• Natural Product Sciences
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• v.15 no.1
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• pp.50-54
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• 2009

A simple and reliable reversed phase HPLC method was developed to determine pharmacologically active compounds ent-continentalic acid, kaurenoic acid, and continentalic acid from the roots of Aralia cordata. Quantitative analysis of diterpenoids of A. cordata were performed by reverse phase C-18 column using a isocratic of acetonitrile : 0.1% trifluoroacetic acid(70:30) with UV detection at 205 nm. The correlation coefficients of each calibration curve of ent-continentalic acid, kaurenoic acid, and continentalic acid were 0.9987, 0.9983, and 0.9986, respectively. The detection limit of ent-continentalic acid, kaurenoic acid, and continentalic acid were $0.5{\sim}1.0\;{\mu}g/mL$, respectively. The contents of ent-continentalic acid (1), kaurenoic acid (2), and continentalic acid (3) of the roots of A. cordata collected from seventeen district markets in Korea were $0.09{\sim}0.75\;mg/g$, $1.09{\sim}5.43\;mg/g$, and $2.69{\sim}9.08\;mg/g$, respectively.

• International Journal of Oral Biology
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• v.35 no.4
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• pp.177-184
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• 2010

In our present study, we investigated the effects of continentalic acid on Streptococcus mutans (S. mutans) biofilm. Methanol extract of Aralia continentalis (A. continentalis) was suspended in water and sequentially partitioned with CHCl3, ethyl acetate (EtOAc), and n-butanol (n-BuOH). The CHCl3 fraction showed the highest activity and an antibacterial compound against S. mutans was isolated from this preparation through various chromatography methods by bioassay guided fractionation. MS, $^1H-NMR$ and $^{13}C-NMR$ analysis showed that the active principle was continentalic acid which was confirmed to show significant inhibitory effects against S. mutans biofilm. These results may provide some scientific rationale for the traditional use these extracts for the treatment of dental diseases.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.3
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• pp.617-622
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• 2006

In the present study, we investigated the anticariogenic compounds from Aralia continertalis (A. continnentalis) has been isolated and identified by MS, $^1H-NMR$ and $^{13}C-NMR$. The MeOH extract was suspended in $H_2O$ and sequentially Partitioned with $CHCl_3$, EtOAc, and n-BuOH. The $CHCl_3$ fraction showed remarkable antibacterial activity against S. mutans. The antibacterial activity compounds against 5. mutans by MIC was isolated successively through the screening system and various chromatography methods. From this active chloroform subfraction, isolation and identification finally gave continentalic acid by spectroscopic methods (MS, $^1H-NMR$ and $^{13}C-NMR$) as an active principle. The compound, continentalic acid, showed significant growth, acid production, adhesion and water-insoluble glucan synthesis inhibitory effect against 5. mutars. These results suggest that continentalic acid from A. continentalis may inhibit cariogenic properties of S. mutans and these properties may provide some scientific rationales that the local inhabitants used the extracts for treatment of dental diseases.

• International Journal of Oral Biology
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• v.33 no.4
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• pp.213-216
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• 2008

Continentalic acid (CA, (-)-pimara-8(14), 15-diene-19-oic acid) was isolated from the roots of Aralia cordata (Araliaceae) using bioassay-guided fractionation of a crude chloroform extract. The antibacterial activity of CA against Enterococcus faecalis and Enterococcus gallinarium was estimated by determining minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs). CA exhibited potent activity against standard vancomycin-resistant enterococci (VRE) and vancomycin-susceptible enterococci (VSE), with MICs and MBCs values between 4 and $8{\mu}g/mL$ and 4 and $16{\mu}g/mL$, respectively. This compound exhibited potent activity against strains of VRE, which are highly resistant to clinically useful antibiotics. These findings suggest that continentalic acid may be useful in controlling enterococcal infection.

• Korean Journal of Medicinal Crop Science
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• v.13 no.4
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• pp.182-185
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• 2005

Bioassay-guided isolation of the dried roots of Aralia continentalis led to the isolation of (-)-pimara-8(14), 15dien-19-oic acid (continentalic acid) and $(24E)-Stigmasta-5,22-dien-3{\beta}-ol$ (stagmasterol). Their structures were elucidated using $^1H-NMR$, $^{13}C-NMR$, UV and mass spectra analyses. The gram-positive bacterial, including methicilline-resistant (MRSA), were more sensitive to the continentalic acid and stagmasterol than gram-negative bacterial.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.19 no.2
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• pp.161-167
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• 2006

독활(Aralia continentalis)로부터 항균활성 물질을 찾아내기 위한 일환으로 항균실험과 분리실험을 병행하여 실시하였다. 항균활성물질 분리는 독활을 클로로포롬으로 추출하여 실리카겔($SiO_2$)과 분취용액체크로마토그래피(prep-HPLC)법으로 2종의 화합물을 분리하여 핵자기공명(NMR) 등 분광학적인 기법으로 이용하여 구조동정을 하였다. 이때 2종의 화합물은 (-)-pimara-8(1),15-diene-19-oic acid와 (24E)-stagmasta-5,22-dien-$3{\beta}-ol$임이 확인되었다. 2종의 화합물에 대한 메티실린 내성 황색포도상구균(MRSA) 및 메터실린 감응 황색포도상구균(MSSA)의 표준균주와 임상분리균주(MRSA)에서의 최소억제농도(MIC)가 $8-16{\mu}g/mL$로 나타났다. 그러므로 본 연구의 결과로부터 화합물(-)pimara-8(1),15-diene-19-oic acid은 항생제 내성균에 대한 치료제로서 개발 가능성을 확인할 수 있었다.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.6
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• pp.1314-1319
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• 2009

In previous study, we have shown that continentalic acid (CA) isolated from Aralia continentalis induced the growth inhibition and apoptosis in HepG2 cells. In this study, we examine the effects of CA from A. continentalis on growth inhibition and apoptosis induction in human leukemia HL-60 and mouse fibroblast NIH 3T3 cell lines. The results demonstrated that CA decreased cell growth of leukemia HL-60 cells but not human HaCaT keratinocytes, assessed with the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] and LDH (lactate dehydrogenase) assay. Flow cytometric analysis of mouse fibroblast cell lines exposed to CA showed that apoptotic cells increased in a time- and dose-dependent manner. Treatment with CA decreased the number of normal cells and increased the number of early apoptotic and late apoptotic cells in a dose-dependent manner. The induction of apoptosis in mouse cell lines by CA was mediated through the activation of caspase-3, Bak, and Bax and the down-regulation of Bcl-2. Our results suggest that CA efficiently induces apoptosis in human leukemia cells.

• Archives of Pharmacal Research
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• v.6 no.1
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• pp.17-23
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• 1983

By tracing albumin stabilizing activity an anti-inflammatory component, continentalic acid was isolated from ether-soluble acidic fraction of Aralia continentalis. Continenetalic acid in a concentration of 0.115mg/3ml gave 50% inhibition for heat denaturation of albumin. The protein stabilizing potency of it was approximately three and eleven times that of phenylbutazone and that of salicylic acid, respectively. The anti-inflammatory actions of it and its methylester were investigated employing carrageenin-induced edema in rat paw. Continentalic acid administered s. c. showed an activity of about three times of hydrocortisone. When administered p. o., it was still active, but its methylester was more active than phenylbutazone, suggesting the poor absorption of it in gastorointestinal tract. Its chemical structure was identified by chemical and spectral studies as (-) pimara 8(14), 15-diene-19-oic acid, which was already isolated from A. dordata, but not reported for its biological activity.

• Korean Journal of Oriental Medicine
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• v.12 no.3 s.18
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• pp.101-115
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• 2006

The purpose of this study was to introduce the differential standard of the types of Angelicae Pubescentis Radix. We established the classificatory standard according to the external and internal morphology and the physicochemistrical pattern for the four types of Aucklandiae Radix. The results follow: 1. At the external shape, Angelica pubescens f. biserrata has rising lenticel and dark brown surface, Its section is light gray and its xylem is yellow gray. Aralia continentalis has big stem mark in upper portion, its section has no dense tissue with yellow gray. Heracleum hemsleyanum has dark brown surface and little lenticel, its cortical layer is white yellow and xylem is isabella and powdered. 2. At the internal shape, Angelica pubescens f. biserrata has phloem with half of the root and rare vessel. Aralia continentalis has phloem with two-thirds of the root and it has broad cutting and putting vessel that formed 1-2 row. Heracleum hemsleyanum also has phloem with half of the root and wide scattered latex tube and many large vessel. 3. At the TLC pattern, Heracleum hemsleyanum has remarkable dark spot at $R_{f}$ 0.23 on the sulphuric acid color pattern test, but others have faint. 4. At the HPLC pattern, all samples have generally patterns. But Angelica pubescens f. biserrata shows diminutive continentalic acid content and the peak at Rt 20.278min comes out on Heracleum hemsleyanum, but do not come out on Aralia continentalis and Angelica pubescens f. biserrata. Heracleum hemsleyanum has remarkable peak at Rt 20.278min, but shows no peak at Rt 29.023min unlike Aralia continentalis or Angelica pubescens f. biserrata. Also Aralia continentalis and Angelica pubescens f. biserrata show one remarkable peak at Rt 29.023, but Heracleum hemsleyanum do not show. Consequently, Aralia continentalis and Angelica pubescens f. biserrata are comparable whit continentalic acid content and Heracleum hemsleyanum is comparable with the peak at Rt 20.273 and Rt 29.023. So it is thought that content of continentalic acid and the peaks at Rt 20.278 and Rt 29.023 can apply to differentiate a species from other. It is considered the results of this study will be furnished the basis to succeeding studies and it is needed to extensive comparative study for the same genus-degree of relatedness.

• Journal of Life Science
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• v.34 no.4
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• pp.215-226
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• 2024

Aralia continentalis is widely distributed in Far East Asian countries such as Korea, China, and Japan. A. continentalis has traditionally been used as an herbal remedy for various conditions, including analgesia, headache, inflammation, lameness, lumbago, rheumatism, and dental diseases in Korea. Previously, epi-continentalic acid, continentalic acid, and kaurenoic acid as major active biological compounds belonging to the diterpenoid class were identified. To synthesize diterpenoid derivatives with enhanced bioavailability, Fusarium fujikuroi was employed to biotransform diterpenoids due to its known antibacterial activity. This yielded two derivatives of kaurenoic acid, namely 16α-hydroxyent-kauran-2-on-19-oic acid and 2β, 16α-dihydroxy-ent-kauran-19-oic acid, with their chemical structures elucidated via NMR analysis. These derivatives exhibited increased polarity compared to kaur- enoic acid, as evidenced by their retention time on preparative HPLC using the ODS-A column and structural modifications. Evaluation of their antidiabetic activity targeting PTP1B, a negative regulator of the insulin signaling pathway, revealed inhibitory activities of 30.8% and 27.6%, respectively, at a concentration of 4 ㎍/ml. Additionally, both derivatives demonstrated low cytotoxicity, with an IC50 value 18 times higher than kaurenoic acid. Therefore, the augmented water solubility and reduced toxicity of 16α-hydroxy-ent-kauran-2-on-19-oic acid and 2β, 16α-dihydroxy-ent-kauran-19-oic acid, resulting from biotransformation by F. fujikuroi, render them promising candidates for industrial applications.