Three xanthones and a benzophenone from Garcinia mangostana.

Investigation of the constituents of Garcinia mangostana has led to the isolation of four new compounds: three minor xanthones, garcimangosone A (1), garcimangosone B (2), and garcimangosone C (3), and a benzophenone glucoside, garcimangosone D (4). The structures of these four compounds were established by spectral (NMR and MS) and chemical methods.

Novel antiplatelet constituents from formosan moraceous plants.

Sixteen constituents from Formosan Moraceous plants were tested for their antiplatelet activities in rabbit platelet suspension and human platelet-rich plasma. Cycloartocarpin A, cycloheterophyllin, broussochalcone A, kazinol A, broussoaurone A, and broussoflavonol F showed strong inhibition of arachidonic acid (AA)-induced platelet aggregation. Of the compounds tested, broussochalcone A exhibited the most potent inhibition of platelet aggregation induced by AA (IC50 = 6.8 microM). The antiplatelet effects of cycloheterophyllin, broussochalcone A, kazinol B, broussoaurone A, and broussoflavonol F are partially due to an inhibitory effect on cyclooxygenase.

Studies on the synthesis of some xanthonoid derivatives possessing antiplatelet effects.

2,3- and 3,4-Dihydroxyxanthone react with ethyl 2,3-dibromopropanoate to form the new, substituted 1,4-benzodioxanes 3 and 4, respectively. The regioisomers 3a and 3b; 4a and 4b were separated by column chromatography and characterized for evaluation of the antiplatelet effects in rabbit washed platelets and human platelet-rich plasma. The ethoxycarbonyl derivatives 3a (20 microM) and 3b (20 microM) strongly inhibited the aggregation of rabbit washed platelets induced by arachidonic acid and collagen. The compound 4b showed the most potent inhibition of rabbit washed-platelet aggregation induced by arachidonic acid (IC50 = 8.3 microM). Of the compounds tested in human platelet-rich plasma, compound 4b exhibited the most potent inhibition of primary and secondary aggregation induced by adrenaline (IC50 = 8.6 microM). We conclude that the antiplatelet effects of these four ethoxycarbonyl derivatives are mainly due to an inhibitory effect on thromboxane formation and interference in the adrenaline-receptor interaction.

[Clinical evaluation of a domestically prepared enzyme immunoassay kit for the detection of hepatitis B surface antigen].

National Institute of Preventive Medicine (NIPM) has succeeded in the development of an enzyme immunoassay (EIA) kit for detection of hepatitis B surface antigen. The sandwich principle was used for the test. Guinea pig anti-HBs IgG was used for coating microtiter plates and Horseradish peroxidase was conjugated with goat specific anti-HBs. Its stability is longer than 4 months. The lowest detectable dose is 0.7 ng/ml or better for subtype ad of HBsAg tested with Hepatitis Sensitivity Panel, Bureau of Drug and Food, Department of Health. The regression curve was determined by testing 66 samples with Auszyme II (EIA Kit. Abbott Lab.) and NIPM Kit, while Auszyme II used as a reference kit. The two EIA kits correlated well with a coefficient of determination (r2) of 0.86. Evaluation on 1,157 patients' and officers' serum samples in Tri-Service General Hospital showed that the positive rate was 24.7% (286/1,157) by RIA (Clinical Assays, Travenol Lab., USA) and that of NIPM EIA Kit was 24.4% (282/1,157). There was no statistical significance in terms of positive rate (p greater than 0.05). The positive rates of 534 blood donors are 22.1% (118/534) and 21.9% (117/534) respectively. Another evaluation on 974 serum samples in National Taiwan University Hospital showed that the positive rate was 27.2% (265/974) by Ausria II-125 (RIA. Abbott Lab.) and that of NIPM EIA Kit was 27.4% (267/974). The undetectable rate and false positive rate of NIPM EIA Kit were 0.41% (4/974) and 0.62% (6/974) respectively. In comparison with four other kind of commercial EIA Kits, the results of NIPM EIA Kit were satisfactory also. We have scaled up the reagent preparations for the kit, except the antibody coated microtiter plate preparation. At the end of March 1985 we will supply 850 EIA kits for the Development Center for Biotechnology for their hepatitis B vaccine production program.