To explore the changes of estradiol (E2) and vascular endothelial growth factor (VEGF) levels of women with polycystic ovary syndrome (PCOS) after treated by Zishenyutai pill combined with letrozole, and to study their influence on the early pregnancy of these women. Methods: From May 2018 to July 2019, 96 women with PCOS were enrolled, and were divided in 52 cases in observation group and 44 cases in control group according to the method of random number table. The women in the control group were treated by letrozole alone, and the women in the observation group were treated by letrozole combined with Zishenyutai pill. 5 days after treatment, the levels of E2 and VEGF, endometrial thickness, and the incidences of ovarian hyperstimulate syndrome (OHSS), ovulation, pregnancy, and adverse reactions of the women in the two groups were observed. Results: After treatment, the total effective rate (98.1%) of the women in the observation group was significant higher than that (84.1%) of the women in the control group, and the levels of E2 and VEGF of the women in the observation group were significant higher than those of the women in the control group (all P<0.05). There were no significant differences in ovulation rate, number of dominant follicles, pregnancy rate, endometrial thickness, and incidence of OHSS of the women between the two groups (P>0.05). There were no significant differences in the incidences of thrombocytopenia, hemoglobin reduction, and total adverse reactions of gastrointestinal tract of the women between the two groups (P>0.05). Conclusion: Zishenyutai pill combined with letrozole can effectively improve the levels of E2 and VEGF of women with PCOS, and can increase the clinical effect without increasing adverse reactions.