• Journal of Oral Medicine and Pain
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• 제24권2호
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• pp.137-143
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• 1999

Aucubin, the natural product, which is isolated from Aucuba japonica, has a variety of pharmacological effects such as liver-protective function, inhibition of liver RNA and protein biosynthesis, hypotensive activity and antimicrobial effect, etc. This study was performed to investigate the effects of iridoid compounds on wound healing. The author prepared 0.1% aucubin solution and 0.1% aucubin ointment as an active form, aucubigenin to which aucubin was converted by ${\beta}$-glucosidase. Artificial surgical wound was made on either 1cm lateral side of the dorsal midline along the axis of spine of Sprague-Dawley rats under sterile technique. Application of 0.1% aucubin solution or 0.1% aucubin ointment to surgical wound was done daily. Light microscopic examination was performed on the postsurgical 3 days, 5 days, and 9 days. The 0.1% aucubin solution group epithelialized earlier than the control group and the fibrosis of granulation tissue of both aucubin groups were more prominent than the control group. Collectively, this study suggests the possibility of aucubin as a topical agent. Further research should be performed on the mechanism of aucubin on wound healing and proper formulation for effective topical agents.

• Journal of Pharmaceutical Investigation
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• 제25권3호
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• pp.239-247
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• 1995

The physico-chemical stability of aucubin, a hepatoprotective iridoid glucoside, in buffered aqueous solutions was studied using a stability-indicating reversed-phase high performance liquid chromatography. The degradation of aucubin followed the pseudo-first-order kinetics. In strong acidic regions, aucubin was rapidly degraded by the specific acid catalysis, forming dark brown precipitates. From the rate-pH profiles, it was found that aucubin was most stable at the pH of about 10. From the temperature dependence of degradation, activation energies for aucubin at pH 2.1 and 4.9 were calculated to be 22.0 and 24.3 kcal/mole, respectively. The shelf-life $(t_{90%})$ for aucubin at pH 9.07 and $20^{\circ}C$ was predicted to be about 603 days. A higher ionic strength accelerated the degradation of aucubin at pH 4.01. The effect of metal ions on the degradation rate of aucubin at pH 7.16 was in the rank order of $Cu^{2+}\;>\;Fe^{3+}\;>\;Co^{2+}\;>\;Fe^{2+}\;>\;Mg^{2+}$. On the other hand, $Mn^{2+}\;and\;Ba^{2+}$ slowed the degradation rate.

• 약학회지
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• 제28권1호
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• pp.35-48
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• 1984

우리나라 사람들에게는 유달리 높은 간염 발병률이 나타나고 있고 더우기 바이러스성 간염의 경우 풍토병 내지 전염병이라고 할 정도의 양상을 띠고 있다. 현재까지는 이러한 간질환에 적절한 치료약이 없는 점을 감안하여 저자들은 생약으로 부터 간질환에 유효한 성분을 분리하여 치료약으로 사용할 수 있도록 하기위하여 집중적인 연구를 지난 5년간 계속하여 왔다. 연구의 내용은 동서양의 고전및 연구보문을 조사하여 간보호 및 치료학으로 사용한 생약에 관한 문헌적 조사, 이들 생약중 채집 및 구입이 가능한 식물을 구하여 생약엑기스 제조, 이들 엑기스를 간염 동물 모델의 하나인 $CCl_{4}$로 유발시킨 간독성에 대한 보호작용의 검색, 보호작용을 나타내는 생약중에서 자원적 측면을 고려하여 국내에서 많이 생산되는 차전자(Plantago asiatica seeds)를 선택하였고, 차전자로 부터 간보호 작용을 나타내는 유효성분으로 iridoid 계열물질인 aucubin을 분리하였다. 그러나 aucubin이 차전자에 소량 밖에 없으므로 aucubin이 다량 함유된 식나무(Aucuba japonica)로 aucubin 추출자료생약을 바꾼후 aucubin의 간보호 작용을 간염 동물모델인, $CCl_{4}$ D-galactosamine 및 $\alpha$-amanitin등으로 유발시킨 간독성에 대한 보호작용을 보여 주었기 때문에, 이러한 간보호작용의 기전을 규명하는 연구를 진행하였고, 다음은 aucubin 자체의 급성 독성 및 기타 독성 유발여부를 밝히는 연구 등으로 요약 될 수 있다.

• 약학회지
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• 제37권4호
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• pp.383-388
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• 1993

Pharmacokinetics of aucubin, an irdoid glucoside, was compared in rats of experimental hepatic failure(EHF). EHF was induced by CCI$_{4}$ or D-galactosamine pretreatment. This work was designed to find out any differences in the pharmacokinetics of aucubin that may explain the different protective effect of aucubin on CCI$_{4}$- and galactosamine-induced EHF : aucubin reportedly protected CCI$_{4}$-inducing hepatotoxicity effectively, but did not for galactosamine-hepatotoxicity. EHF was induced by intraperitoneal injection Of CCI$_{4}$(0.9ml/kg) or galactosamine(250 mg/kg) to Wistar rats 24 hr before the pharmacokinetic study. The rats were fasted during the 24 hr. Aucubin was iv injected at a dose of 15 mg/kg and the plasma aucubin was assayed by HPLC. There were no significant differences in the pathophysiologies(body weight, liver weight, GTP, hematocrit, blood cell distrbution and plasma protein binding of aucubin) between the two EHF models except GOP which was significantly (p<0.05) higher in CCI$_{4}$-than in galactosamine-EHF. On the other hand, pharmacokinetics of aucubin such as total cleatance(CL$_{t}$), distribution volume at steady-state(Vd$_{ss}$), and mean residence time(MRT) differed significantly(p<0.05) between the models : for example, CL$_{t}$ was increased two fold by CCI$_{4}$, but not by galaclosamine ; Vd$_{ss}$, in galactosamine-EHF was higher than that in CCI$_{4}$-EHF ; MRT was decreased by CCI$_{4}$, but increased conversely by galactosamine. The increase of CL$_{t}$(and decrease of MRT) in rats of CCI$_{4}$-EHF was contrary to the general expectation for the hepatic failure : most of the hepatic failures have been known to decrease CL$_{t}$ of the administered drugs. Whether the difference in the pharmacokinetics is responsible for the different protective effect of aucubin against the two EHF models is of interest. However, much more studies on biliary excretion, urinary excretion, and hepatic uptake in cellular level should be preceded before any conclusions are made on the role of different pharmacokinetics on the different pharmacology of aucubin.

• Restorative Dentistry and Endodontics
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• 제24권4호
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• pp.554-559
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• 1999

Aucubin, an iridoid glucoside isolated from Aucuba japonica, has pharmacological effects such as antimicrobial effect, liver protective function and inhibition of liver RNA and protein biosynthesis, etc. This study was performed to observe the effect of aucubin on the pulp tissue after pulpotomy. Aucubin was converted to aucubinogenin as an active form by ${\beta}$-glucosidase. In 3 Mongrel dogs, the pulps were mechanically exposed with a sterile round bur and excised with sterile excavator. After bleeding control, aucubin was applied on remaining pulp tissues and then they were sealed with IRM in experimental group. In control group, $Ca(OH)_2$ powder was applied on remaining pulp tissues and then they were sealed with IRM. After interval of 1 and 12 weeks, the dogs were sacrificed. The teeth were prepared for histologic evaluation and examined by light microscope. Aucubin 1 week group showed that mild inflammation and vascular congestion in most of the specimen. More various degree of inflammation was found in experimental group than in control group. Premature calcified mass were found in the both 1 weeks groups. Continuous well-formed dentin bridge was found in both 12 weeks groups. Collectively, this study suggests that the possibility of aucubin as a medicament after pulpotomy.

• Food Science and Biotechnology
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• 제18권2호
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• pp.475-480
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• 2009

Ultraviolet B (UVB) radiation provokes the generation of reactive oxygen species (ROS) in the cells and skin, which induce oxidative stress in the exposed cells, leading to photoaging and cancer. Using the human keratinocytes HaCaT cell line, we investigated the photoprotective effects of aucubin isolated from Eucommia ulmoides. Pretreatment with aucubin markedly suppressed UVB-induced oxidative stress, which manifests as a decrease in intracellular lipid peroxidation, elevation of catalase activity, and reduced glutathione content. In addition, aucubin significantly reduced expression of matrix metalloproteinase-1 (MMP-1) protein (54%) and mRNA. Taken together, these results suggest that aucubin may offer protection against UVB-induced oxidative stress and may be used as a potential agent in prevention of UVB-induced photoaging.

• 한국약용작물학회지
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• 제25권1호
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• pp.16-21
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• 2017

Background: Rehmannia glutinosa is a perennial herb belonging to the family Scrophulariaceae. Its root has been utilized as a traditional medicine but the aerial parts (flower, flower stalk, leaf) are not used. We aimed to determine the content of three compounds [aucubin, catalpol, and ${\gamma}$-aminobutyric acid (GABA)] in the different organs of R. glutinosa cultivars (Dakang, Tokang, and Suwon 9) Methods and Results: The flower, flower stalk, leaf, and root of R. glutinosa were harvested at the end of August. The aucubin and catalpol contents were analyzed by LC/MS, whereas the GABA content was analyzed by GC/MS. The aucubin content was the highest in the leaf, while catalpol and GABA were the highest in the flower. The aucubin contents of leaf in Dakang, Tokang, and Suwon 9 were 1.43, 0.81, and 1.07 mg/g, respectively. The catalpol contents of flower in Dakang, Tokang, and Suwon 9 were 41.06, 28.78, and 37.48 mg/g, respectively, the GABA contents were 0.79, 0.76, and 0.65 mg/g, respectively. Conclusions: The aucubin, catalpol, and GABA contents were higher in the leaf and flower than that in the root. This study show that R. glutinosa leaf and flower can be used as a potential supplement.

• 생약학회지
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• 제17권2호
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• pp.129-133
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• 1986

Antimicrobial activities of aucubin, an iridoid glycoside, were investigated. Gram-positive bacterium, S. aureus appeared to be more sensitive to aucubin's aglucone, aucubigenin than Gram-negative, E. coli did. Antimicrobial activities produced by aucubigenin may result in part from the inhibition of RNA and protein biosyntheses in bacterial cells. The conversion of aucubin iridoid glycoside into aucubigenin, an aglucone, appears to be a prerequisite step to exhibit the antimicrobial activities.

• Archives of Pharmacal Research
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• 제24권1호
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• pp.55-63
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• 2001

Aucubin, an irdoid g1ucoside, was investigated to determine whether it has a stimulating effect on $\alpha$-amanitin excretion in $\alpha$-amanitin intoxicated rats, and whether there is binding activity to calf thymus DNA. High-performance liquid chromatography (HPLC) analysis of $\alpha$-amanitin in rat urine allowed quantitative measurement of the $\alpha$-amanitin concentration with a detection limit of 50${mu}g/ml$. In this system, a group treated with both $\alpha$-amanitin and aucubin showed that o(-amanitin was excreted about 1.4 times faster than in the $\alpha$-amanitin only treated group. Our previous results showed that the toxicity of $\alpha$-amanitin is due to specific inhibition of RNA polymerase activity and the resultant blockage of the synthesis of certain RNA species in the nucleus. However, no significant activity change on RNA polymerase from Hep G2 cells was observed when aucubin was treated with $\alpha$-amanitin at any concentration tested. Nevertheless, aucubigenin inhibited both DNA polymerase (IC50, 80.5${mu}g/ml$) and RNA polymerase (IC50, 135.0${mu}g/ml$) from the Hep G2 cells. The potential of both $\alpha$-amanitin and aucubin to interact with DNA were examined by spectrophotometric analysis. $\alpha$-Amanitin showed no significant binding capacity to calf thymus DNA, but aucubin was found to interact with DNA, and the apparent binding constant ($K_{app}$) and apparent number of binding sites per D7A phosphate ($B_{app}$) were 0.45$0.45{\times}$$10^4$ $M^{-1}$ and 1.25, respectively.

• 한국임상수의학회지
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• 제23권1호
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• pp.55-60
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• 2006

Aucuba japonica has variable pharmacological effects such as hepatoprotective, choleretic, hemodynamic, antimicrobial, and anti-inflammatory activities. This study was performed to investigate the effects of Aucuba japonica extract on oral wound healing. Aucubin was extracted from Aucuba japonica, and injected on either side of buccal mucosa of male mice. Artificial full thickness wounds were made on the site with 1.5 mm biopsy punch under sterile technique. The specimens had taken on day 1, 3, and 5 with 4 mm biopsy punch. Light microscopic examination and quantitative histologic analysis were performed for reepithelization, inflammatory cell infiltration. Reepithelization of the aucubin (0.1%) group was earlier than the control group. And the number of inflammatory cells of the aucubin group was lesser than the control group. In view of the results so far achieved, the aucubin extracted from Aucuba japonica may be useful for oral wound healing and it can be applied as a topical agent on the oral wound. Further research should be performed on the mechanism of aucubin on oral wound healing and proper formulation for effective topical agents.