Rising trends towards the development of oral herbal male contraceptive: an insight review

Verma, Surender; Yadav, Akash

doi:10.1186/s43094-020-00154-7

Future Journal of Pharmaceutical Sciences

Table 1 List of traditional plants and isolated chemical compounds from plants having antifertility activity

From: Rising trends towards the development of oral herbal male contraceptive: an insight review

Sr. no.	Botanical name	Common name	Family	Part used	Subject	Dose	Active constituents	Duration of administration (days)	Mechanism of action	Antifertility activity	References
Phytoconstituents having spermicidal activity
1.	Acacia auriculiformis Benth.	Ear leaf acacia	Fabaceae	Seeds	Human sperm	0.35 mg/ml	Acacic acid lactone	–	Disintegrate sperm plasma membrane and immobilize sperm	–	[32]
2.	Aegle marmelos (L.) Corrêa	Bael	Rutaceae	Leaves	Rat	200 and 300 mg/kg Body weight (B.W.) /day	Coumarins, tannis, phenols, rutin	60	Suppress gonadotropic hormone	Reversible	[33]
3.	Albizia lebbeck (L.) Benth	Bhandi	Fabaceae	Pods	Rat	100 mg/kg B.W.	Labbekanin-E, saponins	60	Reduce sperm density and sperm motility and decrease testes and prostrate size	–	[34]
4.	Allium sativum L.	Lahsun	Lilliceae	Bulb	Human sperm	0.25 and 0.5 g/ml	Allitridum	–	Disrupt membrane architecture	Irreversible	[20]
5.	Cananga odorata (Lam.) Hook. f. & Thomson	Ylang yalang	Annonaceae	Root bark	Rat	1 g/kg B.W./day	52-kd protein	60	Decrease androgen production, increase 3-hydroxy-3-methyl-glutaryl-CoA (HMG CoA) reductase activity, and decrease 3β-hydroxy steroid dehydrogenase enzyme activity	Reversible	[35]
6.	Cestrum parqui (Lam.) L'Hér.	Chilean cestrum	Solanaceae	Leaves	Human semen	40, 62.5, 100, 150, and 250 μg/ml	Saponin	–	Disrupt sperm plasma membrane sterol	–	[36]
7.	Chenopodium album L.	Lamb’s quarters	Chenopodiaceae	Fruits	Rat/rabbit	2 mg/ml	Oleanolic acid, glucuronic acid	–	Disintegrate sperm plasma membrane and cause the dissolution of acrosomal cap causing sperm death	–	[37]
8.	Chromolaena odoratum (L.)	Tivra gandha	Compositae	Leaves	Rat	250 and 500 mg/kg B.W.	–	14	Decrease biomolecule concentration and disrupt seminiferous tubules	–	[38]
9.	Colebrookia oppositifolia	Bhinda	Lamaceae	Leaves	Rat	100 and 200 mg/kg	5,6,7,4′-tetramethoxy flavones, 5,6,7-trimethoxy flavones, 5,7,4′-trihydroxy flavones 3-o-glucoside	56–70	Reduce sialic acid, fructose concentration, and ascorbic acid	–	[39]
10.	Juniperus phoenica (L.)	Cedar	Cupressaceae	Ripe red cones	Rat	400 and 800 mg/kg	α-Pinene, δ-3-carone, β-phellandrene	21	Inhibit LH and gonadotropin-liberating hormone	–	[40]
11.	Mollugo pentaphylla L.	Five-leaved carpetweed	Molluginaceae	Aerial part	Human sperm	10, 30, 100, and 300 μg/ml	Mollugogenol-A (saponin)	–	Plasma membrane-losing osmoregulatory properties and enhance superoxide ions and lipid peroxidation	–	[41]
12.	Quassia amara L.	Bitterwood	Simaraubaceae	Stem wood	Rat	0.1, 1.0, and 2 mg/kg B.W.	Quassin, 2-methoxycanthin-6-one	56	Decrease serum level testosterone, LH, and FSH	Reversible	[42]
13.	Sapindus mukorossi Gaertn.	Reetha	Sapindaceae	–	Human Semen	0.05%, 0.1%, 1.25%, and 5%	Saponins, digitonin	–	Disruption and erosion of membrane	–	[32]
14.	Terminalia chebula Retz.	Chebulic myrobala	Combretaceae	Dry fruits	Rat	50 and 100 mg/kg/day	Anthraquinones, ellagitamic acid, 4,2,4-chebulyl-β-d-glucopyranose, ellagic acid, gallic acid	60	Inhibit acrosomal enzyme and sperm hyaluronidase enzyme	Reversible	[43]
15.	Tinospora cordifolia (Willd)	Guduchi	Menispermaceae	Stem	Rat	100 mg/rat/day	–	60	Reduce plasma level of testosterone and inhibit glycolysis in spermatozoa	–	[44]
16.	Ziziphus mauritiana Lam.	Ber	Rhamnaceae	Barks	Human semen	0.1 and 0.5 mg/ml	Saponin	20 s–20 min	Disrupt lipid within sperm membrane	–	[45]
Phytoconstituents with antispermatogenic activity
1.	Bacopa monnieri (L.) Wettst.	Brahmi	Scrophulariaceae	All part	Mice	250 mg/kg B.W. /day	–	28 and 56	Decrease fructose level and inhibit spermatogenesis	Reversible	[46]
2.	Barleria prionitis L.	Vajra-danti	Acanthaceae	Root	Rat	100 mg/kg	Barlerin, acetyl barlerin, apigenin-7-o-glucoside	60	Reduce glycogen, protein, and sialic acid content and deplete germinal and Leydig cell constituents	–	[47]
3.	Cannabis sativa L.	Ganja	Cannabinaceae	Seeds	Rat	20 mg/day	Cannabinoids	20	Act on cannabinoids receptors	–	[48]
4.	Chrysophyllum albidum G.Don	White star apple, vdara	Compodeoidea	Root bark	Rat	100 and 200 mg/kg	Alkaloids, tannis, saponin, phenol, flavonoids	147	Reduce gonadotropins level (FSH and LH) and inhibit spermatogenesis	–	[49]
5.	Citrullus colocynthis (L.) Schrad.	Tumba	Cucurbitaceae	Root	Rat	50, 100, and 200 mg/kg B.W./day	Hentriacontane, n-octacosanol, 1,2,6-hexa-cosanediol	60	Inhibit pituitary gonadotropin secretion and reduce sialic acid and protein	Reversible	[50]
6.	Crotalaria juncea L.	Sunn hemp	Papilionaceae	Seed	Mice	25 mg/100 g/day	–	30	Reduce seminiferous tubular fluid and decrease protein content, FSH, and LH	–	[51]
7.	Cuminum cyminumin L.	Jeera	Apiaceae	Seed	Rat	100 mg/rat/day	–	60	Sloughing or death of epithelial cells and reduce glycogen content	–	[52]
8.	Curcuma longa L.	Haldi	Zingiberaceae	Rhizomes	Mice	600 mg/kg B.W./day	–	56 and 84	Inhibit gonadotropin secretion and decrease serum level	Reversible	[53]
9.	Fadogia agrestis Schweinf. ex Hiern	Nagbitenga	Rubiaceae	Stem	Rat	18, 50, and 100 mg/kg B. W.	Alkaloids, anthraquinones, flavonoids, saponin	28	Increase cholesterol level and reduce glycogen content	Reversible	[54]
10.	Hibiscus rosasinensis L.	Gudhal	Malvaceae	Flower	Mice	150 and 300 mg/kg	–	20	Decrease androgen synthesis and reduce spermatogenic element	–	[55]
11.	Lepidium meyenii Walp.	Maca	Brassicaceae	Root	Rat	66.7 mg/ml	–	14	Enhance epididymal weight and reduce stages I–VI of seminiferous epithelium	–	[56]
12.	Leptadenia hastata	Cheila	Asclepediaceae	Leaves and stem	Rat	100, 200, 400, and 800 mg/kg	–	60	Reduce Leydig cell and imbalance LH, prolactin, and testosterone serum level hormones	–	[57]
13.	Momordica charantia L.	Karela	Cucurbitaceae	Seed	Rat	25 mg/100 g B.W.	–	35	Inhibit gonadotrophins (FSH) and enhance cholesterol level and sudanophilic lipids	–	[58]
14.	Mondia whitei (Hook.f.) Skeels	La racine	Periplocaceae	Root	Rat	500 and 1000 mg/kg B.W.	Steriods, triterpenes	30	Reduce intratesticular concentration of cholesterol	Reversible	[59]
15.	Morinda lucida Benth.	Brimstone tree	Rubiaceae	Leaves	Rat	400 mg/kg/day	Anthraquinones, anthraquinols	28 and 91	Reduce serum testosterone level and inhibit acetylcholinesterase	Reversible	[60]
16.	Mucuna urens L.	Ibaba	Cannabaceae	Seed	Rat	70, 140, and 210 mg/kg B.W.	Flavonoids, anthranoid, anthraquinones, polyphenols	14	Inhibit endogenous gonadotrophic activity	–	[61]
17.	Ocimum gratissimum L.	African basil, ram tulsi	Lamiaceae	Leave	Mice	11–88 mg/kg	Eugenol, citral, linalol, charvicol, thymol, gerianol	7, 14 and 28	Deplete Leydig and Sertoli cells and destroy cell membrane	–	[62]
18.	Parkinsonia aculeate L.	Vilyati babul	Caesalpiniaceae	Stem bark	Rat	50, 100, and 200 mg/rat/day	α-Amyrin acetate, β-amyrin acetate, 6-hydroxypentacosylpentanoate ethynoma decanoate, 6-hydroxytritriacontan-3-one	60	Reduce testosterone level and Leydig cell diameter and seminiferous tubular diameter	–	[63]
19.	Piper nigrum L.	long pepper	Piperaceae	Fruits	Mice	25 and 100 mg/kg B.W./day	Piperine	20 and 90	Reduce sialic acid level and decrease fructose concentration in seminal vesicle	Reversible	[64]
20.	Ruta graveolens L.	Rue	Rutaceae	Leave	Rat	500 mg/kg B.W.	–	60	Reduce serum androgen level and degenerate Leydig cells	–	[65]
21.	Semecarpus anacardium	Bhilawa	Anacardiaceae	Fruit	Rat	100, 200, and 300 mg/kg/day	–	60	Decrease sialic acid content and androgen production (LH)	–	[66]
22.	Terminalia bellirica (Gaertn.) Roxb.	Baheda	Combretaceae	Fruit	Rat	10 and 25 mg/100 g B.W.	Triphala	50	Reduce androgen level and increase cholesterol level	–	[67]
23.	Thevetia peruviana	Lucky nut, Mexican oleander	Apocynaceae	Stem bark	Rat	100 mg/rat/day	α-Amyrin acetate, lupeol acetate, α-amyrin, β-amyrin, lupeol, thevetigenin	60	Deform and impair Leydig cell and reduce androgen concentration	–	[68]
Phytoconstituents acts through Sertoli cells
1.	Azadirachta indica A.Juss.	Neem	Meliaceae	Leaves	Rat	100 mg/rat/day	–	48	Degenerate germ cells	Reversible	[69]
2.	Dendrophthoe falcate (L.f.) Ettingsh.	Banda	Loranthaceae	Stem	Rat	100 mg/kg B.W./day	Quercitrin (quercetin-3-o-rhamnoside ), kaempferol, rutin	60	Decrease seminiferous tubular fluid and reduce androgen synthesis and sialic acid	-	[70]
3.	Thespesia populnea (L.) Sol. ex Corrêa	Tulip tree	Malvaceae	Leaves	Mice	400 mg/kg B.W.	–	15	Elongate seminiferous tubules	–	[71]
4.	Tripterygium wilfordi Hook. f.	Yellow vine root	Celastraceae	Root	Rat	100 mg/kg/day	–	–	Degenerative changes of seminiferous epithelium and reduce reproductive cells in testes	Irreversible	[72]
Phytoconstituents acts through Leydig cells
1.	Berberis chitria Buch.-Ham. ex Lindl.	Daruhaldi	Berberidaceae	Root	Dog	30 mg/kg/day	Palmitine hydroxide	60	Decrease postmeiotic germ cells and decrease androgen binding protein of Sertoli cells via FSH	–	[73]
2.	Calotropis procera	Camelweed	Asclepiadaceae	Roots	Gerbil/rabbit	25 mg/kg B.W.	Calotropin	30	Suppress testicular function by decreasing androgenic parameter	–	[74]
3.	Garcinia cambogia	Malabar tamarind	Cluciaceae	Seed	Rat	100 and 200 mg/kg B.W.	Biflavonoid, xanthone	42	Enhance interstitial spaces and reduce Leydig cells in interstitial space and seminiferous tubules contraction	–	[75]
4.	Malvaviscus conzattii Greenm.	Turk’s cap mallow	Malvaceae	Flower	Rat	800 mg/kg B.W. /day	–	30	Reduce germ cells and impairs function of epididymides	–	[76]
5.	Martynia annua L.	Scorpion	Martyniaceae	Root	Rat	50, 100, and 200 mg/kg B.W.	–	30	Reduce scrum concentration of LH and testosterone	Reversible	[77]
6.	Ocimum sanctum L.	Tulsi	Lamiaceae	Fresh leaves	Rabbit	2 g/day	–	30	Reduce pH, mucoprotein, and alkaline phosphatase and make non-viable spermatozoa	Reversible	[21]
Phytoconstituents with antimotility activity
1.	Carica papaya L.	Papita	Caricaceae	Seeds	Monkey	50 mg/kg B.W. /day	–	360	Hasten sperm transport leading to ejaculation and affect composition of epididymal fluid and their enzymes on spermatozoa	Reversible	[78]
2.	Echinops echinatus Roxb.	Utakatira, oontkateli	Asteraceae	Roots	Rat	50, 100, and 200 mg/kg B.W. /day/rat	Echinopsine, echinopsidine, echinozolinone	60	Reduce concentration of protein in the cauda epididymis and testicular glycogen level and reduce ascorbic acid content of the adrenal gland	–	[79]
3.	Gossypum herbaceum	Cotton	Malvaceae	Fruit	Rabbit	20 mg/day	Gossypol acetic acid	84	–	–	[80]
4.	Lagenaria breviflora (Benth.) Roberty	Molina	Cucurbitaceae	Whole fruit	Rat	1000, 2000, 4000, and 8000 mg/kg B.W.	–	14	Degenerate seminiferous tubules	–	[81]
Phytoconstituents acts by unbalancing hormones
1.	Abelmoschus esculentus (L.) Moench	Okra	Malvaceae	Fruit	Rat	70 mg/kg B.W./day	Flavonoids, saponins	28	Reduce serum testosterone level and spermatogenesis	Reversible	[82]
2.	Abrus precatorius L.	Coral bead vine, rosary pea, ratti	Leguminosae	Seed	Rat	250 mg/kg	Abridine	30 and 60	Impair function of sperm plasma membrane, suppress oxidative/energy metabolism, and reduce sperm motility	Reversible	[83]
3.	Bulbine natalensis Baker	Bulbine	Asphodelaceae	Stem	Rat	25, 50, and 100 mg/kg B.W.	Alkaloids, tannis, anthraquinones	7	Reduce serum testosterone and progesterone levels	–	[84]
4.	Curcuma longa L.	Haldi	Zingiberaceae	Rhizomes	Rat	500 mg/kg/day	–	60	Decrease androgen synthesis and Leydig cell nuclei diameter and inhibit Leydig cell function	–	[85]
5.	Psoralea corylifolia L.	Babchi	Leguminosae	Seeds	Rat	10 g/kg B.W.	Corylin, bavachin, psoralen, isopsoralen, psoralidin	84	Decrease serum testosterone and FSH levels and suppress pituitary testicular axis	–	[86]
6.	Stevia rebaudiana	Sugar leaf	Asteraceae	Leave	Rat	2 ml/rat	Stevioside	60	Decrease androgen level	Irreversible	[87]
7.	Syzygium aromaticum (L.) Merr. & L.M.Perry	Lavang	Myrtaceae	Flower buds	Mice	15, 30, and 60 mg/kg B.W.	Eugenol, β-caryophyllene	35	Destroy germ cells and inhibit spermatogonia	–	[88]

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