The meso-2,6-dichlorophenyl boron-dipyrromethene(BODIPY) derivative 1 was synthesized and characterized by single-crystal X-ray diffraction analysis, 1 H NMR and Esi-HRMS. Compound 1 crystallizes in monoclinic, space ...The meso-2,6-dichlorophenyl boron-dipyrromethene(BODIPY) derivative 1 was synthesized and characterized by single-crystal X-ray diffraction analysis, 1 H NMR and Esi-HRMS. Compound 1 crystallizes in monoclinic, space group P21/n with a = 8.717(4), b = 20.938(9), c = 12.402(6) ?, β = 98.660(7)°, V = 2237.7(17) ?3, D3 c = 1.333 Mg/cm, F(000) = 936, μ = 0.319 –mm1, Z = 4, the final R = 0.0537 and wR = 0.1556 for 5064 observed reflections with I > 2ζ(I). Its photophysical properties were investigated by fluorescence and UV-Vis spectrum. 1 shows high fluorescence quantum yield in different solvents and poor solvent effect. In addition, compound 1 has high values of initial decomposition temperature(298 ℃). Moreover, cell imaging experiments showed 1 is promising for further bioimaging applications.展开更多
目的分析患者不同临床特征与晚期乳腺癌(advanced breast cancer,ABC)患者血浆黏度的相关性及血浆黏度对采用含紫杉类药物化疗方案疗效的影响。方法采用免疫组化S-P法和FISH相结合的分子生物技术法,检测ABC患者雌激素受体(ER)和孕激素受...目的分析患者不同临床特征与晚期乳腺癌(advanced breast cancer,ABC)患者血浆黏度的相关性及血浆黏度对采用含紫杉类药物化疗方案疗效的影响。方法采用免疫组化S-P法和FISH相结合的分子生物技术法,检测ABC患者雌激素受体(ER)和孕激素受体(PR)、人表皮生长因子受体-2(HER-2)、细胞核增殖抗原(Ki-67)、突变型p53、血管内皮生长因子受体(vascular endothelial growth factor receptor,VEGFR)等生物学指标的表达情况,采用毛细管黏度测量法检测ABC患者血浆黏度。分析ABC患者中不同临床特征和血浆黏度的相关性及影响因素。并通过配对设计队列对照组研究来分析含紫杉类化疗方案治疗在高血浆黏度ABC患者中的化疗疗效,进一步明确高血浆黏度与化疗疗效的相关性。结果全组90例患者,其中分子分型(t=5.257,P=0.013)、Ki-67表达(t=14.117,P=0.045)及CK5/6表达(t=43.178,P=0.015)均与血浆黏度高低存在相关性,具有统计学意义(P<0.05)。给予高血黏度研究组配对血浆黏度正常对照组,研究显示两组在近期疗效方面差异无统计学意义(P>0.05)。在不良反应方面,研究组中白细胞下降较对照组明显,且差异有统计学意义(χ~2=9.588,P=0.048)。但研究组中血小板下降较对照组明显减轻(χ~2=11.652,P=0.020)。结论ABC患者中不同的临床特征可能对患者血浆黏度高低产生一定的影响,尤其是分子分型、Ki-67表达、CK5/6表达影响明显。血浆黏度高低对于给予含紫杉类方案化疗患者的近期疗效无明显影响。高血浆黏度患者在该类方案化疗过程中白细胞下降较血浆黏度正常患者明显。展开更多
OBJECTIVE The Ginkgo Leaf Extract and Armillariella Mellea Powders Oral(Yinxingmihuan Koufu Rongye,YXMH),a representative drug for"Treating both Brain and Heart",showed considerable clinical effects in isch⁃...OBJECTIVE The Ginkgo Leaf Extract and Armillariella Mellea Powders Oral(Yinxingmihuan Koufu Rongye,YXMH),a representative drug for"Treating both Brain and Heart",showed considerable clinical effects in isch⁃emic cardiovascular and cerebral vascular diseases.Recently,it is reported that YXMH has the potential for treating myocardial and cerebral ischemia related mental disorders,such as post stroke depression(PSD)and chronic heart disease(CHD)associated anxiety disorder.However,its mechanism has not been clearly elucidated.Meanwhile,increasing evidence revealed that there are close functional links between depression and habenular nucleus.The present study investigates the underlying mechanism of YXMH on attenuating the inflammation of microglia in habenular nucleus through CX3CL1-CX3CR1 axis in in a rat model of PSD.METHODS Rats were randomly devided into sham group,model group,Ginaton group(18 mg·kg^-1),Armillariella Mellea group(600 mg·kg-1),Fluoxetine group(10 mg·kg^-1),YXMH high-dose group(618 mg·kg^-1)and YXMH low-dose group(309 mg·kg^-1).The PSD model was induced by transarterial microembolization combined with sleep deprivation(2-Chloro-D-phenylalanine,PCPA,IH,200 mg·kg^-1,for 3 times,before the behavior test)in SD male rats.Then rats were treated with corresponding medicaments through gavage once a day until 3 weeks later,followed by body mass measurement,neurological deficit score evaluation,gripping strength and thermal withdrawl latency measurement,as well as depression related behavioral indicators,the open field test(OFT)and sucrose preference test.The pathological morphological changes of habenular nucleus was observed by HE staining,the expression of IBA-1 was measured and analyzed by immunohistochemistry staining,and alterations of proteins and genes related to the CX3CL1-CX3CR1 axis were analyzed using Western blotting(CX3CL1,CX3CR1)and real-time polymerase chain reaction(PCR)(CX3CL1,CX3CR1).RESULTS Compared with the sham group,rats in the model group manifested as decreased body mass,deficient neurological behavior and gripping strength,reduced loco⁃motor activity and sugar water consumption,as well as elevated thermal withdrawl latency(P<0.05,P<0.01).Mean⁃while,the pathological morphology of the habenular nucleus on the ischemic hemisphere showed significant neuronal degeneration,microglial proliferation,inflammatory cells and glia cells infiltration,together with up-regualted expression of IBA-1,CX3CL1,CX3CR1 protein and CX3CL1,CX3CR1 mRNA.YXMH attenuated inflammation of microglia in habenular nucleus through improving pathological morphology,inhibiting IBA-1 activation,down-regulating the expres⁃sion of CX3CL1 and CX3CR1 proteins and genes,and thus improved the behavior performance of ischemic injury and depression.CONCLUSION YXMH ameliorates neurological deficit and depressive behavior in rat model of PSD induced by transarterial microembolization combined with sleep deprivation,and the mechanism is probably related to attenu⁃ating inflammation of microglia in habenular nucleus through CX3CL1-CX3CR1 axis.展开更多
基金Supported by the National Key R&D Program of China(2016YFD0600804)Natural Scientific Foundation of Jiangsu Province(No.BK20160922)+2 种基金National Natural Scientific Foundation of China(No.21606133)the open Fund of Jiangsu Key Lab of Biomass-based Green Fuels and Chemicals(JSBGFC12002)Postgraduate Research&Practice Innovation Program of Jiangsu Province(KYCX17_0848)
文摘The meso-2,6-dichlorophenyl boron-dipyrromethene(BODIPY) derivative 1 was synthesized and characterized by single-crystal X-ray diffraction analysis, 1 H NMR and Esi-HRMS. Compound 1 crystallizes in monoclinic, space group P21/n with a = 8.717(4), b = 20.938(9), c = 12.402(6) ?, β = 98.660(7)°, V = 2237.7(17) ?3, D3 c = 1.333 Mg/cm, F(000) = 936, μ = 0.319 –mm1, Z = 4, the final R = 0.0537 and wR = 0.1556 for 5064 observed reflections with I > 2ζ(I). Its photophysical properties were investigated by fluorescence and UV-Vis spectrum. 1 shows high fluorescence quantum yield in different solvents and poor solvent effect. In addition, compound 1 has high values of initial decomposition temperature(298 ℃). Moreover, cell imaging experiments showed 1 is promising for further bioimaging applications.
基金National Natural Science Foundation of China(8187304081403141)
文摘OBJECTIVE The Ginkgo Leaf Extract and Armillariella Mellea Powders Oral(Yinxingmihuan Koufu Rongye,YXMH),a representative drug for"Treating both Brain and Heart",showed considerable clinical effects in isch⁃emic cardiovascular and cerebral vascular diseases.Recently,it is reported that YXMH has the potential for treating myocardial and cerebral ischemia related mental disorders,such as post stroke depression(PSD)and chronic heart disease(CHD)associated anxiety disorder.However,its mechanism has not been clearly elucidated.Meanwhile,increasing evidence revealed that there are close functional links between depression and habenular nucleus.The present study investigates the underlying mechanism of YXMH on attenuating the inflammation of microglia in habenular nucleus through CX3CL1-CX3CR1 axis in in a rat model of PSD.METHODS Rats were randomly devided into sham group,model group,Ginaton group(18 mg·kg^-1),Armillariella Mellea group(600 mg·kg-1),Fluoxetine group(10 mg·kg^-1),YXMH high-dose group(618 mg·kg^-1)and YXMH low-dose group(309 mg·kg^-1).The PSD model was induced by transarterial microembolization combined with sleep deprivation(2-Chloro-D-phenylalanine,PCPA,IH,200 mg·kg^-1,for 3 times,before the behavior test)in SD male rats.Then rats were treated with corresponding medicaments through gavage once a day until 3 weeks later,followed by body mass measurement,neurological deficit score evaluation,gripping strength and thermal withdrawl latency measurement,as well as depression related behavioral indicators,the open field test(OFT)and sucrose preference test.The pathological morphological changes of habenular nucleus was observed by HE staining,the expression of IBA-1 was measured and analyzed by immunohistochemistry staining,and alterations of proteins and genes related to the CX3CL1-CX3CR1 axis were analyzed using Western blotting(CX3CL1,CX3CR1)and real-time polymerase chain reaction(PCR)(CX3CL1,CX3CR1).RESULTS Compared with the sham group,rats in the model group manifested as decreased body mass,deficient neurological behavior and gripping strength,reduced loco⁃motor activity and sugar water consumption,as well as elevated thermal withdrawl latency(P<0.05,P<0.01).Mean⁃while,the pathological morphology of the habenular nucleus on the ischemic hemisphere showed significant neuronal degeneration,microglial proliferation,inflammatory cells and glia cells infiltration,together with up-regualted expression of IBA-1,CX3CL1,CX3CR1 protein and CX3CL1,CX3CR1 mRNA.YXMH attenuated inflammation of microglia in habenular nucleus through improving pathological morphology,inhibiting IBA-1 activation,down-regulating the expres⁃sion of CX3CL1 and CX3CR1 proteins and genes,and thus improved the behavior performance of ischemic injury and depression.CONCLUSION YXMH ameliorates neurological deficit and depressive behavior in rat model of PSD induced by transarterial microembolization combined with sleep deprivation,and the mechanism is probably related to attenu⁃ating inflammation of microglia in habenular nucleus through CX3CL1-CX3CR1 axis.
