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Prospective birth control pill for men has its origin in an arrow poison

Date:
January 17, 2018
Source:
American Chemical Society
Summary:
Women have many options for oral contraceptives that are safe, effective and reversible, but despite decades of research, men have none. Now, scientists report a rat study that shows they finally have a good lead for a male birth control pill. It's based on ouabain, a plant extract that African warriors and hunters traditionally used as a heart-stopping poison on their arrows.
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Women have many options for oral contraceptives that are safe, effective and reversible, but despite decades of research, men have none. Now, scientists report a rat study in ACS' Journal of Medicinal Chemistry that shows they finally have a good lead for a male birth control pill. It's based on ouabain, a plant extract that African warriors and hunters traditionally used as a heart-stopping poison on their arrows.

Two types of African plants make ouabain. Mammals also produce it in their bodies, though at lower levels that are thought to help control blood pressure; doctors sometimes prescribe small doses of the compound to treat heart attack patients. Ouabain disrupts the passage of sodium and calcium ions through the membrane protein Na,K-ATPases, which are are found in cell membranes and are made up of protein subunits. Some subunits are found in cardiac tissue, but one type of subunit called ?4 is found only in sperm cells. This protein is known to be critical in fertility -- at least in male mice. Ouabain binds strongly to ?4, but it also binds to other Na,K-ATPase subunits, albeit less tightly. Prior clinical studies have shown that ouabain curbs fertility in men. However, ouabain itself isn't an option as a contraceptive because of the risk of heart damage. So Gunda Georg, Gustavo Blanco and colleagues set out to design ouabain analogs that are far more likely to bind to the ?4 protein in sperm than to subunits found in heart tissue.

By removing a sugar group from ouabain and also replacing its lactone group with a triazole group, the researchers created a derivative that is particularly good at zeroing in on ?4 in sperm cells in rats. Once bound, it interferes with the cells' ability to swim, which is essential to its role in fertilizing an egg, the scientists showed. The compound had no toxicity in rats. The researchers say that the contraceptive effect should be reversible because ?4 is only found on mature sperm cells. That means sperm cells produced after stopping treatment with the ouabain derivative shouldn't be affected.

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Materials provided by American Chemical Society. Note: Content may be edited for style and length.


Journal Reference:

  1. Shameem Sultana Syeda, Gladis Sánchez, Kwon Ho Hong, Jon E. Hawkinson, Gunda I. Georg, Gustavo Blanco. Design, Synthesis, in vitro and in vivo Evaluation of Ouabain Analogs as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception. Journal of Medicinal Chemistry, 2018; DOI: 10.1021/acs.jmedchem.7b00925

Cite This Page:

American Chemical Society. "Prospective birth control pill for men has its origin in an arrow poison." ScienceDaily. ScienceDaily, 17 January 2018. <www.sciencedaily.com/releases/2018/01/180117164007.htm>.
American Chemical Society. (2018, January 17). Prospective birth control pill for men has its origin in an arrow poison. ScienceDaily. Retrieved March 21, 2019 from www.sciencedaily.com/releases/2018/01/180117164007.htm
American Chemical Society. "Prospective birth control pill for men has its origin in an arrow poison." ScienceDaily. www.sciencedaily.com/releases/2018/01/180117164007.htm (accessed March 21, 2019).

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