gossypol-acetic-acid and Endometriosis

Estrogen and progesterone cytosol receptor (ERc, PRc) concentrations of endometrium biopsied during different phases of menstrual cycle were measured by dextran-coated charcoal method in 27 normal fertile women and 24 patients with endometriosis. 15 out of 24 endometriotic patients were put on gossypol for 2 months thereafter. After discontinuation of the drug, ERc, PRc contents of endometrium were reexamined during the same cycle day. Serum estradiol (E2) and progesterone (P) levels were also compared before and after gossypol treatment. In addition, endometriotic tissue and intrauterine endometrium were immediately obtained from the same patient after surgery in 16 cases with endometriosis, and their ERc, PRc concentrations were also compared.. endometrium ERc, PRc concentrations of normal controls fluctuated during the menstrual cycle, with the peak at late follicular phase. In endometriosis group, the ERc, PRc contents and cyclic changes of endometrium in situ were not significantly different from the normal controls. However, the ERc, PRc contents of endometriotic tissue were significantly lower than those of endometrium in situ (P = 0.0036 and < 0.0001 respectively) without cyclic changes during menstrual cycle. After 2 months of gossypol therapy, serum E2 and P levels tended to decrease but the differences were not significant. Glandular secretion of endometrium decreased in only 4 out of 15 cases under pathological examination. In contrast, the ERc, PRc concentrations of endometrium in situ differed significantly from the pretreatment values (P = 0.0217 and 0.01 respectively). These data indicated: (1) The response of endometriotic tissue to estrogen and progestin was lower than that of endometrium in situ.(ABSTRACT TRUNCATED AT 250 WORDS)

Topics: Adult; Antineoplastic Agents, Phytogenic; Endometriosis; Endometrium; Estradiol; Female; Gossypol; Humans; Middle Aged; Ovarian Diseases; Receptors, Estrogen; Receptors, Progesterone; Uterine Diseases

Effects of the gossypol on endometriosis in 12 cases of control were observed. The results showed that the gossypol administered orally was effective in endometriosis patients. The basal body temperature changed from biophase to monophase. Dysmenorrhea disappeared in 11/12 patients. Amenorrhea occurred in 10/12 patients and the ovarian endometrial cyst was shrinkable. Serum progesterone and estradiol were decreased after gossypol administration, but follicle-stimulating hormone and luteinizing hormone were increased evidently. Histochemical and cytochemical observations revealed that the activity of acid phosphate (ACP), nonspecific esterase (NSE) and alkaline phosphate (AKP) in both aberrant uterine endometrium and uterine endometrium in situ were decreased evidently. The above results suggest that the satisfactory therapeutic effect of gossypol on endometriosis may be due to not only the indirect but also the direct action on uterine endometrium.

Topics: Adult; Antineoplastic Agents, Phytogenic; Drugs, Chinese Herbal; Endometriosis; Female; Gossypol; Humans; Middle Aged; Ovarian Neoplasms; Uterine Neoplasms

Gossypol treatment of endometriosis and uterine myomas in 15 cases was started with a daily dose of 20 mg of gossypol-acetic acid twice a day for 20 days as a loading dose, followed by 40 mg (20 mg twice weekly). A maintenance dose of 20 mg was given weekly. The total course of treatment lasted about 6 months. Light and electron microscopic examination of the endometrium was carried out before treatment and 2, 3, 4, and 6 months after gossypol treatment. After gossypol treatment three different characteristics of the endometrium were noted: (1) irregular secretory activity, (2) proliferative activity, and (3) atrophy. On electron microscopic examination it was shown that there were important changes of the organelles, indicating suppressed secretory activity. Based on the above results, the nature and significance of the ultrastructural changes of the endometrium induced by gossypol were analyzed and the possibility of developing a new field of research in female contraception with gossypol was considered.

Topics: Endocrine Glands; Endometriosis; Endometrium; Female; Gossypol; Humans; Leiomyoma; Menstruation; Time Factors; Uterine Neoplasms