In this study, the activities of four ginsenosides Rc, Re, Rd, and Rf on splenic lymphocytes growth were studied by microcalorimetry. Some qualitative and quantitative information, such as the metabolic power–time curves, growth rate constant k, maximum heat-output power of the exponential phase Pmax and the corresponding appearance peak time tmax, total heat output Qt, and promotion rate Rp of splenic lymphocytes growth affected by the four ginsenosides were calculated. In accordance with thermo-kinetic model, the corresponding quantitative relationships of k, Pmax, tmax, Qt, Rp, and c were established. Also, the median effective concentration (EC50) was obtained by quantitative analysis. Based on both the quantitative quantity–activity relationships (QQAR) and EC50, the sequence of promotion activity was Rc > Re > Rd > Rf. The analysis of structure–activity relationships showed that the number, type, and position of sugar moieties on the gonane steroid nucleus had important influences on the promotion activity of Rc, Re, Rd, and Rf on splenic lymphocytes growth. Microcalorimetry can be used as a useful tool for determining the activity and studying the quantity–activity relationship of drugs on cell.
1. Lee, FC Facts about ginseng, the elixir of life 1992 Hollyn International Corp Elizabeth, NJ 37.
2. Wang, YT, You, JY, Yu, Y, Qu, CL, Zhang, HR, Ding, L, Zhang, HQ, Li, XW. Analysis of ginsenosides in Panax ginseng in high pressure microwave-assisted extraction. Food Chem 2008 110:161–167 .
3. Shibata S , Tanaka O, Shoji J, Saito H, Wagner H, Hikino H, Farnworth NR, editors. Economic and medicinal plant research, vol. 1. London: Academic Press; 1985. p. 217.
4. Huang, KC The pharmacology of Chinese herbs 1993 CRC Press Boca Raton, FL 21.
5. Nah, SY. Ginseng: recent advances and trends. Korean J Ginseng Sci. 1997;21:1–12.
6. Li, Z, Niwa, Y, Sakamoto, S, Shono, M, Chen, X, Nakaya, Y. Induction of inducible nitric oxide synthase by ginsenosides in cultured porcine endothelial cells. Life Sci 2000 67:2983–2989 .
7. Saito, H, Morita, M, Takagi, K. Pharmacological studies of Panax ginseng leaves. Jpn J Pharmacol 1973 23:43–56.
8. Bhargava, HN, Ramarao, P. The effect of Panax ginseng on the development of tolerance to the pharmacological actions of morphine in the rat. Gen Pharmacol 1991 22:521–525.
9. Hasegawa, H, Uchiyama, M. Antimetastatic efficacy of orally administered ginsenoside Rb1 in dependence on intestinal bacterial hydrolyzing potential and significance of treatment with an active bacterial metabolite. Planta Med 1998 64:696–700 .
10. Liu, WK, Xu, SX, Che, CT. Anti-proliferative effect of ginseng saponins on human prostate cancer cell line. Life Sci 2000 67:1297–1306 .
11. Panayi, GS, Lanchbury, JS, Kingsley, GH. The importance of the T-cell in initiating and maintaining the chronic synovitis of rheumatoid arthritis. Arthritis Rheumatol 1992 35:729–735 .
12. Murphy, KM. T lymphocyte differentiation in the periphery. Curr Opin Immunol. 1998;10:226–232 .
13. Kong, WJ, Zhao, Y, Xiao, XH, Li, ZL, Jin, C, Li, HB. Investigation of the anti-fungal activity of coptisine on Candida albicans growth by microcalorimetry combined with principal component analysis. J Appl Microbiol 2009 107:1072–1080 .
14. Wadsö, I. Characterization of microbial activity in soil by use of isothermal microcalorimetry. J Therm Anal Calorim. 2009;95:843–850 .
15. Kong, WJ, Jin, C, Xiao, XH, Zhao, YL, Li, ZL, Zhang, P, Liu, W, Li, XF. Comparative study of effects of two bile acid derivatives on Staphylococcus aureus by multiple analytical methods. J Hazard Mater 2010 179:742–747 .
16. Afzal, AB, Akhtar, MJ, Svensson, LG. Thermal studies of DBSA-doped polyaniline/PVC blends by isothermal microcalorimetry. J Therm Anal Calorim 2010 100:1017–1025 .
17. Kong, WJ, Wang, JB, Jin, C, Zhao, YL, Dai, CM, Xiao, XH, Li, ZL. Effect of emodin on Candida albicans growth investigated by microcalorimetry combined with chemometric analysis. Appl Microbiol Biotechnol 2009 83:1183–1190 .
18. Zhao, H, Bennici, S, Shen, J, Auroux, A. Calorimetric study of the acidic character of V2O5–TiO2/SO4 2− catalysts used in methanol oxidation to dimethoxymethane. J Therm Anal Calorim 2010 99:843–847 .
19. Zhao, YL, Yan, D, Wang, JB, Zhang, P, Xiao, XH. Anti-fungal effect of berberine on Candida albicans by microcalorimetry with correspondence analysis. J Therm Anal Calorim 2010 102:49–55 .
20. Kong, WJ, Li, ZL, Xiao, XH, Zhao, YL, Zhang, P. Activity of berberine on Shigella dysenteriae investigated by microcalorimetry and multivariate analysis. J Therm Anal Calorim 2010 102:331–336 .
21. Xie, CL, Tang, HK, Song, ZH, Qu, SS. Microcalorimetric study of bacterial growth. Thermochim Acta 1988 123:33–41 .
22. Popovich, DG, Kitts, DD. Structure–function relationship exists for ginsenosides in reducing cell proliferation and inducing apoptosis in the human leukemia (THP-1) cell line. Arch Biochem Biophys 2002 406:1–8 .
23. Yang, LN, Sun, LX, Xu, F, Zhang, J, Zhao, JN, Zhao, ZB, Song, CG, Wu, RH, Ozao, R. Inhibitory study of two cephalosporins on E. coli by microcalorimetry. J Therm Anal Calorim 2010 100:589–592 .
24. Tian, G, Rao, L, Xia, Y, Friese, JI. Complexation of neptunium(V) with fluoride in aqueous solutions at elevated temperatures. J Therm Anal Calorim 2009 95:415–419 .
25. Dragoi, B, Rakic, V, Dumitriu, E, Auroux, A. Adsorption of organic pollutants over microporous solids investigated by microcalorimetry techniques. J Therm Anal Calorim 2010 99:733–740 .