• Biomolecules & Therapeutics
• /
• 제4권2호
• /
• pp.162-166
• /
• 1996

This study was done to investigate whether cholic acid derivatives have anti-stress activity and what is a cause of this anti-stress effect. Seven cholic acid derivatives (cholic acid, taurocholic acid, ursodeoxycholic acid, tauroursodeoxychoic acid, chenodeoxy cholic acid, dehydrocholic acid, hyodeoxycholic acid) were used, silymarin and valproic acid were used as positive controls. Stress was induced by restraint immobilization technique plus water immersion (24hrs) and adrenal weight, spleen weight, adrenal ascorbic acid, serum cholesterol, lactate dehydrogenase (LDH), alkaline phosphatase (ALP), adrenal cholesterol, glucose and corticosterone levels were measured as stress indicators. Most cholic acid derivatives markedly decreased the adrenal weight, and TUDCA and DHCA increased the spleen weight. The restraint stress induced increments in serum LDH, ALP and cholesterol were attenuated by most cholic acid derivatives. Cholic acid, taurocholic acid and tauroursodeoxycholic acid only increased the content of adrenal ascorbate. While valproic acid showed an inhibitory effect against stress, silymarin did not. Our findings suggest that most cholic acid derivatives have anti-stress effect and that their anti-stress effect is, in part, related to choleretic activity.

• Journal of Microbiology and Biotechnology
• /
• 제28권1호
• /
• pp.109-114
• /
• 2018

Coxsackievirus Type B3 (CVB3) is an enterovirus that belongs to the Picornaviridae and causes various diseases such as myocarditis and hand-foot-mouth disease. However, an effective antiviral drug is still not developed. In this study, we looked for potential inhibitors of CVB3 replication by examining the survival of CVB3-infected HeLa cells. We detected an antiviral effect by cholic acid and identified it as a candidate inhibitor of CVB3 replication. Cholic acid circulates in the liver and intestines, and it helps the digestion and absorption of lipids in the small intestine. HeLa cells were cultured in 12-well plates and treated with cholic acid (1 and $10{\mu}g/ml$) and $10^6PFU/ml$ of CVB3. After 16 h post-infection, the cells were lysed and subjected to western blot analysis and RT-PCR. The production of the viral capsid protein VP1 was dramatically decreased, and translation initiation factor eIF4G1 cleavage was significantly inhibited by treatment with $10{\mu}g/ml$ cholic acid. Moreover, cholic acid inhibited ERK signaling in CVB3-infected HeLa cells. RT-PCR showed that the amounts of the CVB3 RNA genome and mRNA for the ER stress-related transcription factor ATF4 were significantly reduced. These results showed that cholic acid strongly reduced ER stress and CVB3 proliferation. This compound can be developed as a safe natural therapeutic agent for enterovirus infections.

• 생명과학회지
• /
• 제19권12호
• /
• pp.1731-1736
• /
• 2009

최근의 연구에서 생쥐에 장기간 서구식 사료를 급여했을 때 내인성 SHP 단백질의 수준이 증가함을 보고하였다. 또한 HepG2 세포배양을 통한 실험에서, CDCA 처리가 내인성 SHP 단백질의 수준을 증가시킬 뿐만 아니라 외인성으로 발현된 flag-SHP의 분해율을 감소시켰다. 그리고 HepG2 세포를 ad-flag-SHP로 유전자 형질전환 시켰을 때, 담즙산에 의해 유도되어진 소장 FGF-19이 외인성으로 발현된 flag-SHP 단백질의 반감기를 증가시켰다. 그러나 cholic acid와 FGF-19에 의한 내인성 SHP 단백질의 발현수준과 분해율은 생쥐 또는 배양된 간암세포주에서 아직 명확히 이해되고 있지 않다. 이 연구는 cholic acid의 처리가 생쥐에서 내인성 SHP 단백질의 수준에 미치는 영향과, FGF-19이 HepG2 세포주에서 내인성 SHP 단백질의 분해율에 미치는 영향을 조사하였다. 정상적인 사료를 급여한 대조군 생쥐에서의 내인성 SHP 단백질 수준과 비교하여, 0.5%의 cholic acid를 첨가한 사료를 급여한 생쥐에서는 12시간과 24시간의 처리기간 동안에 내인성 SHP 단백질의 수준이 증가하였다. 배양된 인간 간암세포주인 HepG2에서 CDCA의 처리는 CDCA를 처리하지 않은 대조군 세포주와 비교하여 내인성 SHP 단백질의 분해율을 유의성 있게 변화시키지 않았다. 한편 외인성 ad-flag-SHP 단백질에 대한 이전의 연구와 일치하게, HepG2 세포에 cyclohexamide를 처리하였을 때 FGF-19는 내인성 SHP 단백질의 분해율을 현저히 감소시켰다. 이러한 결과는 담즙산과 FGF-19 모두 생쥐의 간과 HepG2 세포주에서 내인성 SHP 단백질의 수준을 증가시킴을 제시한다.

• Biomolecules & Therapeutics
• /
• 제6권3호
• /
• pp.232-241
• /
• 1998

This study was done to investigate whether cholic acid derivatives have anti-stress activity in various stress models. Two cholic acid derivatives, ursodeoxycholic acid (UDCA) and tauroursodeoxycholic acid (WDCA), were used. physical, psychological, chemical and environmental stress models were performed. Adrenal weight, serum glucose levels and ALP activity were elevated in restraint stress model, but this elevation was prevented by UDCA treatment. Moreover, UDCA and TUDCA inhibited exploratory and spontaneous movements in oscillation stress model. In alcohol-induced stress model, TUDCA improved rotarod performance. UDCA and TUDCA significantly reduced the involution of lymphoid organs and the increment of WBC counts in cold stress model. These findings suggest that choric acid derivatives have antistress effects in various stress models.

• 대한화학회지
• /
• 제34권2호
• /
• pp.215-217
• /
• 1990

• Bulletin of the Korean Chemical Society
• /
• 제20권2호
• /
• pp.179-186
• /
• 1999

Several cholic acid derivatives containing 1-3 trifluoroacetylbenzoyl (TFAB) moieties were synthesized using selective acetylations, hydrolysis and/or oxidation of cholic acid derivatives and tested as receptors for a carbonate ion through solvent extraction method. The compounds having two and three TFAB moieties exhibited enhanced binding affinities toward a carbonate ion in comparison with those with one TFAB croup and the extent of complex formation also depended on the position of TFAB group attached.

• 대한화학회지
• /
• 제50권6호
• /
• pp.515-517
• /
• 2006

• 한국자기공명학회논문지
• /
• 제20권2호
• /
• pp.41-45
• /
• 2016

Chemical investigation of a marine-derived fungus, Penicillium sp. 108YD020, resulted in the discovery of six bile acid derivatives, glycocholic acid (1), glycocholic acid methyl ester (2), cholic acid (3), glycochenodeoxycholic acid (4), glycodeoxycholic acid methyl ester (5), and cholic acid methyl ester (6). The structures of six bile acid derivatives 1-6 were determined by the detailed analysis of 1D, 2D NMR and LC-MS data, along with chemical methods and literature data analysis.

• 약학회지
• /
• 제22권4호
• /
• pp.193-200
• /
• 1978

Cholic, ursodesoxycholic, chenodesoxycholic, desoxycholic and hydesoxycholic acids were dissolved in the propylene glycol to make solution and then above solution of cholanic acids on bile secretion was investigated by injection those solutions into small intestine of rabbits and albino rats. The cholates in bile juice from rabbits injected with cholic acid were remarkably increased and therefore it exhibited a typical choleretic action. In view of pharmacological point, desoxycholic acid is considered as superior hydrocholeretic agent, and ursodesoxycholic and chenodesoxycholic acids have similar effect in decreasing order. However, the effect of bile secretion by hyodesoxycholic acid was almost negligible as that by propylene glycol administered. The cholate content in the bile juice from albino rat was increased by cholic and desoxycholic acids in decreasing order: i.e., they exhibited choleretic action. In the case of ursodesoxycholic and chenodesoxycholic acids, the concentration of cholate was slightly increased in bile juice from the rat, so that these cholates showed a weak choleretic action. While total output of bilirubin was increased by chenodesoxycholic acid, the other cholanic acid showed no effect in the rabbit.

• Bulletin of the Korean Chemical Society
• /
• 제27권5호
• /
• pp.739-743
• /
• 2006

Synthesis of cholic acid-based tripodal receptor (1) and its high chloride ion affinity in comparison with that of chenodeoxycholic acid (2) and lithocholic acid-based receptor (3) was achieved. Anion binding affinities of the receptors were evaluated $by\;^1H$ NMR and ITC titrations. Tripodal receptor 1 showed a selective affinity for $CI ^-$ over $Br ^-$, $I^-$, $H_2 PO _4\;^-$, and $CH _3 CO_2\;^-$. The selectivity of 1 for $CI ^-$ is about 3 times that of $Br ^-$, and 17 times that for $H_2 PO_4\;^-$.