Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia.
PLoS One. 2022 Jul 28;17(7):e0271735. doi: 10.1371/journal.pone.0271735. eCollection 2022.
Stinging nettle root and leaf extracts were tested for their effect on prostatic smooth muscle contractility. Root extract did not affect electrical field stimulation induced-nerve mediated contractions of isolated rat prostates. On the other hand, leaf extract attenuated electrical field stimulation-induced contractions at all frequencies. Similarly, contractions elicited by exogenous administration of ATP and αβ-methylene ATP were inhibited by leaf extract, whereas contractions elicited by exogenous administration of noradrenaline or acetylcholine were unaffected. The active component was present within the aqueous phase of the leaf extract. In mouse mating studies, stinging nettle leaf extract (50 mg p.o. daily) reduced male fertility by 53% compared to vehicle-treated male mice. Cardiovascular parameters were unaffected by administration of stinging nettle leaf extract (p ≥ 0.057). Treated mice exhibited normal mating behaviour. Bladder and testes weighed less in stinging nettle leaf extract treated mice. All other organs and total body weight were unaffected. It is concluded that stinging nettle leaf extract reduces contractility of genitourinary smooth muscle by acting as an antagonist at postjunctional P2X1-purinoceptors. These data indicates that blocking sperm transport through pharmacological blockade of P2X1-purinoceptors via oral administration is consistent with an effective and convenient biological strategy male contraception.
荨麻根和叶提取物的前列腺平滑肌收缩性的影响进行了测试。根提取物不影响电刺激诱导的神经介导的分离大鼠前列腺收缩。另一方面，叶提取物在所有频率下均减弱电刺激诱导的收缩。同样，叶提取物抑制由外源性给予 ATP 和αβ-亚甲基 ATP 引起的收缩，而由外源性给予去甲肾上腺素或乙酰胆碱引起的收缩不受影响。活性成分存在于叶提取物的水相部分。在小鼠交配研究中，荨麻叶提取物（每天 50mg p.o.）与载体处理的雄性小鼠相比，雄性生育力降低了 53%。心血管参数不受荨麻叶提取物的影响（p≥0.057）。接受治疗的小鼠表现出正常的交配行为。在荨麻叶提取物处理的小鼠中，膀胱和睾丸的重量减轻。所有其他器官和体重均不受影响。结论是，荨麻叶提取物通过作为后突触 P2X1-嘌呤能受体的拮抗剂来降低泌尿生殖道平滑肌的收缩性。这些数据表明，通过口服药理学阻断 P2X1-嘌呤能受体来阻断精子运输是一种有效的、方便的生物策略，可用于男性避孕。
