[Method for screening cysteinyl leukotriene receptor 2 antagonists and preliminary screening of compounds].

OBJECTIVE: To establish a method for screening cysteinyl leukotriene receptor 2 (CysLT(2)) antagonists and to preliminarily screen a series of synthetic compounds. METHODS: Rat glioma cell line (C6 cells) highly expressing CysLT(2) receptor was used. Intracellular calcium concentration was measured after stimulation with the agonist LTD(4),which was used to screen compounds with antagonist activity for CysLT(2) receptor. Bay u9773, a CysLT1/CysLT(2) receptor non-selective antagonist, and AP-100984, a CysLT(2) receptor antagonist, were used as control. RESULT: PT-PCR showed a higher expression of CysLT(2) receptor in C6 cells. LTD(4) at 1 mumol/L significantly increased intracellular calcium in C6 cells; the maximal effect was about 37.5% of ATP, a positive stimulus.LTD(4)-induced increase of intracellular calcium was blocked by CysLT(2) receptor antagonists, but not by CysLT(1) receptor antagonists. Among the synthetic compounds, D(XW-)1,2,13,23,29 and 30 inhibited LTD(4)-induced increase of intracellular calcium. CONCLUSION: LTD(4)-induced change in intracellular calcium in C6 cells can be used as a screening method for CysLT(2) receptor antagonists. The compounds, D(XW-)1,2,13,23,29 and 30, possess antagonist activity for CysLT(2) receptor.

[Study on extraction technology for extract and flavonoids in Chrysanthemum morifolium by orthogonal design].

OBJECTIVE: To ascertain extraction technology condition for extract and flavonoids from Chrysanthum morifoliwn. METHOD: The optimizing ultrasonic extraction condition on the basis of extractive yield and flavonoids were determined by orthogonal design. RESULT: The order of factors which affected the flavonoid extraction was extraction times > ethanol concentration > ultrasonic time > solvent quantity. CONCLUSION: The optimum ultrasonic extractions are A2B3C3D3. Compared with traditional extraction, ultraction method is timesaving, simple to operate, stable and need not be heated.

[Study on ultrasonic extraction techniques of flavonoids in Chrysanthemum morifolium].

OBJECTIVE: To optimize the ultrasonic extraction condition for flavonoids from Chrysanthemum morifolium. METHOD: The extraction rate of flavonoids optimized condition (ethanol concentration, ultrasonic time, solvent quantity and extraction times) was determined by orthogonal design. UV-Spectrophotometry was used for the determination. RESULT: The order of factors to affect the flavonoid extraction was ethanol concentration > extraction times > solvent quantity > ultrasonic time. CONCLUSION: The optimum ultrasonic extractions were: A2 B2 C3 D3. Compared with traditional extraction, ultraction method can save time, be easy to operate, improve extraction rates and need no heating.