• Archives of Pharmacal Research
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• v.25 no.4
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• pp.528-533
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• 2002

To evaluate the antithrombotic and antiallergic properties of rhaponticin extracted from Rhei Rhizoma, the in vitro and ex vivo inhibitory activities of rhaponticin and its metabolite, rhapontigenin, were measured. These compounds inhibited in vitro ADP- and collagen-induced platelet aggregation. Rhapontigenin was more potent, with $IC_{50}$ values of 4 and $70{\;}{\mu}g/ml$, respectively. In ex vivo ADP- and collagen-induced rat platelet aggregation, these compounds also exhibited a potent inhibitory effect. The antiplatelet aggregation effects of rhaponticin and rhapontigenin were more potent than those of aspirin. Rhapontigenin showed significant protection from death due to pulmonary thrombosis in mice. Rhapontigenin also showed the strongest inhibitory activity against $\beta-hexosaminidase$ release induced by DNP-BSA. These compounds inhibited PCA reaction in mice. Rhapontigenin intraperitoneally administered showed the strongest inhibitory activity and significantly inhibited PCA at doses of 25 and 50 mg/kg, with inhibitory activities of 48 and 85%, respectively. The inhibitory activity of orally administered rhaponticin was stronger than that of intraperitoneally administered rhaponticin. These results suggest that rhaponticin, in the rhizome of Rhei Rhizoma, is a prodrug that has extensive antiallergic and antithrombotic properties.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.1
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• pp.124-128
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• 2008

This study was aimed to analyze the composition and to quantify the contents of stilbenoids in the leaves and fruits of Morus alba L. using high performance liquid chromatography with phodtodiode array detector and UV detector. Optimal wavelength for the detection of various stilbenoids such as resveratrol, piceatannol, rhapontigenin, astringin, pterostilbene, piceid, rhaponticin and vitisin A was screened by DAD detector and set to 308 nm. Seven kinds of stilbenoids except vitisin A were identified in fruits, while 5 kinds of stilbenoids in leaves. Total stilbenoids contents were $609.15{\pm}7.24$ mg/100 g d.w. in fruits and $188.57{\pm}1.70$ mg/100 g d.w in leaves. Stilbenoids contents in fruits were 3 times higher than those in leaves. Rhaponticin was the most profound stilbene, analyzed to $389.26{\pm}5.22$ mg/100 g d.w. (63.8% of total stilbenoids) in fruits and $99.17{\pm}2.79$ mg/100 g d.w. (52.5% of total stilbenoids) in leaves. Astringin and piceatannol were only detected in fruits and vitisin A was not detected. Contents of piceid and rhaponticin were higher than those of aglycone forms, rhapontigenin and resveratrol.

• Food Science and Biotechnology
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• v.17 no.3
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• pp.675-678
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• 2008

Permeability of resveratrol, piceid, rhapontigenin, and rhaponticin in Caco-2 cell assays using high-performance liquid chromatography were compared. Caco-2 cell monolayers were used to evaluate the transport rates of stilbene analogues from the apical to the basolateral sides. All stilbenes experimented in this study were transported to the basolateral side by times. For comparing the permeability of 4 stilbenes, we calculated the slope of the cumulative concentration of each stilbene in basolateral sides over time, resulting in those values of resveratrol, piceid, rhapontigenin, and rhaponticin with $3.766{\times}10^{-5}$, $4.330{\times}10^{-6}$, $5.430{\times}10^{-5}$, and $2.458{\times}10^{-5}\;{\mu}M/sec$, respectively. Apparent permeability coefficient of resveratrol and rhapontigenin were calculated to $9.994{\times}10^{-6}$ and $1.441{\times}10^{-6}\;cm/sec$, respectively, while those of piceid and rhaponticin were to $1.149{\times}10^{-7}$ and $6.523{\times}10^{-7}\;cm/sec$, respectively. These results suggest that aglycones would be absorbed more effectively than glycosides in stilbenoids.

• The Journal of Korean Medicine
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• v.19 no.1
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• pp.89-99
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• 1998

약효(藥效) 및 안정성(安定性)이 입증(立證)된 한약(韓藥)으로부터 새로운 항균제(抗菌劑)를 도출(導出)하고자, 임상(臨床)에서 청열작용(淸熱作用)이 있거나 염증성(炎症性) 질환(疾患)과 박테리아의 감염(感染)으로 비롯된 질환(疾患)에 자주 쓰이는 22개(個)의 처방(處方)에 대(對)해 paper disk 법(法)을 사용(使用)하여 항균(抗菌) 효능(效能)을 검색(檢索)하였다. 시료(試料)는 한약(韓藥)의 고용(股用) 방법(方法)을 고려(考慮)하여 물로 추출(抽出)하였으며, 사용(使用) 균주(菌柱)로는 그람 양성균(陽性菌)인 포도상구균(葡萄狀球菌)과 고초균(枯草菌) 그리고 그람 음성균(陰性菌)인 대장균(大腸菌)과 녹농균(綠膿菌)을 사용(使用)하였고, 대조물질(對照物質)로는 tetracycline을 사용(使用)하여 상법(常法)에 의(依)해 실험(實驗)하였다. 22개(個)의 처방(處方) 가운데 백두옹탕(白頭翁湯), 황연해독탕(黃連解毒湯), 증황연황연해독탕(增黃連黃連解毒湯), 사심탕(瀉心湯), 용담사간탕(龍膽瀉肝湯), 선방활명음(仙方活命飮) 등(等)의 처방(處方)이 탁월(卓越)한 항균(抗菌) 활성(活性)을 보였다. 이 가운데 본(本) 연구(硏究)에서는 탕제(湯劑)의 구성(構成) 약재(藥材)가 다른 처방(處方)들에 비(比)해 비교적(比較的) 다양(多樣)한 선방활명음(仙方活命飮)에 대(對)해 활성(活性) 성분(成分)의 규명(糾明) 및 구성(構成) 약재간(藥材間)의 상화작용(相互作用)을 밝히고자 하였다. 선방활명음(仙方活命飮) 5 kg을 메탄올 (MeOH)로 추출(抽出)한 뒤 우수(優秀)한 항균(抗菌) 활성(活性)을 보인 에칠아세테이트 (EtOAc) 분획(分劃)에 대(對)하여 silica gel 및 Sephadex LH-20 column chromatography를 반복(反復)하여 stilbene 계열(系列)의 화합물(化合物)인 Rhapontigenin (Compound 1)과 Rhaponticin (Compound 2)을 얻었다. S. aureus SG 511에 대(對)해 Rhapontigenin은 50 mg/ml 이상(以上) 농도(濃度)에서 항균(抗菌) 효과(效果)를 나타내었고, Rhaponticin은 $200\;mg/m{\ell}$ 농도(濃度)에서 미약(微弱)하게 유효(有效)한 항균(抗菌) 효과(效果)를 나타내었으며, B. subtilis ATCC 6633에 대(對)해 Rhapontigenin은 50 mg/ml 이상(以上) 농도(濃度)에서 항균(抗菌) 효과(效果)를 나타내었고, Rhaponticin은 200 mg/ml 농도(濃度)에서 우수(優秀)한 항균(抗菌) 효과(效果)를 나타내었으며, 100 mg/ml 농도(濃度)에서 미약(微弱)하게 유효(有效)한 항균(抗菌) 효과(效果)를 나타내었다. 또한 E. coli 055에 대(對)해서는 Rhapontigenin과 Rhaponticin 모두 200 mg/ml 농도(濃度)에서 미약(微弱)하게 유효(有效)한 항균(抗菌) 효과(效果)를 나타내었다. 이상(以上)의 결과(結果)로 보아 선방활명음(仙方活命飮)의 항균(抗菌) 효능(效能)은 군약(君藥)인 대황(大黃)의 성분(成分) 중(中)의 하나인 stilbene 계열(系列)의 화합물(化合物)인 Rhapontigenin과 Rhaponticin의 작용(作用)에 의(依)한 것이며, 이는 한의학(韓醫學) 방제(方劑) 원리(原理)인 군신좌사(君臣佐使) 이론(理論)에서 군약(君藥)이 주증(主症)에 주(主)로 작용(作用)하는 약물(藥物)이라는 것을 밝혀주는 것이라고 사료(思料)된다.

• YAKHAK HOEJI
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• v.54 no.1
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• pp.39-48
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• 2010

The objective of this study was to analyze sennoside A and rhaponticin simultaneously according to sennoside A of Rhei Rhizoma determination in Korean Pharmacopoeia. $NaHCO_3$ solution in KP was compared with methanol which usually used as solution to extract rhaponticin in Rhei Rhizoma. The method was validated through the guidelines of linearity, LOD, LOQ, specificity and accuracy. Two solution weren't different about validation parameter and passed. So this method were applied to the determination of 6 commercial Rhei Rhizoma samples and 2 samples were suitable for the legal standards.

• BMB Reports
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• v.54 no.10
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• pp.516-521
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• 2021

Although arginase primarily participates in the last reaction of the urea cycle, we have previously demonstrated that arginase II is an important cytosolic calcium regulator through spermine production in a p32-dependent manner. Here, we demonstrated that rhaponticin (RPT) is a novel medicinal-plant arginase inhibitor and investigated its mechanism of action on Ca²⁺-dependent endothelial nitric oxide synthase (eNOS) activation. RPT was uncompetitively inhibited for both arginases I and II prepared from mouse liver and kidney. It also inhibited arginase activity in both aorta and human umbilical vein endothelial cells (HUVECs). Using both microscope and FACS analyses, RPT treatments induced increases in cytosolic Ca²⁺ levels using Fluo-4 AM as a calcium indicator. Increased cytosolic Ca²⁺ elicited the phosphorylations of both CaMKII and eNOS Ser1177 in a time-dependent manner. RPT incubations also increased intracellular L-arginine (L-Arg) levels and activated the CaMKII/AMPK/Akt/eNOS signaling cascade in HUVECs. Treatment of L-Arg and ABH, arginase inhibitor, increased intracellular Ca²⁺ concentrations and activated CaMKII-dependent eNOS activation in ECs of WT mice, but, the effects were not observed in ECs of inositol triphosphate receptor type 1 knockout (IP3R1^-/-) mice. In the aortic endothelium of WT mice, RPT also augmented nitric oxide (NO) production and attenuated reactive oxygen species (ROS) generation. In a vascular tension assay using RPT-treated aortic tissue, cumulative vasorelaxant responses to acetylcholine (Ach) were enhanced, and phenylephrine (PE)-dependent vasoconstrictive responses were retarded, although sodium nitroprusside and KCl responses were not different. In this study, we present a novel mechanism for RPT, as an arginase inhibitor, to increase cytosolic Ca²⁺ concentration in a L-Arg-dependent manner and enhance endothelial function through eNOS activation.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.154.1-154.1
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• 2000

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.703-706
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• 1998

The anticomplementary activity of stilbenes from medicinal plants in Korea was investigated in vitro. 3,5-Dihydroxy-4'-methoxystilbene (3) was most potent with $IC_{50}$ value of $1.5{\times}10^{-4}M$ followed by rhapontigenin (4), oxyresverastrol (2), 2,3,4',5-tetrahydroxystilbene-2-O-beta-glucoside (9), rhaponticin (8), resverastrol (1), and piceid (7). The activity was found to be increased by a methylation on a hydroxy group of C-4' of 1, but decreased by further methylation on hydroxy groups of C-3 and C-5 and glucosylation on any hydroxy group of 1. Addition of hydroxy group on C-2' of 1 or C-3' of 3 was little affected on the anticomplementary activity but the activity was increased by O-glucosylation on C-2 of 1.

• Korean Journal of Pharmacognosy
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• v.35 no.2 s.137
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• pp.171-174
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• 2004

In order to examine the anti-ohyul (anti-inflammatory) activity of rhubarb, we investigated the effects of stilbene derivatives obtained from rhizomes of Rheum undulatum on the carrageenan-induced hind paw edema in rats. Administration of stilbene aglycon (rhapontigenin) at doses of 50 and 100 mg/kg exhibited the anti- edema effect in dose dependent manner and stilbene glycosides $(rhaponticin,\;piceatannol-3'-O-{\beta}-D-glucopyranoside)$ at a dose of 100 mg/kg also showed inhibitory effect on the carrageenan-induced edema. These inhibitory effects may ascribed, at least in part, to the anti-ohyul activity of rhubarb.

• Food Science and Biotechnology
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• v.18 no.5
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• pp.1284-1287
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• 2009

Tumor necrosis factor (TNF)-${\alpha}$ is chronically elevated in adipose tissues of obese rodents and humans. Increased levels of TNF-${\alpha}$ have been implicated in both the induction of atherogenic adipokines, such as plasminogen activator inhibitor (PAI)-1, and the inhibition of the anti-atherogenic adipokine, adiponectin. In this study, we investigated the effects of trans-stilbene, piceatannol, rhaponticin, and piceid on the TNF-${\alpha}$-induced atherogenic changes of adipokines in 3T3-L1 cells. Exposure to TNF-${\alpha}$ for 24 hr increased PAI-1 secretion and decreased adiponectin secretion. Among stilbenoids, piceatannol significantly inhibited the increased secretion of PAI-1 induced by TNF-${\alpha}$. Adiponectin secretion decreased by TNF-${\alpha}$ was recovered after trans-stilbene and rhaponticin treatments. Our results showed that stilbenoids exerted different effects on TNF-${\alpha}$-induced changes in adipokines secretion in 3T3-L1 adipocytes according to their structural characteristics.