Tideglusib, a prospective alternative to nonoxynol-9 contraceptive

Chen, Zhiting; Shu, Niyan; Wang, Yuzhu; Yang, Yiting; Shao, Zhiyu; Tian, Fang; Mao, Xia; Wang, Zhikai; Wang, Xin; Xing, Feng; Huang, Xianliang; Li, Weihua; Yu, Huan; Diao, Hua

doi:10.1016/j.conx.2019.100007

Cited by 5 publications

(3 citation statements)

References 32 publications

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“…Up to date, scientists have put forward many alternatives to replace N-9 in spermicides. For example, tideglusib, a protein from Ricinus communis, desgalactotigonin, and bivittoside D from Bohadschia vitiensis have been considered as potential spermicides in animal models ( Nithya et al 2012 , Chakraborty et al 2014 , Chen et al 2019 ). Combinations of N-9 and propranolol or polyvinylpyrrolidone both showed a complementary effect to achieve a complete cessation of sperm motility ( White et al 1995 , Fowler et al 2003 ).…”

Section: Discussionmentioning

confidence: 99%

Effects of nonoxynol-9 (N-9) on sperm functions: systematic review and meta-analysis

Zhao

et al. 2022

Reproduction and Fertility

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Objective: To summarize the currently available Phase I and II clinical trials of the effects of Nonoxynol-9 (N-9) on human sperm structure and functions. Methods: A systematic review and meta-analysis aiming to evaluate the spermicidal activity of N-9 on motility, was conducted in PubMed, EMBASE, and Cochrane databases by 10 March 2021. Counted numbers of progressive motile (PR) sperm in cervical mucus and the vanguard sperm penetration distances were analyzed. Other effects on sperm structures and physiological activities were reviewed as well. Results: In the pooled results, percentages or counted numbers of PR sperm decreased after the treatment of N-9. Vanguard sperm penetration distance was shortened in treated groups. N-9 has been confirmed to damage the structures of sperm, as well as other organelles like acrosome and mitochondria. The physiological activities such as generation of reactive oxygen species (ROS), superoxide dismutase (SOD) activity, acrosin activity, and hemizona binding were all inhibited in the reviewed studies. Conclusions: N-9 has several impacts on sperm owing to its potency in reducing sperm motility and cervical mucus penetration, as well as other functional competencies.

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Section: Discussionmentioning

confidence: 99%

Effects of nonoxynol-9 (N-9) on sperm functions: systematic review and meta-analysis

Zhao

et al. 2022

Reproduction and Fertility

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“…Thinning, by reducing tree density, induces changes in microclimate [11][12][13], resulting in elevated soil temperature and reduced soil moisture [14][15][16][17]. This alteration also affects soil properties by increasing compaction [18,19], soil bulk density, and reducing water-holding capacity 2 and nutrient levels [20,21].…”

Section: Introductionmentioning

confidence: 99%

Enhancing Forest Sustainability: A Comprehensive Exploration of Thinning Practices and their Effects on Soil Chemical and Biochemical Properties

Muscolo,

Oliva,

Mallamaci

et al. 2023

Preprint

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The adoption of sustainable forest management practices emerged as a contemporary imperative for forest biodiversity preservation, functional integrity, and mitigation of climate change. Within the spectrum of these practices, thinning is recognized as an environmentally sustainable strategy. The primary objective of thinning is the equitable redistribution of aboveground growth, diverting resources from younger trees to promote the accelerated development of more valuable specimens compared to unthinned forests. Thinning, while fostering aboveground changes, induces substantial alterations in soil chemical and biochemical properties. This review addresses the often-debated consequences of thinning on soil characteristics, focusing on the intricate interplay involving different thinning intensities and their impact on soil chemical and biochemical parameters. Specifically, the analysis delves into the modulation of organic carbon levels, microbial biomass, and enzymes crucial to the organic matter cycle. Two key aspects are scrutinized: firstly, the influence of thinning intensity and the temporal dimension post-thinning on soil properties; secondly, the comparative impact of thinning intensity versus the time elapsed from the thinning event on soil properties and associated biological processes. The findings underscore pivotal insights: a) temporal dynamics significantly affect soil organic matter across broadleaved (excluding beech), coniferous, and mixed forests, manifesting as early as 2-7 years post-thinning; b) thinning intensity, up to a threshold of 50%, enhances soil quality by augmenting organic carbon content, bolstering microbial communities, and amplifying associated enzyme activities. This review consolidates valuable information for forest managers, providing guidance to optimize natural processes in tandem with achieving specific management objectives. By illuminating the nuanced interactions between thinning practices and soil dynamics, this knowledge equips stakeholders to make informed decisions in the pursuit of sustainable forest management and ecological resilience.

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“…Based on the omics study of post-translational modification, the inhibitor was used to adjust the human sperm motility parameters in vitro. By screening molecules from the small compound library, it was found that the compounds have the ability to inhibit sperm motility [14]. Moreover, it was manifested that tideglusib had more efficient and lower cytotoxicity (mucosal damage) than N-9.…”

Section: Introductionmentioning

confidence: 99%

The Synthesis of 1,2,4-Thiadiazolidin-3,5-Dione Derivatives and Their Effects Against Human Sperm as Novel Spermostatic Compounds

Liu¹,

Chen

Deng

et al. 2019

BJSTR

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Manifesting much less mucosal irritating effect and higher efficiency than the currently used N-9, Tideglusib, a potent contraceptive candidate, exerts limited contraceptive efficacy in the water-soluble gels. Herein various new thiadiazolidine derivatives were synthesized and, for figuring out the essential groups that might be utilized to improve the in vivo efficacy of the lead, their sperm static/spermicidal effects were evaluated. By the analysis of the structure-activity relationship of tideglusib along with its derivatives, it was suggested that when the core ring was retained and the peripheral substituents were supplanted, the multiple derivatives have different levels of inhibition. And the naphthalene ring and benzene ring are non-essential.

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Tideglusib, a prospective alternative to nonoxynol-9 contraceptive

Cited by 5 publications

References 32 publications

Effects of nonoxynol-9 (N-9) on sperm functions: systematic review and meta-analysis

Effects of nonoxynol-9 (N-9) on sperm functions: systematic review and meta-analysis

Enhancing Forest Sustainability: A Comprehensive Exploration of Thinning Practices and their Effects on Soil Chemical and Biochemical Properties

The Synthesis of 1,2,4-Thiadiazolidin-3,5-Dione Derivatives and Their Effects Against Human Sperm as Novel Spermostatic Compounds

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