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Nature-inspired male contraceptive and spermicidal products

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Abstract

The use of hazardous female contraceptives is still the first choice in family planning programs. Moreover, all the drugs examined to be used as infertility inducers in males or as spermicides into the cervix were not sufficiently efficient, in addition to not having complete safety. Therefore, many researchers were directed to assess complementary and alternative medicine to address these harmful effects. Accordingly, this review aimed to evaluate the efficacy of natural products alternatives in the induction of male infertility (male contraception) and/or proceeding of spermicidal action (vaginal contraception), although, that concept may be contradictory or prohibited in some developing and well-developed countries due to low birth rate problems, traditional, and religious beliefs. This study covers the literature from 1968 to 2019. In this review, we included previous controlled experiments with adult rats, mice, rabbits, monkeys and humans with clearly complete experimental criteria. The interventions were natural products derived from raw or refined plants, parts of plants or semi-synthesized compounds. The additional data such as toxicity and safety profiles, irreversibility, mechanism of actions, microbicidal activity, effective doses or concentrations, quantitative analysis in daily food and oral bioavailability, were included to identify the most promising natural products for contraception. In accordance with vaginal contraception, there were some herbal extracts and/or principles that may be used as prospective candidates after performing more pre-clinical and clinical trials. These products are acaciaside-B, Achyranthes aspera protein, xanthotoxin, oleanolic acid 3-β-d-glucuronide, ursolic acid, bivittoside D, subtilosin, Sapindus mukorossi saponins and Sapindus saponaria saponins fractions. Moreover, some products may be considered as effective and safe male contraceptives after clinical evaluation; which are NB-DNJ, NB-DGJ, β-caryophyllene, oleanolic acid, Tripterygium wilfordii glycosides, tripchlorolide, Carica papaya fatty acid esters and ZNF185-derived peptide. Generally, natural products that have high potential to be used as drug candidates concerning male and vaginal contraception are limited.

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Abbreviations

CBR2:

Cannabis-derived cannabinoid receptors type 2

CUC:

Current use of contraceptives

Cu–Cr:

Cupper–curcumin complex

DNJ:

1-Deoxynojirimycin

FSH:

Follicular stimulating hormone

GnRH:

Gonadotropin releasing hormone

HFKS:

Hausa/Fulani/Kanuri/Seriberi

HIV:

Human immunodeficiency virus

HMG CoA:

Hydroxy-3-methylglutaryl coenzyme-A

HSD:

Hydroxysteroid dehydrogenase

HSV:

Herps simplex virus

KATNAL1:

Katanin p60 ATPase-containing subunit A-like 1 protein

LPO:

Lipid peroxidation

MEC:

Minimum effective concentration

N-9:

Nonoxynol-9

NB-DGJ:

N-butyldeoxygalactonojirimycin

NB-DNJ:

N-butyldeoxynojirimycin

P-gp:

P-glycoproteins

PPARs:

Peroxisome proliferator-activated receptor

STDs:

Sexually transmitted diseases

SLs:

Sophorolipids

THC:

Tetrahydrocannabinol

MC-40:

(Cu–Cur)-β-cyclodextrin gel

ZNFs:

Zinc finger proteins

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We thank NUB for financial support.

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MAA collected a complete survey of all compounds; MAA and HMH wrote the manuscript; URA interpreted and revised the results, and wrote the manuscript; HMH, AFT, MBN, and MSH discussed the results scientifically and contributed to the editing of the paper.

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Correspondence to Usama Ramadan Abdelmohsen.

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Hifnawy, M.S., Aboseada, M.A., Hassan, H.M. et al. Nature-inspired male contraceptive and spermicidal products. Phytochem Rev 20, 797–843 (2021). https://doi.org/10.1007/s11101-020-09721-5

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