4.Research progress of anti-acute marrow leukemia drugs by targeting FLT3
Hui-ya JIA ; Bo YANG ; Xiao-meng ZHANG ; Jian-hong GONG ; Ya WU ; Yan-le ZHI
Acta Pharmaceutica Sinica 2023;58(3):605-615
Acute myeloid leukemia (AML) is a genetic heterogeneous disease in which primordial and juvenile myeloid cells proliferate or accumulate abnormally in bone marrow, peripheral blood and other tissues, resulting in damage to normal hematopoietic function. Studies have shown that about 30% of AML patients have FMS-like tyrosine kinase 3 (FLT3), FLT3 abnormal regulation is closely related to the occurrence and development of AML. At present, FLT3 has become an important target for developing small molecular targeted drugs. Currently, a variety of FLT3 inhibitors and FLT3 degraders have been developed targeting FLT3, and some compounds have exhibited good anti-AML activity. This article summarizes and sorts out the current mainstream drugs for AML therapeutic targeting FLT3, in order to provide a reference for the development and design of AML drugs.
5.Mornitoring of the enantiomers of (?) -trans tramadol andits active metabolite in the serum of postoperative patients afterdifferent intravenous doses of (?)-trans tramadol hydrochloride injection
Hui-Chen LIU ; Yan-Yan YANG ; Yan-Ning HOU ; Ya-Li WANG ;
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(02):-
Aim To investigate the relationship between the clinical actions and the serum concentrations of the enantiomers of (?)-trans tramadol and its active metabolite. Methods 20 postoperative patients were divided into two groups and given multiple intravenous doses of (?)-trans tramadol hydrochloride injection, 400 mg?d-1 (group A) or 300 mg?d-1 (group B). The blood samples were taken at 38 h after the initial dose. The concentrations of the enantiomers of (?)-trans tramadol and its active metabolite, (?)-trans O-demethyltramadal were determined with high performance capillary electrophoresis(HPCE). Results The concentrations of the enantiomers of (?)-trans tramadol, the frequency and serious level of adverse reactions were higher in group A than in group B. The concentrations of the enantiomers of (?)-trans O-demethyltramadal, the analgesic effect were similar between group A and group B. Conclusion There is much closer relation between the analgesic effect and the concentration of (+)-O-demethyltramadal. The frequency and serious level of adverse reactions may be attributed to the higher concentrations of the enantiomers of (?)-trans tramadol, which are caused by the saturated metabolism.
6.Role of HMGB 1 in the pathogenesis of adjuvant-induced arthritis in rats
Ya-Ou ZHOU ; Xiaoxia ZUO ; Hui LUO ; Yan-Hui GONG ; Xian-Zhong XIAO ;
Chinese Journal of Rheumatology 2003;0(11):-
Objective To demonstrate high mobility group box chromosomal protein 1(HMGBI) expression in synovium and joint,and to identify the role of HMGB1 in the pathogenesis of synovitis and joint destruction in adjuvant-induced arthritis(AA).Methods AA of 15 male rats were induced in SD rats by intradermal injection of 100?l Freud's complete adjuvant in the foot pad of the left hind paw.All rats were killed at the 18th day.Synovium and joints were collected for histopathology studies and determining the expression of HMGB1 by immunohistochemistry,and serum was collected for determining the expression of HMGB1 by western blotting analysis.Results Immunostaining of specimens from normal rats showed that HMGB1 was primarily confined to the nucleus of synoviocytes with occasional cytoplasmic staining.In contrast, inflammatory synovial tissues from AA rats showed a distinctly different HMGB1 staining pattern.Nuclear HMGBI expression was accompanied by a cytoplasmic staining in many mononuclear cells.The cytoplasmic HMGB1 expression in synovium of AA rats is significantly higher than that of normal rats.Additionally,HMGBI was highly expressed in the nuclei and cytoplasm of the subchondral chondrocytes and inflammatory cells in bone erosion in AA rats(P<0.01),while fewer positive cytoplasmic staining of HMGB1 was found in chondrocytes and fewer positive nuclear staining was found in bone cells in normal rats.HMGB1 concentration was significantly higher in serum of AA rats than that in normal rats(P<0.001).Conclusion The cytoplasmic HMGBI expression in synovium and joints is greatly upregulated;the level of HMGB1 in serum is increased in AA rats which suggests a patbogenetic role of HMGB1 in synovitis and bone destruction of adjuvant-induced arthritis.
7.Characteristics of 86 patients with newly diagnosed cases of pneumoconiosis.
Ru-yan YANG ; Ya-ping HUO ; Shi-jun ZHANG ; Ri-hui ZHOU
Chinese Journal of Industrial Hygiene and Occupational Diseases 2013;31(11):842-843
Adult
;
Aged
;
China
;
epidemiology
;
Female
;
Humans
;
Male
;
Middle Aged
;
Pneumoconiosis
;
diagnosis
;
epidemiology
8.Effects of erythropoietin on neural cells in rats after ischemia/reperfusion injury.
Yan-ling YANG ; Wen-xia ZHU ; Ya-hui CHEN ; Mei-ni CHEN
Chinese Journal of Applied Physiology 2010;26(2):152-153
Animals
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Brain Edema
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prevention & control
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Brain Ischemia
;
physiopathology
;
Erythropoietin
;
pharmacology
;
Female
;
Hippocampus
;
metabolism
;
pathology
;
Male
;
Nitric Oxide
;
metabolism
;
Protective Agents
;
pharmacology
;
Rats
;
Rats, Sprague-Dawley
;
Reperfusion Injury
;
prevention & control
;
Superoxide Dismutase
;
metabolism
9.Effects of the spinal cord intrathecal injected to agmatine on intrathecal morphine analgesia.
Zhong-Ping LAN ; Ya-Hui CHEN ; Nan GU ; Li-Ze XIONG ; Yan-Yuan SUN
Chinese Journal of Applied Physiology 2014;30(3):197-203
Agmatine
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administration & dosage
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pharmacology
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Analgesia
;
methods
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Animals
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Injections, Spinal
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Male
;
Morphine
;
pharmacology
;
Rats
;
Rats, Sprague-Dawley
;
Spinal Cord
;
drug effects