Modulation of intrasperm Ca<sup>2+</sup>: A possible maneuver for spermicidal activity

Gupta, Anshu; Gupta, Puneet; Jain, Subheet Kumar; Moudgil, Pranab; Tiwary, Ashok K.

doi:10.1002/ddr.20006

Cited by 8 publications

(6 citation statements)

References 167 publications

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“…These studies revealed that an elevation of intrasperm [Ca 2þ ] to $1200 nM produced complete loss of viability of human ejaculated sperm cells. Hence, pharmacological modulation for achieving this critical intrasperm [Ca 2þ ] threshold seems to offer a feasible approach for contact spermicidal activity (Gupta et al 2005).…”

Section: Introductionmentioning

confidence: 99%

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Gulati

Tiwary

Jain

et al. 2006

Journal of Pharmacy and Pharmacology

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Elevation of intrasperm Ca(2+) is reported to influence viability of ejaculated spermatozoa. Human spermatozoa possess inositol triphosphate (IP(3))-sensitive Ca(2+) stores, which can be targeted for increasing intrasperm Ca(2+) level. The influence of agents affecting Ca(2+) homeostasis has been investigated. Miconazole nitrate, clotrimazole and loperamide hydrochloride produced a dose- and time-dependent decrease in viability, each requiring respectively 0.5, 1.0 and 1.0 mM for producing death of all sperm cells immediately upon addition to ejaculated human semen samples. The reduction in sperm viability was accompanied by elevation of intrasperm Ca(2+) and was not affected by presence or absence of extracellular Ca(2+). Significantly (P<0.05) less time was required for producing complete loss of sperm viability and increasing intrasperm Ca(2+) when any of these drugs was added to sperm cells previously treated with selected agents affecting Ca(2+) homeostasis. This enhanced spermicidal activity of miconazole, clotrimazole and loperamide appeared to be due to further mobilization of Ca(2+) from partially depleted intrasperm Ca(2+) stores. Synergism of spermicidal activity and intrasperm Ca(2+) elevation by miconazole or clotrimazole was observed when Ca(2+) efflux from sperm cells was simultaneously inhibited by 2',4'-dichlorobenzamil hydrochloride, a Na(+)-Ca(2+) exchange inhibitor. The spermicidal activity of miconazole, clotrimazole or loperamide due to elevation of intrasperm Ca(2+) and its synergism, therefore, has great potential for exploitation of these drugs as contact spermicides.

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Section: Introductionmentioning

confidence: 99%

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Gulati

Tiwary

Jain

et al. 2006

Journal of Pharmacy and Pharmacology

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“…Ca 2+ and pH may in turn control the phosphorylation state of functional proteins in the flagellar axoneme activated directly through cAMP and cAMP-dependent kinase [140,141]. Therefore, each step in the calcium-mediated regulatory process could serve as a potential target site for spermicidal action [142]. To interrupt these steps using inhibitors or blocking agents could provide insight into the mechanisms of spermicidal action.…”

Section: Major Possible Pathways By Which the Spermicides Work Changementioning

confidence: 99%

Insights of Spermicidal Research: An Update

Hazra¹

2014

JFIV Reprod Med Genet

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Spermicides came into existence as a method of contraception for over hundred years. Since then, investigations and developments in this field have led to more and more fruitful as well as promising results but still left enough scope for further studies. The titled article manifests a brief discussion on the development of spermicides from different natural and synthetic sources, a compilation of the promising molecules and even extracts and includes an outline of the basic physiology behind the bioactivity. Since spermicides are only one among several other methods of contraception adopted and practiced, an attempt has been made to probe the necessity and advantage of spermicides over other modes of contraception, emphasizing on the requirements and scope of future investigations in this field.

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“…In summary, while the potential contraceptive and microbicidal activity of acid buffers has been clearly demonstrated in vivo, it remains to be seen whether delivery systems can be developed capable of Calcium ions are involved in regulation of sperm motility. Decreased extracellular Ca 2+ and increased intracellular Ca 2+ are both detrimental to sperm motility [62]. CatSper1 is a gated cation channel that is essential for cAMP induced Ca 2+ influx into sperm [63].…”

Section: Regulation Of Ca 2+mentioning

confidence: 99%

The Search for a Topical Dual Action Spermicide/Microbicide

Hughes¹,

Griffith²,

Aitken

2007

CMC

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There is an urgent clinical need to research novel methods of fertility control that are also protective against sexually transmitted diseases (STDs) such as the human immunodeficiency virus (HIV) or Chlamydia. The most obvious way to generate such a dual-purpose contraceptive method would be to develop safe, effective spermicides that were also active against a wide range of pathogenic organisms. The currently available formulations such as nonoxynol-9, gramicidin and benzalkonium chloride are effective spermicides but are toxic to the vaginal epithelium and do not provide protection against STDs. Over 60 agents are in clinical trials as potentially safer topical spermicides and/or microbicides. Compounds that have reached this stage of development include acid buffers, detergents, dendrimers, non-nucleoside reverse transcriptase inhibitors and anionic polymers. In addition, a number of potential spermicides/microbicides are the subject of preclinical investigation, including beta-cyclodextrin, cyanovirin, porphyrins, cyclotriazadisulfonamides, dermaseptins, short-interfering RNA (siRNA) and HIV antibodies. The chemical principles underlying these disparate approaches and potential avenues for future investigation are discussed.

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Modulation of intrasperm Ca²⁺: A possible maneuver for spermicidal activity

Cited by 8 publications

References 167 publications

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Insights of Spermicidal Research: An Update

The Search for a Topical Dual Action Spermicide/Microbicide

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Modulation of intrasperm Ca2+: A possible maneuver for spermicidal activity

Cited by 8 publications

References 167 publications

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Intrasperm Ca2+ modulation and human ejaculated sperm viability: influence of miconazole, clotrimazole and loperamide

Insights of Spermicidal Research: An Update

The Search for a Topical Dual Action Spermicide/Microbicide

Contact Info

Product

Resources

About

Modulation of intrasperm Ca²⁺: A possible maneuver for spermicidal activity