4.Design, synthesis and pharmacological investigation of isoindoline derivatives as 5-HT/NE double reuptake inhibitors.
Hui WEN ; Yuan SHI ; Jing-wen DONG ; Yan-shen GUO ; Jian-Jun ZANG ; Guang-zhong YANG
Acta Pharmaceutica Sinica 2015;50(9):1148-1155
A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents
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chemical synthesis
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chemistry
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Biological Transport
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Drug Design
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Isoindoles
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chemical synthesis
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chemistry
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Serotonin Uptake Inhibitors
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chemical synthesis
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chemistry
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Structure-Activity Relationship
5.Immunological activity of Streptomyces polysaccharide in normal and immunosuppressed mice.
Xiao-yun WEN ; Chao SHI ; Shu-guang WU
Journal of Southern Medical University 2008;28(7):1168-1171
OBJECTIVETo investigate the immunological activity of Streptomyces polysaccharide (SMP) on normal and immunosuppressed mice.
METHODSThe effect of SMP on the proliferating activity of normal mouse splenocytes was tested in the mixed lymphocyte culture, and the changes of peripheral blood T lymphocytes were evaluated with acid a-naphthyl acetate esterase (ANAE) method. The ratio of Lyt2+ and L3T4+ T cell subsets was measured by flow cytometry.
RESULTSSMP stimulated obvious proliferation of mixed lymphocytes, showed protective effects on T lymphocyte and increased the ratio of Lyt2+ and L3T4+ cell subsets to nearly normal level in immunosuppressed mice.
CONCLUSIONSSMP can regulate the immune function in mice.
Animals ; CD4-Positive T-Lymphocytes ; immunology ; Female ; Immunocompromised Host ; immunology ; Lymphocyte Culture Test, Mixed ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; Polysaccharides ; immunology ; Spleen ; cytology ; Streptomyces ; chemistry ; immunology ; T-Lymphocytes ; cytology ; immunology
6.Effect of Simvastatin on Severe Complications of Subarachnoid Heamorrhage
Shi-wen WU ; Wei-ya MA ; Hong BIAN ; Guang YANG ; Wenbin ZHANG
Chinese Journal of Rehabilitation Theory and Practice 2006;12(4):326-328
ObjectiveTo investigate the effect of simvastatin on severe complications and prognosis of subarachnoid heamorrhage (SAH).Methods98 cases with SAH were randomly divided into the treatment groups and control group (finally, there were 32 cases in treatment group, 48 cases in control group). Patients in treatment group were given simvastatin 20 mg/day, and those in control group were treated with routine therapy. The incidences of cerebral vasospasm, hydrocephalus, rebleeding and mortality between the two groups were compared.ResultsThe incidence of hydrocephalus of treatment group was 3.13%; that of control group was 18.7%, there was a significantly difference between two groups (P<0.05). There were no significant differences for incidences of cerebral vasospasm, rebleeding and mortality between two groups (P>0.05).ConclusionSimvastatin can reduce the occurrence of hydrocephalus after SAH.
7.Effect of Yiqi Yangyin Huoxue decoction on the salivary gland function of the patients with nasopharyngeal carcinoma after the radiotherapy
Wen-Guang SHI ; Hong-Sheng LIN ; Wei HOU ; Yong-Ming ZHOU ;
Cancer Research and Clinic 2006;0(09):-
Objective To observe the clinical effect of Yiqi Yangyin Huoxue decoction(the function of decoction is to tonify Qi,nourish Yin and enhance blood circulation)on salivary gland response attribute to radiotherapy.Methods This study,carried between January 2005 and December 2005,focused on the effect of Chinese herbs on salivary gland response attribute to radiotherapy.In the treatment group,30 cases took Chinese herbs during the duration of radiotherapy,while in the control group 30 cases were given routine therapy.Results Both groups had finished the radiotherapy,however,in the control group,there were 5 cas- es with a break for 1~2 weeks.For the comparison of the salivary gland change in acute stage,there was no variance(x~2=2.387,P=0.122);the latency for the salivary gland change in treatment group was longer than that in control group(x~2=13.106,P=0.000).For the comparison of Karnofsky after radiotherapy,the KS was superior in the treatment group than that in control group(x~2=12.685,P=0.013);For the comparison of objective effect after radiotherapy,the remission rate in treatment group was 90 %,and it was 86.7 % in control group(x~2=0.638,P=0.727).Conclusion The decoction can remit the salivary gland response caused by radiotherapy in clinic,prolong the latency for acute radioactive response;release the pain of the pa- tients,increase the achievement ratio for radiotherapy,and improve the patients'living condition.To combine with radiotherapy,Chinese herbs is a good supplemental therapy for nasopharyngeal carcinoma
8.Follow-up study on multifocal electroretinogram of acute and convalescence stage of Vogt-Koyanagi-Harada syndrome
Guang-wei, LUO ; Fu-tian, JIANG ; Feng, WEN ; Shi-zhou, HUANG ; Cai-jiao, LIU ; Tian-qin, GUAN ; Shi-xian, LONG
Chinese Journal of Experimental Ophthalmology 2011;29(8):718-723
Background Researches showed that multifocal electroretinogram (mfERG) is able to assess the retinal function in the eyes with acute Vogt-Koyanagi-Harada ( VKH ) syndrome. But the mfERG characteristics of convalescence stage of VKH are still below clear. Objective Present study was to compare and follow up the variation process of visual acuity and mfERG in acute and recovery stages of VKH syndrome. Methods This was a clinic-based retrospective study. Visual acuity, mfERG and fundus fluorescence angiography ( FFA ) were recorded from 35 eyes of 18 acute VKH cases. The period of follow-up in recovery stage lasted about 18 months with the repetitive recording results for 4 times. Results In this study, the visual acuity range in acute stage VKH was 0. 01 to 1.0, and 91.4% (32/35 eyes) was below 0.6. Compared with normal control group, the visual acuity was significantly decreased (P<0.01). The response densities (amplitudes) of N1 ,P1 waves of the first-order kernel were significantly lowed in all the 6 rings,and the implicit times of 1-4 rings of both waves were significantly prolonged in acute VKH eyes(P<0. 05). The abnormalities of retinal function showed a regional difference at the posterior pole retina with the dominant change in the first ring,showing a cutting off78% in the P1 amplitude. The abnormal degree of mfERG was more serious as the the increase of retinal eccentricity. In 2 months of convalescence after glucocorticosteroids therapy,the range of visual acuity were 0. 1-1.2 ,and the amplitudes of N1, P1 of 1-2 rings were greatly elevated in comparison with acute on-set (P<0. 05 ). However, there was still a remarkable difference in the amplitudes of from 1 through 6 rings,comparing with normal. The response density of P1 wave from whole recording region was only 44% of normal. Though the visual acuity was stable during the follow-up duration, a decreasing tendency in N1 and P1 amplitudes were seen. The implicit times of both wave shortened only in 1-3 rings in recovery stages of VKH (P<0.05). Conclusion VKH syndrome cause serious damage of posterior retinal function.Macular region is the site with greater retinal functional lesion and restore before and after medication. This hardly recovery of retinal function can last over one and half year,even satisfied visual acuity is stable after proper treatment.
9.Research on spectral reflectance characteristics for Glycyrrhizae Radix.
Hui LI ; Cai-Xiang XIE ; Xiao-Jin LI ; Mei-Jia WEN ; Guang-Lin JIA ; Ming-Hui SHI ; Bao-Lin GUO ; Xiao-Guang JIA
China Journal of Chinese Materia Medica 2014;39(3):427-432
In order to study the spectral reflectance differences of Glycyrrhizae Radix under different growth conditions and lay the foundation for quantitative monitoring of Glycyrrhizae Radix remote sensing images, spectra of Glycyrrhiza species under different growth period and different varieties and different regions were measured by a portable spectrometer. The results showed that the reflectivity of annual G. uralensis was obviously higher than that of the two years plant in the visible light band own to the contents of crown layer chlorophyll. The reflectivity of two years G. pallidiflora was higher than that of G. uralensis in the near infrared band own to the leaf area index and the content of leaf water. The red edge spectrum of annual plant fluctuated largely than that of two years plant due to vegetation coverage and leaf area index. G. pallidiflora grew well than G. uralensis. Under different regions of the Glycyrrhiza species, spectral data analysis showed that within a certain range, the average annual precipitation and average annual evaporation were the major factors to affect the differences of Glycyrrhiza species spectral data under different regions owe to the leaf water content, the higher leaf water content, the lower spectral reflectance. The principal component analysis and continuum-removed method of the spectral data under different regions found that, within a certain range, the average annual precipitation and average annual evaporation were the major factors caused by the differences of Glycyrrhiza species spectral data under the different regions, Glycyrrhiza species spectral similarity related to the spatial distance.
Geography
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Glycyrrhiza
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chemistry
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Principal Component Analysis
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Spectrum Analysis
10.Clinical value of iris fluorescein angiography in diagnosis of uveitis in Chinese with brown iris
Ying, CUI ; Guang-wei, LUO ; Chu-fang, XIE ; Feng, WEN ; Shi-zhou, HUANG ; Cai-jiao, LIU ; Tian-qin, GUAN
Chinese Journal of Experimental Ophthalmology 2012;30(7):625-628
Background The pathological change of the anterior uveitis is the disruption of blood-aqueous barrier.Slit lamp examination appears to be limited for the evaluation of inflammatory response,and fluorescine angiography is an objective approach.However,there are few relative studies up to now in China.Objective Aim of this study was to observe the characteristics and assess the clinical applications of iris fluorescein angiography (IFA)in Chinese uveitis with brown iris.Methods Forty eyes of 40 normal subjects and 21 eyes of 13 patients with the anterior uveitis were collected in this study.IFA,slit-lamp examination and iris photograph were performed on the subjects.All individuals were informed consented at the initiation of this study.Results In normal eyes,fluorescence in iris vessels was blocked by the melanin pigment,but peripupillary weak fluorescent leakage was seen in the normal eyes with the age of >60 years old.The multiple patterns of fluorescence leakage were found in the patients suffered from uveitis of various etiologies although the negative slit-lamp finding,including the leakage of fluorescein around the pupillary margin and radial iris vessels in the eyes with mild diseases,transmitted fluorescence of regular iris vessels in the eyes with diffuse and local iris atrophy,and vascular tufts of the pupillary margin with coiled interwind tight clusters of thin vessels at the early phase in the eyes with dilated capillaries,microvascular anomalies and new vessel formation.The hyperfluorescence remained throughout the IFA duration.Conclusions IFA findings in uveitis vary depending on the topography,type and severity of inflammation.IFA has a good clinical applying value because of its objective assessment ability of the degree of the blood-aqueous barrier breakdown and iris neovascularization breakdown.It can exhibit the unvisible lesion under the slit-lamp and monitor the efficacy of medical theraphy in patients with active or quiescent uveitis.