,Zhang, Jian,Li, Bao-Sheng,Chen, Jin-Hu,Zhu, Jian,Liu, Tong-Hai,Yin, Yong Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.5
Objectives: The purpose of this study was to evaluate the geometric accuracy of thoracic anatomic landmarks as target surrogates of intrapulmonary tumors for manual rigid registration during image-guided radiotherapy (IGRT). Methods: Kilovolt cone-beam computed tomography (CBCT) images acquired during IGRT for 29 lung cancer patients with 33 tumors, including 16 central and 17 peripheral lesions, were analyzed. We selected the "vertebrae", "carina", and "large bronchi" as the candidate surrogates for central targets, and the "vertebrae", "carina", and "ribs" as the candidate surrogates for peripheral lesions. Three to six pairs of small identifiable markers were noted in the tumors for the planning CT and Day 1 CBCT. The accuracy of the candidate surrogates was evaluated by comparing the distances of the corresponding markers after manual rigid matching based on the "tumor" and a particular surrogate. Differences between the surrogates were assessed using 1-way analysis of variance and post hoc least-significant-difference tests. Results: For central targets, the residual errors increased in the following ascending order: "tumor", "bronchi", "carina", and "vertebrae"; there was a significant difference between "tumor" and "vertebrae" (p = 0.010). For peripheral diseases, the residual errors increased in the following ascending order: "tumor", "rib", "vertebrae", and "carina"; There was a significant difference between "tumor" and "carina" (p = 0.005). Conclusions: The "bronchi" and "carina" are the optimal surrogates for central lung targets, while "rib" and "vertebrae" are the optimal surrogates for peripheral lung targets for manual matching of online and planned tumors.
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Yinli Duan,Jing Ma,Jiao Liu,Liang-Sheng Qiang,Juanqin Xue 한국섬유공학회 2020 Fibers and polymers Vol.21 No.4
In this paper, a facile and efficient method was performed to prepare the thermo-responsive Poly(Nisopropylacrylamide)/TiO2 (TiO2/PNIPAM) with the dispersing of TiO2 nanoparticles into PNIPAM. The structures ofnanoparticles and the grafted polymer were confirmed by X-ray diffraction (XRD), Raman spectra, Fourier transforminfrared spectra (FT-IR) and Dynamic Light Scattering (DLS). The interactions between the two components were studied byX-ray photoelectron spectroscopy (XPS), and the morphology of TiO2/PNIPAM was observed by scanning electronmicroscopy (SEM). The results showed that TiO2 exhibited homogeneous dispersion, without sacrificing the properties ofTiO2. Furthermore, The composite was used to photocatalytic degradation of Methylene blue (MB). The highest MB removalefficiency is 86.3 %. The photocatalytic activities above or below the lower critical solution temperature (LCST) of PNIPAMwas also investigated. The experiment results show that the existence of PNIPAM contributed not only the thermo-responsiveabilities to TiO2, but also the enhanced photocatalytic activities to TiO2. In addition, the corresponding mechanism ofenhanced photocatalytic activity was proposed. The results manifest that the well-designed TiO2/PNIPAM is a promisingcandidate in wastewater treatment application.
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Yin Bin Chen,Yu Fang Wang,Wei Hou,Ying-Ping Wang,Sheng-Yuan Xiao,Yang Yang Fu,Jia Wang,Si Wen Zheng,Pei-He Zheng 고려인삼학회 2017 Journal of Ginseng Research Vol.41 No.2
Background: Both ginsenoside Re and B-complex vitamins are widely used as nutritional supplements. They are often taken together so as to fully utilize their antifatigue and refreshing effects, respectively. Whether actually a drugenutrient interaction exists between ginsenoside Re and B-complex vitamins is still unknown. The objective of this study was to simultaneously investigate the effect of B-complex vitamins on the antifatigue activity and bioavailability of ginsenoside Re after their oral administration. The study results will provide valuable theoretical guidance for the combined utilization of ginseng and B-complex vitamins. Methods: Ginsenoside Re with or without B-complex vitamins was orally administered to mice to evaluate its antifatigue effects and to rats to evaluate its bioavailability. The antifatigue activity was evaluated by the weight-loaded swimming test and biochemical parameters, including hepatic glycogen, plasma urea nitrogen, and blood lactic acid. The concentration of ginsenoside Re in plasma was determined by liquid chromatographyetandem mass spectrometry. Results: No antifatigue effect of ginsenoside Re was noted when ginsenoside Re in combination with Bcomplex vitamins was orally administered to mice. B-complex vitamins caused to a reduction in the bioavailability of ginsenoside Re with the area under the concentrationetime curve from zero to infinity markedly decreasing from 11,830.85 2,366.47 h$ng/mL to 890.55 372.94 h$ng/mL. Conclusion: The results suggested that there were pharmacokinetic and pharmacodynamic drugenutrient interactions between ginsenoside Re and B-complex vitamins. B-complex vitamins can significantly weaken the antifatigue effect and decrease the bioavailability of ginsenoside Re when simultaneously administered orally.
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Yin Yang,Qian Li,Qi-Hua He,Ji-Sheng Han,Li Su,You Wan 생화학분자생물학회 2018 Experimental and molecular medicine Vol.50 No.-
Activation of the cholecystokinin type B receptor (CCKBR) by cholecystokinin octapeptide (CCK-8) inhibits opioid analgesia. Chronic opiate treatment leads to an increase in the CCK-8 concentration and thus enhances the antagonism of CCK-8 against opioid analgesia; the underlying molecular mechanisms remain of great interest. In the present study, we validated the colocalization of the μ-opioid receptor (MOR) and CCKBR in pain signal transmissionrelated spinal cord dorsal horn and dorsal root ganglion neurons of rats. Co-immunoprecipitation (Co-IP) and fluorescence lifetime-imaging-microscopy-based fluorescence resonance energy transfer (FLIM-FRET) assays showed that MOR heteromerized with CCKBR directly in transfected HEK293 cells. Combined with MOR mutant construction, the third transmembrane domain of MOR (TM3MOR) was demonstrated to participate in heteromerization with CCKBR. Receptor ligand binding, ERK phosphorylation and cAMP assays showed that MOR heteromerization with CCKBR weakened the activity of MOR. A cell-penetrating interfering peptide consisting of TM3MOR and TAT (a transactivator of HIV-1) sequences from the N terminal to the C terminal disrupted the MOR–CCKBR interaction and restored the activity of MOR in transfected HEK293 cells. Furthermore, intrathecal application of the TM3MOR-TAT peptide alleviated CCK-8-injection-induced antagonism to morphine analgesia in rats. These results suggest a new molecular mechanism for CCK-8 antagonism to opioid analgesia in terms of G-protein-coupled receptor (GPCR) interaction through direct heteromerization. Our study may provide a potential strategy for pain management with opioid analgesics.
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