Natural Products with Potential for Nonhormonal Male Contraception

Abstract

Despite increased access to contraception over the last 60 years, unplanned pregnancies continue to contribute to economic disparities and overpopulation. Additionally, the burden of family planning falls primarily on women, as a reliable pharmaceutical male contraceptive has yet to be developed. The objective of this literature-based systematic review was to identify compounds for future study from natural sources with potential nonhormonal male contraceptive activity. After the exclusion of extracts and compounds with known hormonal mechanisms, 26 unique compounds were identified from natural species. The plant source, compound class, structure, target, mechanism of action, safety/toxicity profile, and in vitro, in vivo, and human studies for each compound were evaluated and discussed. β-Caryophyllene, embelin, oleanolic acid, triptonide, and N-butyldeoxynojirimycin (NB-DNJ) were selected as the five most promising compounds for future study using prespecified criteria such as number of studies, efficacy and safety profile, reversibility, and previous use in humans for any indication. In order to move forward with development of a male contraceptive from a natural source, additional studies are needed to determine the predicted safety and efficacy for in vivo and human clinical trials.

The nutritional and industrial significance of cottonseeds and genetic techniques in gossypol detoxification

“…Wang et al (1987) reported that gossypol is an anti‐fertility compound; 30 mg/kg of orally administered (−)‐gossypol for 7 days adversely influenced rat fertility (Wang et al, 1987) by causing azoospermia (spermless ejaculation) in males (Coutinho, 2002). This finding is consistent with those of Shunnarah et al (2021), who reported that gossypol stifles reactions in the acrosomes of human and mammal sperms (Shunnarah et al, 2021). Notwithstanding its usefulness as a bioactive contraceptive, it has serious ramifications, such as irreversible sterility, anorexia, and respiratory disorders (Lim et al, 2019).…”

KUALITAS SPERMATOZOA DAN BERAT ORGAN REPRODUKSI MENCIT (Mus musculus) SETELAH PEMBERIAN EKSTRAK BIJI KLABET (Trigonella foenum-graecum L.)

“…Rata-rata morfologi abnormal spermatozoa paling banyak ditemukan pada mencit dengan perlakuan dosis tertinggi (P3) yaitu 66,00% dan paling sedikit ditemukan pada perlakuan kontrol (P0) yaitu 19,20%. Hal ini dapat terjadi dikarenakan adanya senyawa alkaloid pada biji klabet yang diduga dapat menurunkan kadar enzim antioksidan yang menyebabkan peningkatan Reactive Oxygen Species (ROS) di epididimis, sehingga dapat mengganggu pematangan dan penyimpanan spermatozoa menyebabkan spermatozoa abnormal (Shunnarah et al, 2021). Menurut penelitian Susilawati et al (2022) yang menunjukkan terjadinya kenaikan spermatozoa yang abnormal.…”

Structure, properties of gossypol and its derivatives—from physiological activities to drug discovery and drug design

“…Gossypol inhibits the acrosomal reactions of human and mammalian sperm. 56 In 1978, Chinese scientists announced that oral gossypol was used as a reversible male infertility agent. Gossypol was effective in antifertility, 0.3 mg kg −1 of body weight caused azoospermia.…”