• 대한본초학회지
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• 제23권4호
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• pp.149-157
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• 2008

Objectives: This study was to analyze the content changes of ${\beta}$-asarone and ${\alpha}$-asarone in A. gramineus according to its parts, extraction method, and fermentation. Methods: The change of ${\beta}$-asarone and ${\alpha}$-asarone was analysed with GC/MS, IR, and NMR. Results: In A. gramineus, ${\beta}$-asarone and ${\alpha}$-asarone in rhizome are 7 times and 4 times more than those in leaves respectively. And, in water extract of Acori Graminei Rhizoma, ${\beta}$-asarone was reduced to 77.8%-83.5%, and ${\alpha}$-asarone was reduced to 69.4%-72.2% compared with 50% MeOH extract. The amounts of ${\beta}$-asarone and ${\alpha}$-asarone were decreased apparently by 1 and 3 weeks fermantation with yeast activated solution. Conclusions: There was a change in the content of asarone pursuant to the medicinal part, extraction solvent, and fermentation. This result can be used as the basic data contributing to the stability of A. gramineus according to an appropriate clinical application.

• 한국식품과학회지
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• 제45권3호
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• pp.279-284
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• 2013

본 연구에서는 UPLC를 이용하여 석창포의 기원종을 비교하기 위하여 4종 창포류(A. gramineus, A. tatarinowii, A. calamus, Anemone altaica)의 ${\alpha}$-asarone과 ${\beta}$-asarone의 함량 분석을 실시하였고, 분석법 validation은 ICH 지침에 따라 검증하였다. 창포류 4종에 대한 함량분석에서는 모든 시료에 대해 2% 이하의 상대 표준편차를 나타내었고, ${\beta}$-asarone의 함량은 석창포, 중국석창포, 창포, 구절창포 순으로 나타났으며, ${\alpha}$-asarone은 창포, 중국 석창포, 석창포 순으로 나타났다. 특히, 구절창포에서는 ${\beta}$-asarone이 미량이었고, ${\alpha}$-asarone는 검출되지 않았다. PCA 분석에서도 4종의 창포류가 네 그룹으로 나누어 지는 것을 확인할 수 있었다. 이와 같이, 본 실험 결과를 통하여 석창포, 중국 석창포, 창포 및 구절창포를 명확히 구별할 수 있었고, 석창포의 품질평가에 응용할 수 있을 것이라 기대된다.

• 동의생리병리학회지
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• 제28권3호
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• pp.317-321
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• 2014

Amyloid-${\beta}$ protein ($A{\beta}$) is a pathological component of Alzheimer's disease (AD) by participating in the senile plaque formation in the patient's brain. Although the exact mechanism of $A{\beta}$ toxicity is not fully elucidated, it is considered to be closely related to its fibrillation process. For prevention of AD, recent studies have suggested various small molecules which inhibit $A{\beta}$ fibrillation. In this report, ${\beta}$-asarone found in acorus plant has been investigated as an anti-amyloid molecule. ${\beta}$-Asarone was demonstrated to prevent in vitro fibrillation of $A{\beta}$ by inducing the oligomer formation that obviously decreased cytotoxicity. Therefore, ${\beta}$-asarone could be suggested as an inhibitory agent of $A{\beta}$ fibrillation and toxicity, which would help us not only to understand underlying principle of amyloidogenesis mechanism but also to develop a controlling strategy toward AD.

• 생명과학회지
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• 제28권2호
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• pp.195-200
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• 2018

베타아사론은 널리 알려진 석창포의 주요 효능 성분이다. 본 연구에서는 모기의 oviposition 페로몬 성분인 MOP와 석창포 효능성분 베타아사론의 열대집모기 후각 단백질 CquiOBP1 활성 부위에 대한 친화도 분석 실험을 컴퓨터 분자결합 분석 방법을 통해 비교하였다. CquiOBP1 후각 단백질의 3차원 구조 정보는 PDB database (PDB ID: 3OGN)를 활용하였다. In silico 결합 분석을 수행하기 위해 PyRx, Autodock Vina, Discovery Studio Version 4.5, and NX-QuickPharm 프로그램을 각 분석 조건에 따라 활용하였다. CquiOBP1 후각단백질 활성 부위에 대한 베타아사론의 결합친화도는 -6.40 kcal/mol으로 나왔으며 이는 -6.00 kcal/mol으로 나온 MOP의 결합친화도 보다 훨씬 더 높고 효율적인 것으로 분석되었다. 리간드와 상호작용 하는 CquiOBP1단백질 활성 부위의 아미노산들 가운데 TRP114가 공히 MOP와 베타아사론과 결합 하였다. CquiOBP1 단백질 활성부위의 아미노산들을 전혀 다른 전기적 성질을 지닌 아미노산으로 치환 시킨 후 분자결합 분석을 해 본 결과 리간드들의 X,Y,Z Grid 값에 현격한 변화가 유도되었으며 결합 친화도 또한 감소되었다. 이러한 결과를 통하여 베타아사론은 CquiOBP1 단백질 활성을 조절하는 리간드로서 효과적으로 작용할 것으로 보인다. 결론적으로 석창포 추출물 또는 베타아사론은 곤충기피제 신물질 연구 개발 분야에 효율적으로 활용할 수 있을 것으로 사료된다.

• 한국환경농학회지
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• 제30권1호
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• pp.76-81
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• 2011

식의약소재로서 석창포의 활용성을 조사하고자 석창포 추출물의 모기에 대한 기피효과를 시험한 결과 모기를 방사한 장소에서 추출물에 노출된 공간으로 이동한 모기 마리수 비율은 추출물을 함유하지 않은 공간으로 이동한 모기 마리수 비율에 대비하여 현저하게 낮았다. 또한, 방사한 공간에 남아 있는 모기 마리수 비율은 석창포 추출물을 함유하지 않은 공간으로 이동한 모기 마리수 비율에 비해 낮았다. 이는 모기가 석창포 추출물을 기피하는 경향에서 비롯된 결과임을 의미하였다. 석창포 추출물의 모기기피 활성성분을 조사하고자 추출물을 GC/MS 분석한 결과 주요 성분은 ${\beta}$-asarone으로 밝혀졌다. 시판중인 asarone을 이용하여 기피실험을 실시한 결과 ${\alpha}$-asarone과 ${\beta}$-asarone 모두 기피활성을 보였으며 ${\beta}$-asarone이 ${\alpha}$-asarone에 비해 기피활성이 높았다. 이러한 결과는 석창포 추출물이 친환경적으로 모기를 제어하기 위한 식의약소재로 활용될 수 있음을 의미하였다.

• Asian Pacific Journal of Cancer Prevention
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• 제13권10호
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• pp.5291-5298
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• 2012

Beta-asarone is one of the main bioactive constituents in traditional Chinese medicine Acorus calamu. Previous studies have shown that it has antifungal and anthelmintic activities. However, little is known about its anticancer effects. This study aimed to determine inhibitory effects on LoVo colon cancer cell proliferation and to clarify the underlying mechanisms in vitro and in vivo. Dose-response and time-course anti-proliferation effects were examined by MTT assay. Our results demonstrated that LoVo cell viability showed dose- and time-dependence on ${\beta}$-asarone. We further assessed anti-proliferation effects as ${\beta}$-asarone-induced apoptosis by annexin V-fluorescein isothiocyanate/propidium iodide assay usinga flow cytometer and observed characteristic nuclear fragmentation and chromatin condensation of apoptosis by microscopy. Moreover, we found the apoptosis to be induced through the mitochondrial/caspase pathway by decreasing mitochondrial membrane potential (MMP) and reducing the Bcl-2-to-Bax ratio, in addition to activating the caspase-9 and caspase-3 cascades. Additionally, the apoptosis could be inhibited by a pan-caspase inhibitor, carbobenzoxy-valyl-alanyl-aspartyl-[O-methyl]-fluoromethylketone (Z-VAD-FMK). When nude mice bearing LoVo tumor xenografts were treated with ${\beta}$-asarone, tumor volumes were reduced and terminal deoxynucleotide transferase-mediated dUTP nick end labeling (TUNEL) assays of excised tissue also demonstrated apoptotic changes. Taken together, these findings for the first time provide evidence that ${\beta}$-asarone can suppress the growth of colon cancer and the induced apoptosis is possibly mediated through mitochondria/caspase pathways.

• Biomolecules & Therapeutics
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• 제22권1호
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• pp.17-26
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• 2014

${\alpha}$-Asarone exhibits a number of pharmacological actions including neuroprotective, anti-oxidative, anticonvulsive, and cognitive enhancing action. The present study investigated the effects of ${\alpha}$-asarone on pro-inflammatory cytokines mRNA, microglial activation, and neuronal damage in the hippocampus and on learning and memory deficits in systemic lipopolysaccharide (LPS)-treated C57BL/6 mice. Varying doses of ${\alpha}$-asarone was orally administered (7.5, 15, or 30 mg/kg) once a day for 3 days before the LPS (3 mg/kg) injection. ${\alpha}$-Asarone significantly reduced TNF-${\alpha}$ and IL-$1{\beta}$ mRNA at 4 and 24 hours after the LPS injection at dose of 30 mg/kg. At 24 hours after the LPS injection, the loss of CA1 neurons, the increase of TUNEL-labeled cells, and the up-regulation of BACE1 expression in the hippocampus were attenuated by 30 mg/kg of ${\alpha}$-asarone treatment. ${\alpha}$-Asarone significantly reduced Iba1 protein expression in the hippocampal tissue at a dose of 30 mg/kg. ${\alpha}$-Asarone did not reduce the number of Iba1-expressing microglia on immunohistochemistry but the average cell size and percentage areas of Iba1-expressing microglia in the hippocampus were significantly decreased by 30 mg/kg of ${\alpha}$-asarone treatment. In the Morris water maze test, ${\alpha}$-asarone significantly prolonged the swimming time spent in the target and peri-target zones. ${\alpha}$-Asarone also significantly increased the number of target heading and memory score in the Morris water maze. The results suggest that inhibition of pro-inflammatory cytokines and microglial activation in the hippocampus by ${\alpha}$-asarone may be one of the mechanisms for the ${\alpha}$-asarone-mediated ameliorating effect on memory deficits.

• Biomolecules & Therapeutics
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• 제20권5호
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• pp.477-481
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• 2012

The rhizomes of Acorus gramineus have frequently been used in traditional medicine mainly for sedation as well as enhancing brain function. In this study, the anti-allergic activity of A. gramineus was investigated. The 70% ethanol extract of the rhizomes of A. gramineus was found to inhibit the allergic response against 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and ${\beta}$-hexosaminidase release from RBL-2H3 cells with $IC_{50}$'s of 48.9 and > $200{\mu}g/ml$, respectively. Among the 9 major constituents isolated, ${\beta}$-asarone, (2R,3R,4S,5S)-2,4-dimethyl-1,3-bis (2',4',5'-trimethoxyphenyl)tetrahydrofuran (AF) and 2,3-dihydro-4,5,7-trimethoxy-1-ethyl-2-methyl-3-(2,4,5-trimethoxyphenyl)indene (AI) strongly inhibited 5-LOX-catalyzed LT production in A23187-treated RBL-1 cells, AI being the most potent ($IC_{50}=6.7{\mu}M$). Against ${\beta}$-hexosaminidase release by antigen-stimulated RBL-2H3 cells, only AI exhibited strong inhibition ($IC_{50}=7.3{\mu}M$) while ${\beta}$-asarone and AF showed 26.0% and 39.9% inhibition at $50{\mu}M$, respectively. In addition, the ethanol extract of A. gramineus showed significant inhibitory action against the hapten-induced delayed hypersensitivity reaction in mice by oral administration at 200 mg/kg. Therefore, it is suggested that A. gramineus possesses anti-allergic activity and the constituents including ${\beta}$-asarone and AI certainly contribute to the anti-allergic activity of the rhizomes of A. gramineus.

• Bulletin of the Korean Chemical Society
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• 제32권5호
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• pp.1547-1553
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• 2011

An effective analytical method of gas chromatography/mass spectrometry (GC/MS) was developed for the rapid determination of essential oils in the crude extract of Acorus species (Acorus gramineus, Acorus tatarinowii, and Acorus calamus). Major phenypropanoids (${\beta}$,${\alpha}$-asarone isomers, euasarone, and methyleugenol) and ${\beta}$-caryophyllene in Acorus species were used as marker compounds and determined for the quality control of herbal medicines. To extract marker compounds, various extraction techniques such as solvent immersion, mechanical shaking, and sonication were compared, and the greatest efficiency was observed with sonication extraction using petroleum ether. The dynamic range of the GC/MS method depended on the specific analyte; acceptable quantification was obtained between 10 and 2000 ${\mu}g/mL$ for ${\beta}$-asarone, 10 and 500 ${\mu}g/mL$ for ${\alpha}$-asarone, 10 and 200 ${\mu}g/mL$ for methyleugenol, and between 5 and 100 ${\mu}g/mL$ for ${\beta}$-caryophyllene. The method was deemed satisfactory by inter- and intra-day validation and exhibited both high accuracy and precision, with a relative standard deviation < 10%. Overall limits of detection were approximately 0.34-0.83 ${\mu}g/mL$, with a standard deviation (${\sigma}$)-to-calibration slope (s) ratio (${\sigma}$/s) of 3. The limit of quantitation in our experiments was approximately 1.13-3.20 ${\mu}g/mL$ at a ${\sigma}$/s of 10. On the basement of method validation, 20 samples of Acorus species collected from markets in Korea were monitored for the quality control. In addition, principal component analysis (PCA) and hierarchical cluster analysis (HCA) were performed on the analytical data of 20 different Acorus species samples in order to classify samples that were collected from different regions.

• Biomolecules & Therapeutics
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• 제23권6호
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• pp.571-581
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• 2015

${\beta}$-asarone (BAS) is an active component of Acori graminei rhizoma, a traditional medicine used clinically in treating dementia and chronic stress in Korea. However, the cognitive effects of BAS and its mechanism of action have remained elusive. The purpose of this study was to examine whether BAS improved spatial cognitive impairment induced in rats following chronic corticosterone (CORT) administration. CORT administration (40 mg/kg, i.p., 21 days) resulted in cognitive impairment in the avoidance conditioning test (AAT) and the Morris water maze (MWM) test that was reversed by BAS (200 mg/kg, i.p). Additionally, as assessed by immunohistochemistry and RT-PCR analysis, the administration of BAS significantly alleviated memory-associated decreases in the expression levels of brain-derived neurotrophic factor (BDNF) and cAMP-response element-binding protein (CREB) proteins and mRNAs in the hippocampus. Also, BAS administration significantly restored the expression of Bax and Bcl-2 mRNAs in the hippocampus. Thus, BAS may be an effective therapeutic for learning and memory disturbances, and its neuroprotective effect was mediated, in part, by normalizing the CORT response, resulting in regulation of BDNF and CREB functions and anti-apoptosis in rats.