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Objective To study the potential antidepressive-like effect of tetramethylpyrazine (TMP). Methods Forced-swimming and chronic mild stress (CMS) tests were performed to assess the antidepressant-like activity of TMP. Male Sprague-Dawley (SD) strain rats were divided into six matched groups (n= 13 or 14 in each group) based on their sucrose consumption:control, CMS, CMS + fluoxetine, and CMS + TMP groups. The rats except control were housed separately in different rooms, and the rat model of depression was established by exposing to an unpredictable sequence of stressors for 28 days; the rats in CMS + fluoxetine were exposed to CMS and received administration of FLU (2.0 mg· kg-1·d-1 ,ig) for 28 days; the rats in CMS + TMP groups were exposed to CMS and received administration of TMP (10,20,40 mg·kg-1·d-1 ,ig) , respectively, for 28 days. The rats in control group were given ordinary daily care and received ig administration of normal saline simultaneously. The body weight, food intake and fluid consumption were measured, and the behaviors were examined by open field during the duration of the stress procedure, and forced-swimming test was performed 1 day after last unpredictable stressor. Results Acute administration of TMP markedly decreased the duration of immobility during forced-swimming test((89.0 ±37.0)s vs (117.1 ±32. 1)s, P<0.05) . Chronic administration of TMP partially countered the effects of CMS on consumption of sucrose solution and locomotion and exploration behavior, and potently shortened the immobility time during forced-swimming test following CMS in rats. The results showed that long-term administration of TMP partially reversed the effects of CMS on the body weight gain,the consumption of sucrose solution,the squares crossing in open field test and the immobility time during forced-swimming test in rats ((91.9 ±31.5) vs (124.4±27.0)s,P<0.05).Conclusion TMP shows obvious antidepressant-like activity.
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OBJECTIVE: To explore the general pattern and characteristics of adverse drug reactions (ADRs) induced by Tetramethylpyrazine(TMP) so as to provide references for clinical rational drug use. METHODS: A statistical analysis was conducted on 30 TMP-induced ADR cases reported in domestic medical journals. RESULTS: ADRs of TMP were independent of patient's sex, and which were more often seen in patients aged above 50. The ADRs could occur at any time after medication and involve multiple organs and systems. The clinical manifestations were various and manifested as allergic reaction or even allergic shock in severe cases. CONCLUSION: Doctors and pharmacists should master the pattern and characteristics of ADRs induced by TMP, and strengthen monitoring on the use of TMP to reduce the incidence of ADRs induced by TMP.
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Aim To study the effect of tetramethylpyrazine(TMP) on binding of 125I-VEGF to VEGF receptor. Methods The mice sera were collected after peritoneal injection with big-dose TMP,low-dose TMP,protamine and NS. A reversed-phase high performance liquid chromatography(RP-HPLC) method was used to determine the TMP in mice serum. The culture medium of ECV304 was treated with the mice sera in different groups. Radioligand binding assay(RBA) of receptor and Scatchard pot were performed to observe the changes of the maximum binding capacity(B_ max) and dissociation constant(K_d).Results The sera of big-dose TMP inhibited 125I-VEGF binding to its receptor, K_d=343.30?36.64 pmol?L-1,B_ max=46.26?5.85 fmol/2?10~5 cells(P0.05),but B_ max decreased(P
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Objective To observe the effect of tetraethylplyrazine(TMP) on outward K~+ channel of outer hair cells in guinea pig cochlea.Methods 60 guinea pigs were divided into 6 groups randomly in the experiment.Auditory brainstem response was used to monitor the change of ABR thresholds and patch clamp techniques to observe the effect of TMP on outward K~+ channel.Results TMP decreased the elevated ABR threshold caused by streptomycin. The TMP increased the amplitudes of calcium sensitive potassium channels (I_ K(Ca) ) and delayed outward potassium channels (IK) of outer hair cells of guinea pig cochlea.Conclusion The study indicates that TMP may act as a protective agent against ototoxicity of streptomycin. The amplitudes of I_ K(Ca) and IK of outer hair cells are increased by the TMP,suggesting the possible mechanisms of reducing ototoxicity.
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Objective To observe the effects of rat tetramethylpyrazine (TMP)-containing serum on the proliferation of human liver cancer cells Hep G2. Methods Thirty SD male rats were divided into three groups randomly and the serum was collected after ip TMP with the dosage of 143.0, 71.5 mg/kg or NS 0.8 mL to prepare the TMP-containing serum in large- and small-dose groups and NS group as well. A reversed-phase high performance liquid chromatography (RP-HPLC) method was used to determine the TMP concentration in rat serum. Human liver cancer cells Hep G2 was treated with rat TMP-containing serum for 48 h. Inhibition of the TMP-containing serum on proliferation of Hep G2 was detected by MTT assay. Results The serum of large dose TMP (20%, 10%, and 5%) and small dose TMP (20% and 10%) could obviously inhibit Hep G2 multiplication (P
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Objective To observe the effects of tetramethylpyrazine (TMP) on acute nociception in rat hindpaw induced by purine 2X (P2X) receptor agonists, such as adenosine triphosphate (ATP) and ?, ?-meATP, prostaglandin E 2 (PGE 2), and substance P (SP). Methods The effects of TMP administered intraplantarlly on the acute nociception induced by P2X receptor agonists, PGE 2, or SP in the rat hindpaw were investigated by the method of the behavioral study. Results TMP (10 mmol/L) significantly depressed the acute nociception induced by ATP (1 ?mol/L) or ?, ?-meATP (0.6 ?mol/L) in the rat hindpaw. TMP (10 mmol/L) could inhibit the acute nociception induced by PGE 2 (5 ?mol/L) or ?, ?-meATP (0.2 ?mol/L) coinjected with PGE 2 (5 ?mol/L). TMP (10 mmol/L) could not affect the acute nociception induced by ?, ?-meATP (0.2 ?mol/L) coinjected with SP (10 ?mol/L). TMP could not obviously affect the inflammatory edema in rat hindpaw induced by the local administration of PGE 2, SP, or ?, ?-meATP coinjected with PGE 2 or SP individually. Conclusion The antinociceptive effects of TMP may mainly be associated with inhibiting the transmission of nociceptive information mediated by P2X receptor activation.
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Object To investigate the effects of tetramethylpyrazine (TMP) and Danshen (DS) on the growth and metastasis of Lewis lung carcinoma and tumor angiogenesis. Methods C 57BL mice with Lewis lung carcinoma were used in this study, which were injected respectively with TMP injection 50, 100, and 200 mg/(kg?d) and DS injection 5, 10, and 20 g/(kg?d), ip, for 21 days. Then the volume, weight, and numbers of the metastatic foci on lungs, tumor microvessel density (MVD) were determined, the expression of vascular endothelial growth factor (VEGF) of Lewis lung carcinoma was observed. Results TMP could remarkably reduce the volume, weight, and numbers of the metastatic foci, MVD, and the expression of VEGF of Lewis lung carcinoma. But DS did not show remarkably effect on Lewis lung carcinoma. Conclusion TMP can remarkably inhibit the growth and metastasis of Lewis lung carcinoma on mice, and its mechanism might be relative to inhibiting the expression of VEGF and angiogenesis. DS injection has no remarkably effect on Lewis lung carcinoma.