Based on the theory of
traditional Chinese medicine, modern methods for drug investigation such as molecular targets in vitro and effects in vivo were used to study the prescription of Jingdan Yimin(JD), including selection of raw materials, composition, proportion, and effective dose of the compounds for treatment of
metabolic syndrome. The IRF mice models, characterized by
insulin resistance and
hypercholesterolemia, were induced by high fat diet. The
insulin sensitivity was estimated with
insulin tolerance test(ITT) and
glucose tolerance test(GTT); the levels of
blood glucose and total
cholesterol(TC), and the activities of α-
glucosidase,
protein tyrosine phosphatase 1B(PTP1B), and
fructose phosphate amide transferase(GFAT)were measured with biochemical methods, respectively. The sample H13(h) extracted from Rhodiola crenulata, Y12(y) from Cordyceps militaris, and
D(d) from Rheum palmatum were selected according to the inhibition activity on both PTP1B and α-
glucosidase in vitro, regulation on
hypercholesterolemia in IRF mice, and effects on GFAT activity, respectively; their synergistic effects on the treatment of
metabolic syndrome were determined in IRF mice; composition proportion of h∶y∶d was measured in accordance with the results of L8(27) orthogonal experiments targeting on the inhibition of both PTP1B and α-
glucosidase; finally, the effective dose was assessed based on the effects on IGT and
hypercholesterolemia, respectively, in IRF mice. In conclusion, the prescription JD is composed by R. crenulata, C. militaris, and R. palmatum with the rate of 20∶1∶1, and its effective oral dose is 200 mg•kg⁻¹ for treatment of
metabolic syndrome; its main mechanism is to inhibit the targets PTP1B and α-
glucosidase. Monarch drug, R. crenulata, can clear away the lung-heat, tonify Qi, resolve stasis and nourish the heart. Adjuvant drug, C. militaris, can tonify the lung Qi and the kidney essence, strengthen waist and knee, accompanied with R. crenulata to enhance the function of invigorating lung and kidney. Assistant drug, rhubarb, can clear heat, detoxify, and remove blood stasis. These three herbs are compatible to show the effects of tonifying Qi, nourishing essence, clearing heat, reducing phlegm and resolving masses for the treatment of
metabolic syndrome.