The Research On Dehydroabietylamine And Its Derivatives About Anti-Gastric Ulcer And The First Step Study On Its Function Mechanism

OBJECTIVE Observe DHAA-Fe²⁺, DHAA-K⁺ to influence that various animals experiment ulcerate, combine the first step inquiries into its function mechanism.METHODS Mice, Rats in tubal ligation in adoption; The small rat peritoneum injects to eliminate inflammation the painful method; Restraining the water immerses the small rat method; Have no the water ether stomach method; Big rat gland stomach a variety for ex-wall syrup descending injecting acetic acid aqua method resulting in every kind of experiment stomach ulcer model, measurement stomach liquid measuring, red cell counting, widespread bleeding ordering, ulcerating area, stomach acid value and stomach egg white activity etc. index signs; Joins the DHAA-Fe²⁺, DHAA-K⁺ two kinds of medicine after culturing a spiral rod bacteria（Hp）, measurese their suppress the germ a diameter.RESULTS DHAA-Fe²⁺ 0.1、0.2g/kg with DHAA-K⁺ 0.1, 0.2g/kg can show the reduces the small rat a tubal ligation type ulcerates the red cell counts to bleed to order with the widespread, DHAA-Fe²⁺ 0.4g/kg, DHAA-K⁺ 0.4g/kg can show the reduces the small rat a tubal ligation type the ulcer the widespread bleeds to order, can reduce obviously the red cell in small rat count; DHAA-Fe²⁺ 0.2, 0.4g/kg with DHAA-K⁺0.2, 0.4g/kg can reduce obviously the small rat eliminates inflammation the painful type ulcerates the area, DHAA-Fe²⁺ 0.1g/kg, DHAA-K⁺ the 0.1g/kg can show the reduces the small rat eliminates inflammation the painful type ulcerates the area; DHAA-Fe²⁺ 0.2g/kg can reduce obviouslythe small rat water immerse and should arouse the type ulcerates the area, DHAA-Fe²⁺0.1g/kg can show the reduces the small rat water immerse and should arouse the type ulcerates the area, but DHAA-K⁺ each one has no this phenomenon. DHAA-Fe²⁺ 0.1、0.2、0.4g/kg with DHAA-K⁺ 0.1、0.2、0.4g/kg all can show the reduces the small rat has no the water ether type ulcerates the area; DHAA-Fe²⁺ 0.2g/kg, DHAA-K⁺ 0.2g/kg all can show the reduces the big rat a tubal ligation type ulcerates the area, DHAA-Fe²⁺ 0.05、0.1g/kg, DHAA-K⁺ 0.05, 0.1g/kg all can reduce obviously the big rat a tubal ligation type ulcerates the area, DHAA-K⁺ 0.2g/kg can reduce obviously with a ratio the big rat a tubal ligation type ulcerates the area. DHAA-Fe²⁺ 0.1, 0.2g/kg can show the lowers the big rat a tubal ligation type ulcerates the stomach acid value, DHAA-K⁺ 0.2g/kg can show the lowers the big rat a tubal ligation type ulcerates the stomach egg white activity, DHAA-K⁺ 0.2g/kg can lower obviously the big rat a tubal ligation type ulcerates the stomach acid the value, with male set ratio DHAA-K⁺ 0.1g/kg can lower obviously the big rat a tubal ligation type ulcerates the area.DHAA-Fe²⁺ 0.2g/kg, DHAA-K⁺ 0.2g/kg can show the reduces the big rat ulcerates the area; DHAA-Fe²⁺ 0.1g/kg, DHAA-K⁺ 0.1g/kg all can reduce obviously the big rat acetic acid type ulcerates the area. DHAA-Fe²⁺ have to the Hp to suppress the germ function certainly, but DHAA-K⁺ suppresses the germ function to the Hp weaker. Conclusion DHAA-Fe²⁺, DHAA-K⁺ can resist the occurrence of various types stomach ulcer. OBJECTIVE To proof the Withdrawing LHT to Ca²⁺ passage represses the function.METHODS After educating PC12 cells and the aorta vascular smooth muscle cells （VSMCs）. make use of Wallac 1420 Victor multilabel measurement Ca²⁺ density inside the cell.RESULTS The present study investigated the effects of Chinese Herb component LHT on high K⁺ and glutamate （10mmol/L）-induced increase in cytosolic free Ca²⁺ in attached PC12 cells; the effects of LHT on caffeine and cyclopiozonic acid （CPA） induced calcium release from internal stores in attached PC12 cells; the effects of LHT on high K⁺ and norepinephrine（NE, 1μmol/L）-induced increase in cytosolic free Ca²⁺ in attached vascular smooth muscle cells （VSMCs）. Attached cells were loaded with the novel calcium fluorescent indicator Fluo-3/AM with the final concentration of 5μmol/L for 50min at 37°C. The cytosolic free Ca²⁺ was expressed as fluorescent intensity （FI） and measured with a Wallac 1420 Victor² multilabel counter （excitation: 488 nm; emission: 535 nm. Perkin-Elmer Life Sciences）. When PC12 cells were exposed to extracellular Ca²⁺( [Ca²⁺]_o ) 2.0mmol/L, the FI for resting [Ca²⁺]i was 1188±163, high K⁺ （75mmol/L） and glutamate （10mmol/L） induced an increase in [Ca²⁺]i to 4270±982 and 3096±402, respectively. LHT（0.1-100μmol/L） had no effect on resting [Ca²⁺]_i, but inhibited high K⁺ and glutamate induced the increase in [Ca²⁺]_i in dose-dependent manner with the inhibiting rate of 39.5% and 79.2% for 1μmol/L LHT, respectively. When PC12 cells were exposed to Ca²⁺-free solution, the FI for resting [Ca²⁺]_i was 804±77, caffeine （40mmol/L） and CPA （30μmol/L） stimulated Ca²⁺ release from caffeine-ryanodine and IP3-sensitive internal calcium stores, inducing an increase in [Ca²⁺]_i to 2938±362 and 1816±291, respectively. LHT（0.1-100μmol/L） inhibited caffeine and CPA stimulated intracellular calcium release in dose-dependent manner with more potent inhibition for caffeine stimulation. The FI of VSMCs for resting [Ca²⁺]_i was 1253±262 in the presence of extracellular Ca²⁺, high K⁺ （75mmol/L） and NE （1μmol/L） stimulated voltage-gated and receptor-dependent calcium channel, inducing an increase in [Ca²⁺]_i to 5110±752 and 5298±933, respectively. LHT（0.1-100μmol/L） inhibited high K⁺ and NE induced the increase in [Ca²⁺]_i in dose-dependent manner with the inhibiting rate of 47.4% and 61.1% for LHT（1μmol/L）, respectively. CONCLUTION In summary, the novel component LHT isolated from Chinese Herb not only inhibited Ca²⁺ influx induced by stimulation of voltage-gated and receptor-dependent calcium channel but also Ca²⁺ release from internal stores, This indicated that LHT is a promising leading compound in the development of a novel class of calcium antagonists.