Backgrounds: The shifts of bellets targeting refractory disease have happened from magic to dirty or (herbal)combination. Herbs contain countless chemicals. Thought their active comparison produces ERBCs, groupings are too many to finish within the century. Also, following oral herbs unabsorbed compounds-induced responses likely is untruth by in vivo or vitro study because of interference. Without linking herbal compounds, absorbed profile and efficacy pose dilemma and scientific challenge for TCM or herbal products.
Aim: To establish an approach rapidly linking herbal compounds and pharmacology.
Method: 11 TCMs were selected including SLC(Salvia miltiorrhiza Bge., Ligusticum chuanxiong Hort.(LCH), Carthamus tinctorius L), GX II(SLC + Paeonia lactiflora P(PIP), and Dalbergiae odoriferae lignum), FA(Fructus Aurantii), FM(FA + Magnolia Bark), FL(FA + LCH), FP(FA+PIP), FC(FA+Chinese angelica), SNS(FA + PIP + Radix Bupleuri + licorice), CSS(SNS + LCH + rhizoma cyperi + pericarpium citri reticulatae), rheum officinale and Rhizoma Drynariae. All are compared their activities with their absorbed bioactive compounds(ABCs) whose doses each is or not identical to its content in parent formula(in vivo study) and concentration in blood(in vitro experience) to obtain truly efficacy or cellular and molecular mechanism.
Results and highlights: GXII/DCH/FA/FL/FM or FA/FM/FL/SNS/CSS/rheum officinale/Rhizo- ma Drynariae and their corresponding ABCs induced identical or similar effects. Of these, three studies each rapidly elucidated its ABCs precisely responsible for their parent formula's efficacy for the first time: i) FTA(ferulic acid, hydroxyl safflor yellow A, tanshinol) represent GXII for acute cardioprotection via increase in coronary flow and anti-apoptosis; ii) F is quantitatively linked to DCH-induced APV(antidepressants, prokinetic and vasodilation) via mediating shared ghrelin; and iii)FTA endothelium-dependently contribute vasodilation by GXII via increasing coronary flow and antiapoptosis.
Conclusion and significance: Via simply active comparison between formula and absorbed compounds, 300～1000 chemicals-selected 1～8 quantitatively or widely linked herbal traditional efficacy, triggering innovations e.g., novel target and lead compounds via deciphering ancient efficacy and subsequent related pathogenesis.
This work was supported by National Natural Science Foundation of China (No.30070932, 30271648, 30325045, 30572339, 81072967, 81173591, 81373855 and 81573797). A project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions (integration of Chinese and western medicine) and high-level talents of Nanjing University of Chinese Medicine.
