Indolyl Heterocycle Sperm Activators for Cryopreserved Boar Semen
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Solution Overview
Problem
Cryopreservation of boar sperm leads to decreased sperm motility, viability, and fertility due to temperature sensitivity, resulting in lower fertilization rates and economic losses for the pork industry, as existing extenders do not enhance sperm motility effectively.
Innovation Solution
The use of specific compounds, such as 5-(1H-indol-3-yl)-oxazole, -oxadiazole, and -furan derivatives, as sperm activators to enhance sperm motility and fertility in boar semen, even after cryopreservation or storage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of stationary object
If cryopreservation is used to store boar sperm for extended periods, then storage duration is improved, but sperm motility and viability deteriorate
Solution Approach 1:
The patent applies preliminary action by adding specific compounds (such as caffeine, theophylline, or other phosphodiesterase inhibitors) to the sperm sample before storage or before use. These compounds are pre-introduced to maintain sperm motility and viability throughout the storage period, counteracting the damaging effects of cryopreservation beforehand rather than attempting to repair damage after storage.
Solution Approach 2:
The patent uses chemical compounds as intermediaries between the sperm and the cryopreservation process. These compounds (e.g., phosphodiesterase inhibitors) act as mediators that protect sperm cells from the harmful effects of freezing and storage, maintaining intracellular cAMP levels and preventing motility loss without directly altering the sperm structure or requiring complex equipment modifications.
2Adaptability or versatility
If cryopreservation is used to enable sperm transport and storage, then adaptability is improved, but sperm fertility deteriorates
Solution Approach 1:
The patent applies parameter changes by modifying the biochemical environment of the sperm through the addition of specific compounds. These compounds change the physiological parameters of sperm (such as intracellular cAMP concentration, membrane fluidity, and metabolic activity) to maintain fertility despite the cryopreservation process. The compounds adjust the sperm's biochemical state to be more resilient to freezing and storage conditions.
3Duration of action of stationary object
If extenders are added to prolong semen half-life, then storage duration is improved, but sperm motility enhancement is not achieved
Solution Approach 1:
The patent effectively copies or replicates the natural physiological conditions that maintain sperm motility by introducing compounds that mimic endogenous signaling molecules (such as cAMP elevating agents). Instead of relying solely on extenders that merely preserve sperm, these compounds actively replicate the biochemical signals necessary for maintaining and even enhancing motility during storage, going beyond simple preservation to active motility support.
Data Source
AI summary
The invention relates to the use of compounds of formula (I), stereoisomers, and physiologicaily tolerable salts thereof, to enhance the motility of sperm obtained from a non-human mammal: wherein in formula I: X is —NR′— (in which R′ is H or C1-3 alkyl. e.g. —CH3), —O—, —S— or —CH2—; Y is —S—, —O—, —NR″— (in which R″ is H or C1-3 alkyl, e.g. —CH3), or —CH2—; Z1 and Z2 are independently selected from N and CH; R1 to R3 are independently selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, —OH, —CN, —NO2 and —NR12R13; R4 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, or —OH; R5 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, or C1-6 haloalkyl; R6 and R7 are independently selected from hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, —OH, —CN, —NO2 and —NR12R13; R8 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, —CN, —NO2 or —NR12R13; R9 is hydrogen or C1-4 alkyl; R10 and R11 are independently selected from hydrogen and C1-3 alkyl; or R10 and R11, together with the intervening —O— and ring atoms, are joined to form a dioxolane ring; and R12 and R13 are independently selected from H and C1-3 alkyl. The compounds find particular use in animal husbandry to increase the rate of fertilization in artificial insemination of livestock, especially pigs. They can also be used to prepare, pre-treat or store semen for use in artificial insemination procedures.