• Advances in Traditional Medicine
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• 제7권4호
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• pp.395-408
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• 2007

This study reports the analgesic, anti-inflammatory and membrane-stabilizing property of alcoholic extract of Ophiorrhiza nicobarica (ON), a wild herb, used as an anti-infective ethnomedicine of Nicobarese and Shompen tribes of Great Nicobar Island, India. We for the first time investigated the analgesic and antiinflammatory potential of this herb in acute, subacute and chronic model of inflammation in Swiss albino mice and Wistar albino rats, along with sheep RBC-induced sensitivity and membrane stabilization. The acetic acid induced writhing, tail flick and tail immersion tests are used as a model for evaluating analgesic activity; while the carrageenin-induced paw oedema was used as the model for acute inflammation, dextran-induced oedema as sub-acute and cotton-pellateinduced granuloma as chronic inflammatory model. The probable mode by which ON mediate its effect on inflammatory conditions was studied on sheep RBC-induced sensitivity and membrane stabilization. The in vitro results revealed that the ON extract possesses significant (P < 0.05) dose dependent analgesic and antiinflammatory activity at 200 and 300 mg/kg and its fractions at 50 mg/kg, p.o. respectively, compared to the control groups. However, the extract failed to exhibit membrane-stabilizing property as it unable to reduce the level of haemolysis of RBC exposed to hypotonic solution. The acute toxicity studies of ON extract in rats and mice revealed that the extract was nontoxic even up to 3.0 g/kg body weight of the animals, with a high safety profile. We have isolated ursolic acid, ${\beta}$-sitosterol and harmaline respectively, from the bioactive part of the extract. The results indicated that the O. nicobarica is indeed beneficial in primary health care, and suggest that its anti-inflammatory activity may not be related to membrane-stabilization.

• 한국식품영양학회지
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• 제32권4호
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• pp.364-370
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• 2019

This study was conducted to select cultivars and determine the harvest period suited for the availability of biological activities in unripen apple. To analyze effective the components in the apple (Malus domestica), three cultivars, 'Summerking', 'Hongro', 'Fuji' were harvested from 40~50 days after full bloom to harvest time. Soluble solid content increased gradually by ripening but titratable acidity decreased with ripening regardless of the cultivars. The total phenol content significantly reduced with ripening from May 30 to July 30 (p<0.05). Substantially, the total phenol content of 'Hongro' in May 30 was four times higher than that of 'Summerking' in the same period and ten times higher than that of 'Hongro' in August 30. The total flavonoid content reduced with ripening regardless of cultivars (p<0.05) and that of 'Hongro' in May 30 was significantly highest (p<0.05). The ascorbic acid content was the highest in 'Hongro' in May 30 (p<0.05). The contents of tannin and ursolic acid significantly reduced with ripening from May 30 to July 30 (p<0.05), while no significant difference was observed between Hogro and Fuji after July 30. Therefore, 'Hongro' harvested in May 30 was considered to be best in the utilization of the effective components of immature apple.

• 한국식품저장유통학회지
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• 제24권7호
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• pp.1007-1016
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• 2017

다슬기는 예로부터 간염, 간경화, 지방간 등의 치료 및 개선에 이용되어 왔으며, 특히 소변불통, 소갈증(당뇨) 등의 약용으로 이용되어 왔다. 본 연구에서는 이러한 다슬기를 대상으로 항당뇨에 대한 효능을 과학적으로 검증하고 그 기작을 규명하고자 하였다. 먼저 다슬기의 생물학적 기능성을 높이기 위해 효소 가수분해를 실시하였으며, protamex에 의한 가수분해도는 10시간 후 약 43% 수준을 나타내었다. PTP1B는 인슐린 신호전달기전에서 IRS-1의 인산화를 방해하여 인슐린 민감성을 저해시키는 효소이다. protamex를 이용한 다슬기 가수분해물(MPH)의 PTP1B에 대한 저해활성은 $15.42{\pm}1.1{\mu}g/mL$의 $IC_{50}$ 값을 나타내어 양성대조군 ursolic acid의 $16.7{\mu}g/mL$ 보다 높은 저해활성을 보이면서 강한 항당뇨 활성 소재로서의 가능성을 보였다. 이에 따라 유리지방산을 이용하여 C2C12 myoblast에서 인슐린 저항성을 유도하고, MPH에 의한 포도당 흡수 정도를 확인하였다. 그 결과, 1 mM PA 처리에 의해 약 32% 수준으로 떨어진 포도당 흡수율은 MPH 처리에 의해 약 199% 수준으로 증가하였다. 또한 장기간 고농도의 포도당(30 mM)에 의해 유도된 당독성 조건에서 MPH는 췌장의 베타세포 INS-1 세포의 생존율을 증가시키고, 대조군에 비해 약 160% 인슐린 mRNA 발현량을 증가시켰다. 이러한 결과에서 MPH는 PTP1B 활성을 저해함으로써 인슐린 신호전달 기작을 활성화하고, 인슐린저항성 환경에서 포도당 흡수를 증진시켜 인슐린저항성을 개선하며, 나아가 고농도 포도당에 의해 유도되는 당독성환경에서 췌장 베타세포를 보호하고 인슐린 mRNA발현량을 정상화할 수 있다는 것을 확인할 수 있었다.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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• pp.108-109
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• 2003

Ursolic acid (UA) and Oleanolic acid (ONA), known as urson, micromerol, prunol and malol, are pentacyclic triterpenoid compounds which naturally occur in a large number of vegetarian foods, medicinal herbs, and plants. They may occur in their free acid form or as aglycones for triterpenoid saponins, which are comprised of a triterpenoid aglycone, linked to one or more sugar moieties. Therefore UA and ON A are similar in pharmacological activity. Lately scientific research, which led to the identification of UA and ONA, revealed that several pharmacological effects, such as antitumor, hepatoprotective, anti-inflammatory, antimicrobial, and anti-hyperlipidemic could be attributed to UA and ONA. Here, we introduced the effects of UA and ONA on acute barrier disruption and normal epidermal permeability barrier function. To clarify the effects of UA and ONA on skin barrier recovery, both flank skin of 8-12 weeks hairless mice were topically treated with samples (2mg/ml) after tape stripping, then measured recovery rate using TEWL on hairless mice. The recovery rate increased in UA and ONA treated groups at 6h more than 20% compared to vehicle treated group (p <0.05). For verifying the effects of UA and ONA on normal epidermal barrier, hydration and TEWL were measured for 1 and 3 weeks after UA and ONA applications (2mg/ml per day). We also investigated the features of epidermis and dermis using electron microscopy (EM) and light microscopy (LM). Both samples increased hydration compared to Vehicle group from 1 week without TEWL alteration (p<0.005). EM examination using Ru04 and OsO4 fixation revealed that secretion and numbers of lamellar bodies and complete formation of lipid bilayers were most prominent (ONA$\geq$UA>Vehicle). LM finding showed that stratum corneum was slightly increased and especially epidermal thickening and flattening was observed (UA>ONA>Vehicle). Using Masson-trichrome and elastic fiber staining, we observed collagen thickening and elastic fiber increasing by UA and ONA treatments. In vitro results of collagen and elastin synthesis and elastase inhibitory experiments were also confirmed in vivo findings. This result suggested that the effects of UA and ONA related to not only skin barrier but also collagen and elastic fibers. Taken together, UA and ONA can be relevant candidates to improve barrier function and pertinent agents for cosmetic applications.

• Bulletin of the Korean Chemical Society
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• 제33권5호
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• pp.1505-1508
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• 2012

Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound ($\mathbf{4}$) was first observed to have moderate inhibitory activity against PTP1B with an $IC_{50}$ value of $13.72{\pm}1.53{\mu}M$. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound ($\mathbf{4}$) as the lead compound. Compound $\mathbf{4l}$ ($IC_{50}=3.12{\pm}0.18{\mu}M$) was 4.4-fold more potent than the lead compound $\mathbf{4}$ ($IC_{50}=13.72{\pm}1.53{\mu}M$), and more potent than the positive control, ursolic acid ($IC_{50}=3.40{\pm}0.21{\mu}M$). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.

• 한국식생활문화학회지
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• 제27권4호
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• pp.391-399
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• 2012

In this study, the sensory and mechanical characteristics of white bread containing different levels of Korean and Chinese sansa powder were evaluated. Korean sansa was smaller and more reddish than that of Chinese sansa. Sansa powder contained ursolic acid, citric acids, and flavonoids, which have antioxidative effects. Contents of total flavonoids in Korean and Chinese sansa powder were $217.67{\pm}7.64$ mg/100 g and $127.67{\pm}7.85$ mg/100 g, respectively. The mechanical and sensory characteristics of bread added with different levels (0, 2, 4, and 6%) of Korean and Chinese sansa powder were evaluated. Lightness of crust and crumb of bread containing Korean sansa powder decreased as the level of Korean sansa powder increased, whereas they increased as the level of Chinese sansa powder increased. Mechanical texture parameters such as hardness and gumminess increased as the level of Korean and Chinese of sansa powder increased. In a sensory evaluation, control, bread containing 2 or 4% Korean sansa powder, and bread containing 2% Chinese sansa powder showed higher overall acceptability than the others. In conclusion, these results indicate that the recommended substitution level for sansa powder in bread is 2 or 4% Korean sansa powder and 2% Chinese sansa powder.

• 대한화장품학회지
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• 제30권1호
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• pp.15-22
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• 2004

홍화(Carthamus tincforiu L.)는 한방에서 어혈, 통경 및 고지혈증 치료제로서 그리고 홍화씨는 진정 및 보혈 등의 약용 소재로 이미 널리 이용되고 있으며, 화장품 원료로서 홍화추출물과 홍화씨유가 사용되고 있다. 본 실험에서는 홍화씨 유박(oil cake)으로부터 식물성유사여성호르몬(phytoestrogen) 거동의 세로토닌(serotonin)유도체를 함유한 정제분말을 제조하여 화장품 원료로서리 적용 가능성을 실험하였다. 홍화씨추출물을 식물성유사여성호르몬으로 알려진 레즈베라트롤(resyeratrol)과 제니스테인(genistein) 및 기능성 주름개선제로 알려진 레티놀(retinol)과 우르소릭애씨드(ursolic acid)와 함께 항주름 효과와 관련한 항산화 효과, 엘라스타제 활성저해 효과, 섬유아세포 활성촉진 효과 및 콜라겐 생성촉진 효과에 대하여 비교 실험하였다. 실험 결과, 세로토닌유도체를 함유한 홍화씨추출물은 피부에 자극없이 항산화 효과, 엘라스타제 활성저해 효과, 섬유아세포로 활성촉진 효과 및 콜라겐 생성촉진 효과가 우수하여 주름개선용 기능성 화장품 원료로 기대되고 있다. 피부의 주름을 개선할 수 있는 가능성있는 원료로 기대되었다.

• 생약학회지
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• 제51권2호
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• pp.93-99
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• 2020

This study was performed to find anti-inflammatory or antitumor compounds from the polar fraction obtained from the extract of Clinopodium chinense var. shibetchense (H. Lev) Koidz (Labiatae). Chromatography of the BuOH fraction yielded two flavonoid glycosides (compounds 1 and 2) and two saponins (compounds 3 and 4). On the basis of spectroscopic data, compounds 1 and 2 were identified to be ponciretin 7-O-α-L-rhamnopyranosyl-(1→6)-α-D-glucopyranoside (neoponcirin) and naringenin 7-O-α-L-rhamnopyranosyl-(1→6)-α-D-glucopyranoside (isonaringin). Compounds 3 and 4 were identified to be 3-O-{β-D-glucopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-β-D-fucopyranosyl}-saikogenin F (buddlejasaponin IV) and 3-O-{β-D-glucopyranosyl-(1→2)-[β-D-glucopyranosyl-(1→3)]-β-D-fucopyranosyl}-21β-hydroxysaikogenin F (clinoposaponin XV). In addition, ursolic acid (5) was isolated and identified from the CHCl₃ fraction. Inducible nitric oxide synthase (iNOS) assay and sulforhodamine B (SRB) assay were performed to lead a potential anti-inflammatory or anti-tumor compounds from C. chinense var. shibetchense. Of the four compounds (1 - 4), compound 3 considerably inhibited cancer cell growth and NO production (IC₅₀s, 5.59 μM in iNOS assay and 6.62 - 14.88 μM in SRB assay).

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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• pp.224-230
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• 1998

This study showed the anti-invasive activity of ginseng components, panaxadiol (PD) and panamatrlol (PT) on the highly metastatic HT1080 human flbrosarcoma cell line. PD and PT reduced tumor cell invasion through a reconstitute basement membrane in the transwell chamber. A significant down regulation of MMP-9 by PD and PT was detected by northern blot analysis. However, MMP-2 was constantly expressed. Quantitative gelatin based zymography confirmed a marked reduced expression of MMP-9 but not MMP-2 in the treatment of PD and PT. Since the chemical structures of PD and PT are very similar to that of dexamethasone, a synthetic glucocorticoid, it was investigated whether PD and PT act through GR. Western blot analysis and immunocytochemistry showed that PD and PT increased the GR fraction in the nucleus. These results suggest that ursolic acid may induce repression of MMP-9 by stimulating the nuclear translocation of GR and hence inhibiting the activity of AP-1 to TPA-responsible element of MMP-9 promoter region. In conclusion, we suggest that CR-induced down-regulation of MMP-9 by PD and PT contributes to reduce the invasive capacity of HT 1080 cells.

• 동의생리병리학회지
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• 제17권4호
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• pp.1059-1064
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• 2003

Oldenlandiae Herba has been used for the prevention or treatment of cancer in oriental medicine for years. Experimentally its antitumor activity was reported. However, in order to develop new Korean original plants. we tried to study the antitumor activity of Chinese and Korean origin Oldenlandiae Herba. We first evaluated the cytotoxicity of Oldenlandiae Herba originated from China and Korea on HT1080, U937 and SK-mel tumor cells. MeOH extract of Chinese Oldelandiae Herba was more effective than MeOH extract of Korean Oldenlandiae Herba. Approixmately IC50 of two species of Oldelandiae Herba was 380-450 ug/ml. For evaluation of antiangiogenic activity, proliferation assay with HUVECs(Human umblical vein endothelial cells) was done with three samples. Chinese Herba and Korean Herba and root. Korean root and herba was more effective than Chinese Herba. Thus, we found Korean Oldenlandiae was more effective on angigenic activity than Chiness Oldenlandiae. In an anlytical study on effective compounds from Oldenlandiae, the spot of ursolic acid was more marked by Korean Oldenlandiae than by Chinese Oldenlandiae. whereas the spot of asperuloside was more pronounced by Chinese Oldenlandiaethan by Korean Oldenlandiae by TLC analysis.