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Effect of rapamycin on the potential metastasis of squamous cell carcinoma in vitro

Chinese Pharmacological Bulletin.2014;(4):550-553,554. doi:10.3969/j.issn.1001-1978.2014.04.024

Aim To investigate the effect of rapamycin on proliferation, migration, and invasion of squamous cell carcinoma A431 cells in vitro. Methods Human squamous cell carcinoma A431 cells were cultured in vitro. MTT assay was used to investigate proliferation of A431 cells treated by rapamycin at different concentra-tions of (5,10,20 nmol·L-1). Wound healing and transwell assay were performed to detect migration and invasion of A431 cells treated by rapamycin, respec-tively. Reverse transcription PCR ( RT-PCR ) and Western blot were used to determine the expression of the osteopontin ( OPN ) in A431 cells at mRNA level and protein level, respectively. Results Rapamycin significantly increased the inhibitory rates of prolifera-tion and inhibited the migration and invasion of A431 cells in vitro. Furthermore, rapamycin treatment re-duced the expression of OPN in A431 cells. Conclu-sions Rapamycin can inhibit the migration and inva-sion of A431 . The intrinsic mechanism of rapamycin might be related to the down-regulation of the OPN ex-pression.

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The effects of superoxide anion on intracellular Ca2+ concentration and contractility in cultured bovine aortic smooth muscle cells

Wei CHENG ; Zhi LI ; Koyama TETSUYA ; Oike MASAHIRO ; Ito YUSHI

Chinese Pharmacological Bulletin.2001;17(2):190-193.

AIM　To study the effects of superoxide anion (O.2) on Ca2+ homeostasi and contractility in cultured bovine aortic smooth muscle cell. METHODS　Using Fura-2 fluorescence technique to determine Ca2+ level and collagen gel contraction system to analyze muscle contractility. RESULTS　ATP (10 μmol*L-1 )-induced Ca2+ transient was smaller in xanthine oxidase treated cells(X/XO) than control. The mean peak increment of ［Ca2+］i(△［Ca2+］i peak) and the time integral of the elevated ［Ca2+］i(∫△［Ca2+］i dt) for 5 min were decreased from (206.1±10.2) to (147.4±14.7) nmol·L-1,and from (12.2±0.5) to (9.8±0.8) μmol·L-1·s-1. Δ［Ca2+］i peak induced by thapsigargin（1 μmol·L-1 ）in Ca2+-free solution was not affected by X/XO, but was decreased from (27.3±1.0) nmol·L-1 to (13.5±1.0) nmol·L-1 in Ca2+-containing solution because of the activation of CRAC(△［Ca2+］i CRAC). X/XO accelerated the velocity of thapsigargin-induced Ca2+ leak from (78.7±3.4) s to (64.8±4.40) s. Gel contraction area in X/XO-treated cells induced by ATP or thapsigargin (in Ca2+ free solution and in Krebs solution)was decreased from 23.6%±4.6% to 7.4%±0.2%, from 3.5%±0.6% to -1.0%±0.5%, and from 7.9%±1.4% to -0.5%±0.7%, respectively. CONCLUTION　O.2 attenuats smooth muscle contraction by impairing some of Ca2+ mobilization pathways.

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Effect of erythromycin on interdigestive and postprandial gastrointestinal contractile activity and its mechanism in dogs

Chunmin YANG ; Xiurong ZHANG ; Gaoping MAO ; Yinhui ZHANG ; Chuanping CAO ; Xiaohua BU

Chinese Pharmacological Bulletin.2001;17(2):186-189.

AIM　To observe the effect of intravenous injection of erythromycin (EM) on interdigestive migrating motor complex (MMC) and postprandial gastrointestinal contraction in conscious dogs , and to study its possible mechanism. METHODS　Gastrointestinal contractile activity was recorded using low compliance capillary water perfusion manometric system. EM was administered intravenously during phaseⅠ and after meal, and blood samples were drawn for measuring plasma motilin concentrations. RESULTS　①Plasma motilin levels showed cyclical fluctuations in different phases of MMC, and plasma motilin reached peak during phaseⅢ and lowest during phaseⅠ.②EM induced phaseⅢ-like contractions in the antrum and duodenum, which was not accompanied by a peak in plasma motilin level. The optimum dose of EM for resulting in a premature phaseⅢ with the same characteristics as the spontaneously occurring phaseⅢ was established to be 0.5 mg*kg-1. The dose of 10 mg*kg-1 EM induced gastrointestinal continuous contractions and duodeno-gastric retrograde peristalsis which was associated with retching and vomiting. ③Atropine obviously inhibited EM-induced phaseⅢ activity in the antrum and duodenum. ④EM powerfully enhanced postprandial gastrointestinal contractile activity. CONCLUSIONS The results suggests that EM is a potent prokinetic agent. The mechanism is not related to the release of motilin, but may be mediated partially by cholinergic pathway.

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Preliminary study of insulin resistance induced by neonatal monosodium glutamate treatment in normal Wistar rats

Shiying DING ; Zhufang SHEN ; Mingzhi XIE

Chinese Pharmacological Bulletin.2001;17(2):181-185.

AIM　To study the glucose and lipids metabolis m and insulin sensitivity of MSG rats during their growing period, and to evalua te the effects of insulin sensitizer pioglitazone on the model rats. MET HODS　Body weights were measured regularly, and glucose and insulin tole rance tests were taken. In their 3 and 10 months old, rats were given insulin se nsitizer pioglitazone orally, then the effects on serum glucose, triglyceride, c holesteral, free fatty acid and insulin concentrations were determined. RESULTS　Compared with normal rats, a slight but significant increase of glucose in MSG rats was revealed. The serum triglyceride, cholesteral, free fat ty acid and insulin concentrations were significantly higher in model rats. More over, gluconeogenesis increased significantly, and insulin tolerance showed abno rmal. However, glucose tolerance was nearlly normal. Pioglitazone could ameliora te all these metabolic disorders. CONCLUSION　Obesity and insuli n resistance were induced by injecting monosodium glutamate (MSG) to neonatal Wi star rats. Pioglitazone can significantly improve the insulin sensitivity of MSG rats. These results suggested that MSG obese rats can be used as an easily acce ssible and inexpensive insulin resistance animal model for evaluating the effica cy and mechanisms of antidiabetic agents.

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The effect of OX-LDL and simvastatin on PKC activity and cytosolic free Ca 2+ in cultured human monocytes

Jinchuan YAN ; Zonggui WU ; Lingzhen ZHANG ; Li LI ; Jie FAN ; Ling LING ; Wenyu HAN ; Suolong ZHANG

Chinese Pharmacological Bulletin.2001;17(2):178-180.

AIM　To investigate the effect of OX-LDL and HMG- CoA reductase inhibitors simvastatin on PKC activity and cytosolic free Ca2+ in cultured human monocy tes. METHOD　The activity of PKC was determined by its ability to tr ansfer phosphate from ［32P］ATP to lysine-rich histone and cytosolic free calcium［Ca2+］i was measured by flow cytometric analysis loading with the Ca2+ dye fluo3/Am. RESULTS　OX-LDL increased PKC tot al activity in a dose-dependent manner with phase peaking at 12 min, then decre ased slowly and maintained for at least 20 min, while OX-LDL induced biphasic ［Ca2+］i responses including the rapid initial transient phase and the sustained phase. Removal of extracellular Ca2+ did not inhibit the rapid i nitial transient phase of OX-LDL-induced rise in ［Ca2+］i,but abolish ed the sustained phase of ［Ca2+］i response to OX-LDL. When simvastati n was added, the activity of PKC was markedly decreased and simvastatin did not impair the initial peak response to OX-LDL but significantly reduced the subseq uent plateau phase. CONCLUSION OX-LDL can significantly activate t he activity of PKC and elevate ［Ca2+］i in monocytes. The rapid initial transient phase was the result of mobilization of ［Ca2+］i from intrac ellular pool and sustained phase resulted from the influx of extracellular Ca 2+. The inhibition of PKC activity induced by simvastatin may be contribute to the changes of intracellular Ca2+.

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Characteristics of the delayed rectifier K+ current in guinea pig hypertrophied ventricular myocytes induced by thyroxine

Guangqin ZHANG ; Xuemei HAO ; Yuping MA ; Peiai ZHOU ; Caihong WU ; Dezai DAI

Chinese Pharmacological Bulletin.2001;17(2):174-177.

AIM　To study the characteristic of th e rapidly activating component (Ikr) and the slowly activating compone nt (Iks) of the delayed rectifier K+ current in guinea pig hypertrop hi ed ventricular myocytes induced by thyroxine. METHOD　The whole c ell patch clamp techniques were used. RESULTS　In hypertrophied ve ntricular myocytes, the magnitude of IKr and IKs were great ly augmented with more positive depolarizations, and the degree of increase of IKr tail and IKs were greater than that of IKr an d IKs tail, respectively. By measuring the amplitude of tail currents which reflected the degree of activation, the activation curve of IKs was shifted toward more negative potential, but that of IKr was marked ly unaffected in hypertrophied myocytes. CONCLUSION　Hypertrophied ventricular myocytes induced by thyroxine obviously increased IKr and IKs.

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Effect of Ganoderma polysacchride on intracellular free calcium and intracellular pH in murine T cells

Mingchun LI ; Linsheng LEI ; Qingbiao WANG ; Dongsheng LIANG ; Ziming XU ; Shuqin YANG ; Lisha SUN

Chinese Pharmacological Bulletin.2001;17(2):167-170.

AIM　To extend the approach of the act ion of ganoderma polysacchride on intracellular signal events in T cells. METHODS　Laser scanning confocal microscope imaging of the calcium and p H fluorescent indicator dye Fluo-3/AM and SNARF-1/AM were used to determine th e kinetic changes of ［Ca2+］i and ［pH］i in murine T cells induced b y a ganoderma polysacchride,designated GLB7. RESULTS　It was fou nd that GLB7(20 mg*L-1) could increase ［Ca2+］i and ［pH］i at 1 min were 334.7%±16.4%(n=3)、171.6%±10.4%(n=3) respectively. T he increase in ［Ca2+］i induced by GLB7 was due to the influx of extr acellular Ca2+ and intracellular Ca2+ release through both IP3-se nsitive and IP3-insensitive Ca2+ stores, and increase in ［pH］i indu ced by GLB7 was relative to Na+/H+ exchange systems and ［Ca2+］i. GLB 7 did not influence ［Ca2+］i and ［pH］i in murine T cells induced by Con A(3 mg*L-1). CONCLUSION　Stimulation of the increase in ［Ca2+］i and ［pH］i may be an important channel for gano derma polysacchrides to achieve their pharmacological actions.

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Effect of inulin-type hexasaccharide on forced swimming tests in mice and rats and DRL 72 s in rats

Zhongqi ZHANG ; Li YUAN ; Nan ZHAO ; Yukun XU ; Ming YANG ; Zhipu LUO

Chinese Pharmacological Bulletin.2001;17(2):164-167.

AIM　To determine whether O-β -D-fructofuranosyl-〔(2→1 )-O-β-D-fructofuransyl〕4α-D-glucopyranoside (inulin-type hexasaccharide, IHS), a monomer extracted from the roots of Morinda of ficinalis How, has antidepressant action. METHODS Fo rced swimming tests in mice and rats and differential-reinforcement-of-low-r ate 72 second schedule (DRL 72 s) in rats were used. RESULTS In the forced swimming test in mice, IHS (80 mg*kg-1, po), like the effe ct of clinically effective antidepressant desipramine (10 mg*kg-1, ip)， produced significant decrease in immobility time. IHS (20 mg*kg-1，po ) also elicited significant decrease in immobility time in forced swimming test in rats, which was comparable to the effect of desipramine (40 mg*kg-1, po). Moreover, in the DRL 72 s in rats, IHS (5～10 mg*kg-1, ip), s imilar to desipramine (5 mg*kg-1, ip), elicited significant increase in reinforcers. CONCLUSION These findings demonstrate that IHS has antidepressant action and is an effective component extracted from the root s of Morinda officinalis How.

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The relationship between sulfated polysaccharides and atheroscle rosis

Jinfeng HU ; Meiyu GENG ; Juntian ZHANG

Chinese Pharmacological Bulletin.2001;17(2):127-131.

The atherogensis was involved in a complex pathological process. Injury to endothelial cells of blood vessels was confirmed to be the in itial stage of this process. Migration to subendothelial layer and accumulation and proliferation of smooth muscle cells were attributed to various cytokines an d adhesive molecules secreted by activated endothelial cells, subsequently resul ting in aggregation of lymphocytes,platelets, monocytes and macrophages in the i ntima of artery. These cellular components ultimatedly led to the formation of a mature atherosclerotic plaque. Its quite acknowledged that a better understan ding of the atherogenic events might promise us the development of new chemical entities of anti-atherosclerotic therapies. A large body of evidence has demons trated that sulfated polysaccharides played a critical role in the development o f atherosclerosis. The underlying mechanisms of the anti-atherosclerotic activi ty of sulfated polysaccharides were reported to contribute to protecting against endothelial cells injury,inhibiting migration and proliferation of vascular smo oth muscle cells, and reducing the adhesion of inflammatory cells, platelets and lymphocytes. And also, the prevention of complement activation by sulfated poly saccharides could not be excluded. On the other hand,the promoting effects of su lfated polysaccharides atherosclerosis was also reported. Its therefore conclu ded that the relationships between atheriosclerosis and sulfated polysaccharides remained to be further elucidated.

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Tissue specificity in structure and function of ATP-sensitive potassium channel

Qinglei ZHU ; Hai WANG ; Wenbin XIAO

Chinese Pharmacological Bulletin.2001;17(2):121-127.

ATP-sensitive potassium channels (KATP channels) play important roles in various tissues under physiological and pathophysiological conditions by coupling cell metabolic status to electrical activity. The KATP channe l is a tetrameric complex of inwardly rectified potassium (Kir) and ATP binding protein (ABP). The Kir subunits form the channel pore, whereas ABP is required for activation and regulation. Both Kir and ABP are divided into different subu nits and the various Kir and ABP subunits “mix and match” to form KATP c hannels with different pharmacological and nucleotide sensitivities. This revie w focuses on the molecular structure, physiological roles, pathophysiological an d pharmacological properties of KATP channels in different tissues.

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