• 대한화학회지
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• 제57권2호
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• pp.227-233
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• 2013

A series of newer substituted-imidazolidine derivatives 3a-k were synthesized and assayed in vivo to investigate their anti-inflammatory, analgesic and antiulcer activity. The results of biological evaluation revealed that the three compounds, 4-[1,3-bis(4-hydroxy-3-methoxybenzyl)-2-imidazolidinyl]phenyldiethylamine (3g), 4-[1,3-bis(3-Ethoxy-4-hydroxybenzyl)-2-imidazolidinyl] phenyldiethylamine (3h) and 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-diethylbenzenamine (3j) were good in their anti-inflammatory and analgesic actions. Additionally these derivatives showed superior GI safety profile as compared to that of the standard drug in terms of low severity index. The results are statistically treated for its significance.

• 셀메드
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• 제6권2호
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• pp.11.1-11.7
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• 2016

The aimed of the presence study was to determine the antiulcer potential of virgin coconut oil (VCO), either extracted by wet process (VCO_A) or fermentation process (VCO_B), and to compare their effectiveness against the copra oil (CO) using the HCl/ethanol-induced gastric ulcer model. Earlier, the oils underwent chemical analysis to determine the free fatty acids composition, physicochemical properties and anti-oxidant capability. In the antiulcer study, rats (n=6) were pre-treated orally for 7 consecutive days with distilled water (vehicle), 100 mg/kg ranitidine (positive group) or the respective oils (10, 50, and 100% concentration). One hour after the last test solutions administration on Day 7^th, the animals were subjected to the gastric ulcer assay. Macroscopic and microscopic analyses were performed on the collected rat's stomachs. From the results obtained, the chemical analysis revealed i) the presence of high content of lauric acid followed by myristic acid and palmitic acid in all oils and; ii) the significant (^*p< 0.05) different in anisidine- and peroxide-value, percentage of free fatty acid, total phenolic content and total antioxidant activity among the oils. The animal study demonstrated that all oil possess significant (^*p< 0.05) antiulcer activity with VCO_B being the most effective oil followed by VCO_A and CO. The macroscopic observations were supported by the microscopic findings. Interestingly, all oils were more effective than 100 mg/kg ranitidine (reference drug). In conclusion, coconut oils exert remarkable antiulcer activity depending on their methods of extraction, possibly via the modulation of its antioxidant and anti-inflammatory activity.

• 한국식품과학회지
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• 제31권3호
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• pp.764-770
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• 1999

41종의 약용식물을 열수추출하여 위궤양 원인균으로 보고된 Helicobacter pylori에 대해 항균활성을 탐색하였다. 2-fold dilution 방법에 의해서는 백련초, 어성초, 방기, 황련은 100 ppm이하, 백두옹, 연교, 종대황, 소엽은 200 ppm 이하, 사간, 우방자, 결명자, 귤피, 희침, 소목은 300 ppm 이하와 농도에서 H. pylori에 대해 항균활성을 나타냈다. 이중 3가지 추출물만이 disc 방법을 통해 항균활성이 재확인되었으며, 소목, 황련, 소엽의 순으로 강한 항균활성을 나타냈다. 항균활성이 확인된 3가지 추출물을 chloroform, ethyl acetate, butanol로 순차 분획하여 H. pylori에 대한 항균활성을 확인하였다. 소목의 경우는 ethyl acetate 분획물에서, 소엽의 경우는 butanol 분획물에서, 황련의 경우는 butanol과 chloroform 분획물에서 가장 강한 항균활성을 나타내었다. 추출물의 분획에 따른 항균활성의 상승효과는 모든 추출물에서 확인할 수 있었다. H. pylori의 crude-urease를 분리하여 urea R broth에서 흡광도와 pH를 조사한 결과, 반응 2시간 후 pH가 8.15까지, 560 nm에서의 흡광도는 1.7까지 증가하는 것으로 나타났다. H. pylori의 urease 활성은 소목, 소엽, 황련에 의해 80%이상 억제되었으며, 이중 소목은 urease 활성을 95%이상 억제시켰다.

• 동의생리병리학회지
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• 제21권6호
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• pp.1549-1554
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• 2007

To verify the effects of JAUN-1, which is a water-extracted herbal mixture, on gastroenteric disorders induced by 0.1 percent of iodoacetamide (IA) in rats. We divided four groups, $Na{\&quot;{\i}}ve$ + Distilled Water (DW), 0.1% IA + DW, 0.1% IA + Proton pump inhibitor (Lansoprazole, 5 mg/kg) and 0.1% IA + Herbal mixture (JAUN-1, 50mg/kg) and performed following experimental methods to confirm its advantageous effects against ulcerogenic stomach in rats induced by 0.1% IA; cell cytotoxicity, analysis of lesions score, Hematoxylin & Eosin (H&E) stain, RT-PCR for ${\beta}-actin$, COX-1 and COX-2 and evaluation of intestinal prokinetic activity. No cytotoxicity was elucidated at the concentration of 1, 5, 10, 50, 100, $500\;{\mu}g/ml$ and 1mg/ml JAUN-1 through MTT Assay using by human stomach epithelial AGS cells, respectively. In addition, the JAUN-1 treated group and the lansoprazole treated group significantly decreased in lesions score compared to the DW treated group in the gastritis induced rat model, and results of immunohistochemistry by H&E staining showed that histological recovery in Proton Pump Inhibitor (PPI) and JAUN-1 treated groups rather than the DW administrated group. Another outcome was that ${\beta}-actin$ relative COX-2 expression level was significantly promoted in the DW treated group while ${\beta}-actin$ relative COX-1 expression level was no meaningful change in this rat model. Finally, intestinal prokinetic activity was recovered from low level of prokinetic activity due to 0.1% IA induced gastritis to the similar level of Normal group. These results suggested that JAUN-1 may have beneficial effects against 0.1% IA-induced gastritis rat model through decreasing lesions score, histological recovery, ${\beta}-actin$ relative COX-1, 2 expression level and prokinetic activity.

• 한국식품과학회지
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• 제35권6호
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• pp.1182-1187
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• 2003

위질환 원인균으로 알려진 H. pylori 생육을 저해하는 물질을 탐색하기 위하여 호장근 메탄을 추출물 및 분획물을 이용하여 H. pylori에 대한 항균실험 및 urease 활성 억제효과를 검토하였다. 호장근 메탄올 추출물의 항균실험을 실시한 결과 5mg/cylinder의 농도일 때 inhibition zone이 17mm 정도로 높은 항균성을 가지는 것으로 나타났으며, 분획물의 경우 1mg/cylinder의 농도일 때 hexane 분획과 chloroform 분획물에서 각각 24mm, 17mm로 높은 항균 활성을 보였다. H. pylori의 crude urease를 분리하여 urea broth에서 흡광도와 pH를 조사한 결과, 반응 2시간 후 pH가 8.35까지 증가하였고 $O.D._{560nm}$에서의 흡광도는 0.859까지 증가하였다. 호장근에 의한 urease 활성억제는 호장근의 메탄올 추출물의 농도가 0.5 mg/mL에서 대조구에 비해 35% 억제효과를 보였고, 2 mg/mL에서는 85% 이상으로 매우 높은 억제활성을 보였다. 또한. 각 분획물의 저해 효과를 10배 농도의 메탄올추출물과 비교하였을 때. $20\;{\mu}g/mL$의 농도에서 water 분획을 제외한 모든 분획물들이 반응 2시간 후 $30{\sim}40%$의 저해를 보여 $200\;{\mu}g/mL$ 농도의 메탄올추출물이 20% 이하의 저해를 보인 것과 비교해 높은 활성을 보였다. 호장근 메탄올 추출물 처리에 의한 H. pylori의 형태변화를 조사하기 위하여 주사 및 투과전자 현미경으로 균의 형태를 관찰하였다. 주사전자 현미경 관찰 시 대조구는 균체 표면이 깨끗하고 완전한 구형을 이루고 있는 반면, 호장근 처리구는 균체 표층 구조가 심하게 허물고 떨어져 나간 것을 볼 수 있었고 또한 세포가 팽대하였고 일부 세포벽은 완전히 파괴되어 균체내 성분이 모두 유출되어 균 형태가 없어져 버린 것도 관찰되었다.

• Archives of Pharmacal Research
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• 제29권7호
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• pp.591-597
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• 2006

Aerial parts of Artemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor $(NF)-{\kappa}B$ inhibitor from A. asiatica by activity-guided fractionation. Artemisolide inhibited $NF-{\kappa}B$ transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $5.8\;{\mu}M$. The compound was also effective in blocking $NF-{\kappa}B$ transcriptional activities elicited by the expression vector encoding the $NF-{\kappa}B$ p65 or p50 subunits bypassing the inhibitory kB degradation signaling $NF-{\kappa}B$ activation. The macrophages markedly increased their $PGE_2$ and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced $PGE_2$ and NO production with $IC_{50}$ values of $8.7\;{\mu}M$ and $6.4\;{\mu}M$, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a $NF-{\kappa}B$ inhibitor that attenuates LPS-induced production of $PGE_2$ or NO via down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine, A. asiatica.