The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring syntho...The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring synthons(15 and 19) respectively. The enantioselective synthesis of substituted bicyclic hexanes structure A ring synthons, started from all cis 3,5 dihydroxy 4 ethyl 1 (methoxycarbonyl)cyclohexane via lipase catalyzd asymmetrization, was demonstrated.展开更多
1,25-dihydroxyvitamin D3 （VD3）, an active form of Vitamin D, is photosynthesized in the skin of vertebrates in response to solar ultraviolet B radiation （UV-B）. VD3 deficiency can cause health problems such as imm...1,25-dihydroxyvitamin D3 （VD3）, an active form of Vitamin D, is photosynthesized in the skin of vertebrates in response to solar ultraviolet B radiation （UV-B）. VD3 deficiency can cause health problems such as immune disease, metabolic disease, and bone disorders. It has also been demonstrated that VD3 is involved in reproductive functions. Female sex hormones such as estrogen and progesterone are biosynthesized mainly in ovarian granulosa cells as the ovarian follicle develops. The functions of sex hormones include regulation of the estrus cycle and puberty as well as maintenance of pregnancy in females. In this study, we isolated granulosa cells from porcine ovaries and cultured them for experiments. To examine the effects of VD3 on ovarian granulosa cells, the mRNA and protein levels of genes were analyzed by Real-time PCR and Western blotting assay. Production of progesterone from granulosa cells was also measured by ELISA assay. As a result, transcriptional and translational regulation of progesterone biosynthesis-related genes in granulosa cells was significantly altered by VD3. Furthermore, progesterone concen- trations in porcine granulosa cell-cultured media decreased in response to VD3. These results show that VD3 was a strong regulator of sex steroid hormone production in porcine granulosa cells, suggesting that vitamin D deficiency may result in inappropriate sexual development of industrial animals and eventually economic loss.展开更多
Objective:To evaluate the development of ovarian follicles in female albino rats following vitamin D3 supplementation.Methods:Eighteen prepubertal female albino rats,aged 3-4 weeks,weighing(70.25±9.16)g,were assi...Objective:To evaluate the development of ovarian follicles in female albino rats following vitamin D3 supplementation.Methods:Eighteen prepubertal female albino rats,aged 3-4 weeks,weighing(70.25±9.16)g,were assigned to three groups(n=6 in each group).Group A was treated with 5.00 mL/kg of distilled water and served as the control group,group B was treated with 0.025 mg/kg of vitamin D3 dissolved in distilled water,and group C was treated with 0.125 mg/kg of vitamin D3 dissolved in distilled water.All treatments were administered orally,twice weekly for 28 days.Blood and ovaries were harvested under anaesthesia.Serum vitamin D3 levels were determined by using spectrophotometric method.Ovaries were processed for histology and every10th hematoxylin and eosin stained-section was selected for histomorphometry.The number of follicles at each developmental stage was estimated.Results:Both 0.025 mg/kg and 0.125 mg/kg of vitamin D3 significantly increased serum concentrations of vitamin D3 and calcium(P<0.05),but did not alter inorganic phosphorus concentration(P>0.05).The control group had fewer growing follicles(primary,secondary and antral follicles)and more non-growing follicles(primordial and atretic follicles)when compared with the vitamin D3-supplemented groups(P<0.05).Vitamin D3 at 0.025 mg/kg significantly increased antral follicles and corpora lutea counts(P<0.05).Vitamin D3 at 0.125 mg/kg significantly increased total,primordial and atretic follicles counts(P<0.05),but significantly decreased primary,secondary,antral follicles count,ovarian weight,relative ovarian weight,and ovarian surface area when compared with the control group and rats treated with 0.025 mg/kg of vitamin D3(P<0.05).Conclusions:Vitamin D3 supplementation at 0.025 mg/kg can enhance optimal ovarian follicle recruitment and development in female rats.展开更多
A silica gel-anchored photosensitizer was synthesized with anthracene as sensitizer moiety. The photoisomerization of tachysterol to previtamin D3 was carried out with this heterogeneous photosensitizer in ethanol. T...A silica gel-anchored photosensitizer was synthesized with anthracene as sensitizer moiety. The photoisomerization of tachysterol to previtamin D3 was carried out with this heterogeneous photosensitizer in ethanol. The experiment results demonstrate that this solid phase photosensitizer is efficient for the photoisomerization and can be simply separated from the reaction mixture by filtration.展开更多
The impact of various vitamin D3(VD3)doses(1.0,2.5,or 5 mg/kg,s.c.)in mitigating the negative consequences of chronic unpredictable mild stress(CUMS)was investigated.Adult female rats with long-term estrogen deficienc...The impact of various vitamin D3(VD3)doses(1.0,2.5,or 5 mg/kg,s.c.)in mitigating the negative consequences of chronic unpredictable mild stress(CUMS)was investigated.Adult female rats with long-term estrogen deficiency were assessed using the sucrose preference test(SPT),the elevated plus-maze(EPM),the light/dark test(LDT),and the open-field test(OFT)to measure anhedonia-like and anxiety-like behavior.The corticosterone(CS)and adrenocorticotrophic hormone(ACTH)concentrations in blood serum and the brain-derived neurotrophic factor(BDNF)expression in the hippocampus of long-term ovariectomized(OVX)rats were measured by ELISA kits and/or western blotting.Treatment with VD3(5.0 mg/kg),similarly to fluoxetine(10.0 mg/kg),significantly reduced the anhedonia profile in the SPT and anxiety-like behavior in the EPM and LDT,and CS and ACTH levels in blood serum.It also elevated BDNF levels in the hippocampus of long-term OVX/CUMS compared to OVX/CUMS/solvent rats.Thus,these findings suggest that VD3(5.0 mg/kg)administration might attenuate the anxiety-like profile in long-term OVX adult rats subjected to the CUMS.This might occur via activation of the BDNF signaling pathway in the hippocampus and via restoration of CS and ACTH levels in blood serum.展开更多
Two modes of heterogeneous photoisomerization of trans-vitamin D3 to cis-vitamin D3 are described. The occurrence of isomerization on the substrate bounded to the polymeric support gives us the possibility in successi...Two modes of heterogeneous photoisomerization of trans-vitamin D3 to cis-vitamin D3 are described. The occurrence of isomerization on the substrate bounded to the polymeric support gives us the possibility in succession synthesis of 1α-hydroxyvitamin D3. The polymer-bound anthracene can sensitize isomerization of trans-vitamin D3 to cis-vitamin D3 efficiently and ease the separation process.展开更多
A solid-phase synthesis of 1α-hydroxylation of 5,6-trans-vitamin D3 8 is described.The solid phase resin acts as a special protecting group, which gives a higher stereoselectivity in oxidation step than classical pro...A solid-phase synthesis of 1α-hydroxylation of 5,6-trans-vitamin D3 8 is described.The solid phase resin acts as a special protecting group, which gives a higher stereoselectivity in oxidation step than classical protecting groups. The stereochemistry control is favored by using high crosslinkage polymer support in a poor solvent. This work may be of benefit to the synthesis of vitamin D system.展开更多
The photoisomerization of provitamin D-3 is carrried out in silica gel-hexane matrix, ethanol and hexane. The results show that in silica gel-hexane matrix and ethanol, the desired product of provitamin D-3 and vitami...The photoisomerization of provitamin D-3 is carrried out in silica gel-hexane matrix, ethanol and hexane. The results show that in silica gel-hexane matrix and ethanol, the desired product of provitamin D-3 and vitamin D-3 can be obtained in high yield, while the undesirable byproducts are greatly limited.展开更多
A convenient and highly efficient conversion of 1β-OH-trans-vitamin D3, a main byproduct in synthesis of active vitamin D3, to 1α-OH-trans-vitamin D3 is reported. The conversion could be accomplished in 1 minute wit...A convenient and highly efficient conversion of 1β-OH-trans-vitamin D3, a main byproduct in synthesis of active vitamin D3, to 1α-OH-trans-vitamin D3 is reported. The conversion could be accomplished in 1 minute with 90% yield.展开更多
文摘The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring synthons(15 and 19) respectively. The enantioselective synthesis of substituted bicyclic hexanes structure A ring synthons, started from all cis 3,5 dihydroxy 4 ethyl 1 (methoxycarbonyl)cyclohexane via lipase catalyzd asymmetrization, was demonstrated.
基金supported by a 2-Year Research Grant of Pusan National University
文摘1,25-dihydroxyvitamin D3 （VD3）, an active form of Vitamin D, is photosynthesized in the skin of vertebrates in response to solar ultraviolet B radiation （UV-B）. VD3 deficiency can cause health problems such as immune disease, metabolic disease, and bone disorders. It has also been demonstrated that VD3 is involved in reproductive functions. Female sex hormones such as estrogen and progesterone are biosynthesized mainly in ovarian granulosa cells as the ovarian follicle develops. The functions of sex hormones include regulation of the estrus cycle and puberty as well as maintenance of pregnancy in females. In this study, we isolated granulosa cells from porcine ovaries and cultured them for experiments. To examine the effects of VD3 on ovarian granulosa cells, the mRNA and protein levels of genes were analyzed by Real-time PCR and Western blotting assay. Production of progesterone from granulosa cells was also measured by ELISA assay. As a result, transcriptional and translational regulation of progesterone biosynthesis-related genes in granulosa cells was significantly altered by VD3. Furthermore, progesterone concen- trations in porcine granulosa cell-cultured media decreased in response to VD3. These results show that VD3 was a strong regulator of sex steroid hormone production in porcine granulosa cells, suggesting that vitamin D deficiency may result in inappropriate sexual development of industrial animals and eventually economic loss.
基金This research was supported by TETFUND-IBR and TETFUNDAST&D with reference number UN/VC/T/19/N.2.
文摘Objective:To evaluate the development of ovarian follicles in female albino rats following vitamin D3 supplementation.Methods:Eighteen prepubertal female albino rats,aged 3-4 weeks,weighing(70.25±9.16)g,were assigned to three groups(n=6 in each group).Group A was treated with 5.00 mL/kg of distilled water and served as the control group,group B was treated with 0.025 mg/kg of vitamin D3 dissolved in distilled water,and group C was treated with 0.125 mg/kg of vitamin D3 dissolved in distilled water.All treatments were administered orally,twice weekly for 28 days.Blood and ovaries were harvested under anaesthesia.Serum vitamin D3 levels were determined by using spectrophotometric method.Ovaries were processed for histology and every10th hematoxylin and eosin stained-section was selected for histomorphometry.The number of follicles at each developmental stage was estimated.Results:Both 0.025 mg/kg and 0.125 mg/kg of vitamin D3 significantly increased serum concentrations of vitamin D3 and calcium(P<0.05),but did not alter inorganic phosphorus concentration(P>0.05).The control group had fewer growing follicles(primary,secondary and antral follicles)and more non-growing follicles(primordial and atretic follicles)when compared with the vitamin D3-supplemented groups(P<0.05).Vitamin D3 at 0.025 mg/kg significantly increased antral follicles and corpora lutea counts(P<0.05).Vitamin D3 at 0.125 mg/kg significantly increased total,primordial and atretic follicles counts(P<0.05),but significantly decreased primary,secondary,antral follicles count,ovarian weight,relative ovarian weight,and ovarian surface area when compared with the control group and rats treated with 0.025 mg/kg of vitamin D3(P<0.05).Conclusions:Vitamin D3 supplementation at 0.025 mg/kg can enhance optimal ovarian follicle recruitment and development in female rats.
文摘A silica gel-anchored photosensitizer was synthesized with anthracene as sensitizer moiety. The photoisomerization of tachysterol to previtamin D3 was carried out with this heterogeneous photosensitizer in ethanol. The experiment results demonstrate that this solid phase photosensitizer is efficient for the photoisomerization and can be simply separated from the reaction mixture by filtration.
基金funded by the Russian Science Foundation(RSF)(research project N°16-15-10053(extension)).
文摘The impact of various vitamin D3(VD3)doses(1.0,2.5,or 5 mg/kg,s.c.)in mitigating the negative consequences of chronic unpredictable mild stress(CUMS)was investigated.Adult female rats with long-term estrogen deficiency were assessed using the sucrose preference test(SPT),the elevated plus-maze(EPM),the light/dark test(LDT),and the open-field test(OFT)to measure anhedonia-like and anxiety-like behavior.The corticosterone(CS)and adrenocorticotrophic hormone(ACTH)concentrations in blood serum and the brain-derived neurotrophic factor(BDNF)expression in the hippocampus of long-term ovariectomized(OVX)rats were measured by ELISA kits and/or western blotting.Treatment with VD3(5.0 mg/kg),similarly to fluoxetine(10.0 mg/kg),significantly reduced the anhedonia profile in the SPT and anxiety-like behavior in the EPM and LDT,and CS and ACTH levels in blood serum.It also elevated BDNF levels in the hippocampus of long-term OVX/CUMS compared to OVX/CUMS/solvent rats.Thus,these findings suggest that VD3(5.0 mg/kg)administration might attenuate the anxiety-like profile in long-term OVX adult rats subjected to the CUMS.This might occur via activation of the BDNF signaling pathway in the hippocampus and via restoration of CS and ACTH levels in blood serum.
基金This work was supported by the Major State Basic Research Development Program,Grant No.G2000078100the National Natural Science Foundation of China,No.20172059 and Chinese Academy of Sciences.
文摘Two modes of heterogeneous photoisomerization of trans-vitamin D3 to cis-vitamin D3 are described. The occurrence of isomerization on the substrate bounded to the polymeric support gives us the possibility in succession synthesis of 1α-hydroxyvitamin D3. The polymer-bound anthracene can sensitize isomerization of trans-vitamin D3 to cis-vitamin D3 efficiently and ease the separation process.
基金supported by the Major State Basic Research Development Program(Grant No.F2000078100)the National Natural Science Foundation of China(No.20172059)the Found of Chinese Academy of Sciences.
文摘A solid-phase synthesis of 1α-hydroxylation of 5,6-trans-vitamin D3 8 is described.The solid phase resin acts as a special protecting group, which gives a higher stereoselectivity in oxidation step than classical protecting groups. The stereochemistry control is favored by using high crosslinkage polymer support in a poor solvent. This work may be of benefit to the synthesis of vitamin D system.
基金This work was supported by the National Natural Science Foundation of China, No. 29971031 and the Chinese Academy of Sciences.
文摘The photoisomerization of provitamin D-3 is carrried out in silica gel-hexane matrix, ethanol and hexane. The results show that in silica gel-hexane matrix and ethanol, the desired product of provitamin D-3 and vitamin D-3 can be obtained in high yield, while the undesirable byproducts are greatly limited.
基金to the Major State Basic Research Development Program,Grant No.F2000078100the National Natural Science Foundation of China(No.20172059)and Chinese Academy of Sciences.
文摘A convenient and highly efficient conversion of 1β-OH-trans-vitamin D3, a main byproduct in synthesis of active vitamin D3, to 1α-OH-trans-vitamin D3 is reported. The conversion could be accomplished in 1 minute with 90% yield.
