• Title/Summary/Keyword: pharmacognosy

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In-silico Studies of Boerhavia diffusa (Purnarnava) Phytoconstituents as ACE II Inhibitor: Strategies to Combat COVID-19 and Associated Diseases

  • Rahul Maurya;Thirupataiah Boini;Lakshminarayana Misro;Thulasi Radhakrishnan
    • Natural Product Sciences
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    • v.29 no.2
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    • pp.104-112
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    • 2023
  • COVID-19 caused a catastrophe in human health. People infected with COVID-19 also suffer from various clinical illnesses during and after the infection. The Boerhavia diffusa plant is well known for its antihypertensive activity. ACE-II inhibitors and calcium channel blockers are reported as mechanisms for the antihypertensive activity of B. diffusa phytoconstituents. Various studies have said ACE-II is the virus's binding site to attack host cells. COVID-19 treatment commonly employs a variety of synthetic antiviral and steroidal drugs. As a result, other clinical illnesses, such as hypertension and hyperglycemia, emerge as serious complications. Safe and effective drug delivery is a prime objective of the drug development process. COVID-19 is treated with various herbal treatments; however, they are not widely used due to their low potency. Many herbal plants and formulations are used to treat COVID-19 infection, in which B. diffusa is the most widely used plant. The current study relies on discovering active phytoconstituents with ACE-II inhibitory activity in the B. diffusa plant. As a result, it can be used as a treatment option for patients with COVID-19 and related diseases. Different phytoconstituents of the B. diffusa plant were selected from the reported literature. The activity of phytoconstituents against ACE-II proteins has been studied. Molecular docking and ligand-protein interaction computation tools are used in the in-silico experiment. Physicochemical, drug-likeness, water solubility, lipophilicity, and pharmacokinetic parameters are used to evaluate phytoconstituents. Liriodenine has the best drug-likeness, bioactivity, and binding score characteristics among the selected ligands. The in-silico study aims to find the therapeutic potential of B. diffusa phytoconstituents against ACE-II. Targeting ACE-II also shows an effect against SARS-CoV-2. It can serve as a rationale for designing a drug for patient infected with COVID-19 and associated diseases.

Effects of 3,5-di-O-Caffeoylquinic acid from Artemisia scoparia Waldstein et Kitamura on the Function of HPV 16 Oncoproteins (인진에서 분리한 3,5-di-O-Caffeoylquinic acid가 자궁경부암 바이러스 발암단백질의 기능에 미치는 영향)

  • Baek, Tae-Woong;Lee, Kyung-Ae;Ahn, Min-Jung;Joo, Hae-Kyung;Cho, Min-Chul;Kang, Jung-Woo;Kim, Hee-Seo;Shim, Jung-Hyun;Lee, Hee-Gu;Oh, Hyun-Cheol;Ahn, Jong-Seok;Cho, Yong-Kwen;Myung, Pyung-Keun;Yoon, Do-Young
    • Korean Journal of Pharmacognosy
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    • v.35 no.4 s.139
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    • pp.368-374
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    • 2004
  • Cervical cancer is one of the leading causes of female death. Viral oncoproteins E6 and E7 are selectively retained and expressed in carcinoma cells infected with HPV (Human papillomavirus) type 16. The HPV is cooperated in immotalization and transformation of primary keratinocyte. E6 and E7 oncoproteins interfere the functions of tumor suppressor proteins p53 and retinoblasoma protein (pRb), respectively. Among a lots of natural products, Artemisia scoparia Waldstein et Kitamura has inhibitory effects on the binding between E6 oncoprotein and tumor suppressor p53, or the binding between E6 and E6 associated protein (E6AP), an E3 ubiquitin-protein ligase. HPV oncoprotein inhibitors from Artemisia scoparia W. were isolated by solvent partition and column chromatography (Silica gel, RP-18) and the inhibitory compounds were finally purified by HPLC using an ELISA screening system based on the binding between E6 and E6AP. The aim of this study is to identify the structure of inhibitory compounds and to investigate whether these compounds have inhibitory effects on the functions of E6 oncoprotein. We investigated whether 3,5-di-O-caffeoylquinic acid (DCQA) extracted from Artemisia scoparia W. Could inhibit the function of E6 oncoprutein. DCQA inhibited the in vitro binding of E6 and E6AP which are essential for the binding and degradation of the tumor suppressor p53 and also inhibited the proliferation of human cervical cancer cell lines (SiHa and CaSKi) in a dose response manner. These results suggest that DCQA inhibited the function of E6 oncoprotein, suggesting that it can be used as a potential drug for the treatment of cervical cancers infected with HPV.

Current Status of Korean Ginseng Research (한국인삼론(韓國人蔘論))

  • Han, Byung-Hoon
    • Korean Journal of Pharmacognosy
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    • v.3 no.3
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    • pp.151-160
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    • 1972
  • Recent achievements of scientific research on the pharmacologic activities and the chemical problems of dammalene glycosides, which are considered to be effective principles of Korean ginseng, are reviewed and analyzed in view of structure-activity relationship. 1) S. Shibata and his co-workers detected 12 glycoside spots of dammalene series on the two dimensional T.L.C. of total glycoside fraction from Japanese ginseng, and designated them Ginsenoside Rx(x=a, b, c, g, h, etc.) in the order of increasing Rf-value. The aglycones of those glycosides were characterized to be protopanaxadiol for the Ginsenoside $Rx(x=a,\;b_{1},\;b_{2},\;c,\;d,\;e,\;f)$ and protopanaxatriol for the Ginsenoside $Rx(x=g_{1},\;g_{2},\;g_{3},\;h_{1}\;'h_{2})$. Using Korean ginseng as the material for our study, the author and his coworkers isolated a new dammalene glycoside(Panax Saponin C), which comes under the category of protopanaxadiol glycosides based on the classification of S. Shibata et al., and characterized this saponin to be the glycoside of protopanaxatriol series. Furthermore, Panax Saponin C dissociated into $two\;components(C_{1}\;and\;C_{2}-acetate)$ by acetylation, both of which returned to original Panax Saponin C by deacetylation. Based on this result, more than 13 glycoside components of dammalene series will be expected in the Korean ginseng. 2) The structures of protopanaxadiol and protopanaxatriol, the genuine aglycones of dammalene glycosides, are fully established to be structural analogues by S. Shibata and his co-workers, therefore antagonistic and/or analogical activities will be expected for the pharmacologic activities of these glycoside series of structural analogues. K. Takaki and his co-workers found central nervous system (CNS) stimmulant activity from the glycosides of protopanaxatriol series and CNS-depressant activity from the glycosides of protopanaxadiol series. On the other hand, the author and his co-workers found stimmulating activity on the protein synthesis from both the series of dammalene glycosides with delayed and long-lasting characteristics. This delayed and long-lasting characteristics were also observed in the anti-inflammatory activity of glycosides of protopanaxatriol series on their time course tendency. For the convenience's sake of argument, pluralistic pharmacologic activities of dammalene glycosides, which were observed by many workers at various pharmacologic site, may be classified into two main categories; one is pan-cellular activity and the other is organ specific activity to the certain tissue which is a mass of cells differentiated to a certain direction for their special functions in the body. Based on the data of K. Takaki and those of the authors, following assumption will be probable; Pharmacologic activities of both series of glycosides of protopanaxadiol and protopanaxatriol aglycones may be antagonistic on their tissue-specific activities and analogic on their pan-cellular activities. Therefore, the mixture of these two series of glycosides in an appropriate ratio, as the case of total extract of Korean ginseng, will be probably beneficial to the host by increasing the synthesis of some functional proteins, due to the additive action of pan-cellular activity, and with the disappearance of any significant behavioral symptoms due to the antagonism of tissue specific activity. This fact will probably be the main reason why classical trials of pharmacologists failed in re-discovering the efficacy of Korean ginseng with their behavioral test. 3) The author and his co-workers achieved the synthesis of $C^{14}-labelled\;Panax\;Saponin\;A\;on\;C_{25}-C_{27}\;position\;of\;aglycone$ in the interest of tracer studies in vivo. The method will be applicable to other dammalene glycosides regardless of their chemical structure. 4) The author and his co-workers converted chemically betulafolienetriol, a triterpene component of Betula platyphylla, to the protopanaxadiol, one of genuine aglycone of dammalene glycosides.

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Effects of Herbal Complex on Blood Glucose in Streptozotocin-induced Diabetic Rats and in Mice Model of Metabolic Syndrome (생약복합제의 Streptozotocin 유발 당뇨 및 대사성증후군 모델 동물에서의 혈당에 미치는 효과)

  • Park, Han-Seok;Lee, Yeon-Sil;Choi, Se-Jin;Kim, Jin-Kyu;Lee, Yun-Lyul;Kim, Hyun-Gwen;Koo, Sam-Hoi;Ku, Dae-Hoy;Ki, Seung-Il;Lim, Soon-Sung
    • Korean Journal of Pharmacognosy
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    • v.40 no.3
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    • pp.196-204
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    • 2009
  • This study was carried out to investigate the in vivo and in vitro inhibitory effect of a traditional herbal complex (HC) extract prepared from a mixture of four oriental herbs (Dioscorea Rhizoma, Glycine soja Sieb. et Zucc, Bombycis corpus, Fermented Glycine soja) that have been widely used for the treatment and prevention of diabetes mellitus on hyperglycemia. The water extract of HC showed potent inhibitory effect on $\alpha$-glucosidase with $IC_{50}$ value of 1.24 mg/mL. Additionally, the ethanol extract of HC was also found to exhibit significant inhibitory effect against protein tyrosine phosphatase $1{\beta}$ ($PTP1{\beta}$), which is known as a major regulator of both insulin and leptin signaling. In the $PTP1{\beta}$ inhibitory assay, the most active n-hexane fraction obtained from the ethanol extract of HC, was identified as a mixture of fatty acid derivatives by gas chromatography-mass spectrometry (GC-MS). In high-fat diet-low dose streptozotocin (STZ)-induced diabetic rat, the water extract of HC improved the oral glucose intolerance as compared with rosiglitazone. HC also caused a marked decrease of body weight and fasting blood glucose and a significant improvement on glucose tolerance in metabolic syndrome mice model. These findings support that this traditional HC may be useful in the control of blood glucose in diabetes mellitus and metabolic syndrome.

A New Forma of Acanthopanax Species(I) (신품종(新品種)을 포함한 한국산(韓國産) Acanthopanax속(屬)의 분류(分類)(I))

  • Yook, Chang-Soo;Lee, Dong-Ho;Seo, Yoon-Kyo
    • Korean Journal of Pharmacognosy
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    • v.7 no.3
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    • pp.179-190
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    • 1976
  • 1. The Korean Acanthopanax genus includes 12 kinds consisting of 9 species and 3 forma. 2. The Korean Oga-pi which is on market sale has been used as bark for the medicinal purpose, and Oga-pi shall use Radicis Cortex. That is why it is basic rule that herbalogy shall use Radicis Cortex. 3. The origin of Oga-pi on sale is Acanthopanax sessiliflorum forma chungbunensis C.S. Yook. 4. $C_{HUNG}\;and\;N_AKAI'S}$ report on A. koreanum told us that there are brown hair on the mid-leaf junction, but in addition to it, our investigation was resulted in the fact that there are thorn along mid-rib sometimes. 5. 2 kinds of new forma are similar to A. sessiliflorum, but are different in the view-point of chemotaxonomy, compared with A. sessiliflorum. In its morphology, we can find some difference between 2 kinds of new forma and A. sessiliflorum. Our effort of examination on documents tell us that the all plants growing in the central part of our country is A. sessiliflorum forma chungbunensis C.S. Yook. The one which has thorn on both side among the plants collected in Mt. Dukyu, is called A. sessiliflorum forma nambunensis C.S. Yook. 6. A. sessiliflorum is growing in the southern part in Korea, and most Chungbu Oga-pi A. sessiliflorum forma chungbunensis in the central part of our country. For the convenience of our study, the key of Korean Acanthopanax plant is classified into, I-IV, as shown on the following items: I. No hair on both side of leaf A. Flower stalk is longer than petiole, and there are thorn under the petiole (5-7 stigma).${\cdots}A.\;sieboldianum$. B. Flower stalk is longer than petiole, or same length. The serration lie down, and the stem has short thorn (stigma is divided into 3 part).${\cdots\;\cdots}A.\;seoulense$ II. There are a lot of thorn or hair on back of leaf. A. A lot of thorn and hair on the vein of leaf back, and a number of small thorn on petiole.${\cdots}A.\;chiisanensis$. B. There are thorn on the vein of leaf back.${\cdots\;\cdots}A.\;sessiliflorum\;forma\;chungbunensis.$ III. There are hairs on both side of leaf. A. There are small hairs on the back of leaf.${\cdots\;\cdots}A.\;sessiliflorum.$ B. There are small hairs on both side of leaf.${\cdots\;\cdots}A.\;sessiliflorum\;f.\;nambunensis.$ C. There are thick hairs on junction of main vein on back of leaf.${\cdots\;\cdots}A.\;koreanum.$ D. There are brown hairs on vein of leaf back, and brown hairs on small petiole.${\cdots\;\cdots}A.\;rufinerve.$ E. There are shrunk hairs in grey-brown on back of leaf, and tense hairs on new branch (one stigma).${\cdots\;\cdots}A.\;divaricatum.$ IV. There are long thorn, just like needles, on the stem and petiole. A. Long needle grows on whole stem tensely, and long needles on petiole.${\cdots\;\cdots}A.\;senticosus.$ B. There are no needles, just like needles aid hairs on petiole, and needles grow on the stem thinly.${\cdots\;\cdots}A.\;asperatus.$ C. There are no needle on small brarch, leaf and inflorescence are larger than A. senticosus. ${\cdots\;\cdots}A.\;senticosus\;forma\;inermis.$.

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Comparative Study on Biological Activities and Ingredient Contents of Different Solvent Extracts of Samchulkunbi-tang (삼출건비탕의 추출용매에 따른 성분 함량 및 효능 비교 연구)

  • Jin, Seong Eun;Seo, Chang-Seob;Ha, Hyekyung;Lim, Hye-Sun;Kim, Yeji;Jeon, Woo-Young;Yoo, Sae-Rom;Kim, Jung-Hoon;Shin, In-Sik;Kim, Seong-Sil;Shin, Na Ra;Lee, Mee-Young;Jeong, Soo-Jin;Kim, Ohn Soon;Shin, Hyeun-Kyoo
    • Korean Journal of Pharmacognosy
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    • v.43 no.4
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    • pp.328-337
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    • 2012
  • In order to investigate anti-inflammatory, anti-allergic and anti-obesity activities of Samchulkunbi-tang (SCT; Shen zhu jian pi-tang) water and 70% ethanol (EtOH) extracts, in vitro inhibitory activities against nitric oxide (NO), prostaglandin $E_2$ $PGE_2$), interleukin (IL)-6 and tumor necrosis factor (TNF)-${\alpha}$ production in lipopolysaccharide-stimulated RAW 264.7 cells, and macrophage-derived chemokine (MDC/CCL22) and regulated on activation of normal T-cell-expressed and -secreted (RANTES/CCL5) production in TNF-${\alpha}$/interferon-${\gamma}$-stimulated HaCaT and BEAS-2B cells as well as glycerol-3-phosphate dehydrogenase (GPDH) activity and leptin production in 3T3-L1 cells were determined. A HPLC was used for quantification of the seven marker components (albiflorin, paeoniflorin, liquiritin, naringin, hesperidin, poncirin and glycyrrhizin) of SCT water and 70% EtOH extracts. SCT showed inhibitory effects against MDC and RANTES production in HaCaT cells, as well as RANTES production in BEAS-2B cells. In addition, SCT reduced not only NO, $PGE_2$, IL-6 and TNF-${\alpha}$ production in RAW 264.7 cells, but also GPDH activity and leptin production in 3T3-L1 cells. Furthermore, the biological activities and the contents of six compounds (except paeoniflorin) were higher in 70% EtOH extract than water extract. These results suggest that SCT has anti-inflammatory, anti-allergic and anti-obesity activities. These efficacies of 70% EtOH extract are relatively higher than that of water extract.

Effects of Natural Product on the Inhibition of $5{\alpha}-Reductase$ Type 2 for the Development of Chemopreventive Agents in LNCaP Cells

  • Lee, Sung-Jin;Kim, Kyeong-Ho;Cho, Myung-Haing;Lee, Sang-Kook;Mar, Woong-Chon
    • Natural Product Sciences
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    • v.5 no.2
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    • pp.97-103
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    • 1999
  • The enzyme steroid $5{\alpha}-reductase$ is responsible for the conversion of testosterone into the most potent androgen dihydrotestosterone (DHT). In man, this steroid acts on a variety of androgen-responsive target tissues to mediate such diverse endocrine processes as male sexual differentiation in the fetus and prostatic growth in men. Androgen levels in the prostate may influence carcinogenesis in this organ. The use of a $5{\alpha}-reductase$ inhibitor, finasteride, in the chemoprevention of prostate cancer is being evaluated in a clinical trial and have been used successfully for treatment of benign prostatic hyperplasia. Therefore, for the discovery of $5{\alpha}-reductase$ type 2 inhibitors, we have evaluated the inhibitory effects of solvent fractionated extracts of natural products on $5{\alpha}-reductase$ type 2 activity. We have tested approximately 80 kinds of natural products after partition into n-hexane, ethyl acetate and aqueous layers from 100% methanol extracts of plants. The ethyl acetate fractions of Perilla sikokiana $(seed,\;IC_{50}\;:\;6.2\;ug/ml)$, Sophora flavescens $(root,\;IC_{50}\;:\;8.9\;ug/ml)$, and Angelica tenuissima $(root,\;IC_{50}\;:\;11.7\;ug/ml)$ revealed inhibitory effects on $5{\alpha}-reductase$ 2 activity in LNCaP cells. The effective ethyl acetate fractions of Perilla sikokiana, Sophora flavescens, Hydnocarpus anthelmintica, and Angelica tenuissima were subfractionated by column chromatography and tested. The subfractions $F4\;(IC_{50}\;:\;1.1\;ug/ml),\;F5\;(IC_{50}\;:\;2.0\;ug/ml),\;and\;F6\;(IC_{50}\;:\;5.8\;ug/ml)$ of the ethyl acetate fraction of Perilla sikokiana and the subfraction $F8\;(IC_{50}\;:\;5.3\;ug/ml)$ of the ethyl acetate fraction of Sophora flavescens displayed greater inhibition of $5{\alpha}-reductase$ type 2 than did finasteride in LNCaP cells. These active fractions are under the process of further sequential fractionation to find the effective pure compounds against $5{\alpha}-reductase$ 2 activity.

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The Chemical Quality Properties during Processing Treatment of Brown Rice Varieties with Different Amylose Content (아밀로오스 함량이 다른 현미의 품종별 가공 처리에 따른 화학적 품질 특성)

  • Lee, Jong-Gu;Kwon, Kwang-Il;Choi, Ji-Young;Choi, Jong-Dong;Choung, Myoung-Gun;Im, Moo-Hyeog
    • Journal of Applied Biological Chemistry
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    • v.53 no.1
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    • pp.37-43
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    • 2010
  • This study was carried out to determine the chemical quality properties during processing treatment using the brown rice varieties with different amylose content. It was investigated using Hwaseonchalbyeo, Baegjinjubyeo, Ilpumbyeo and Goamibyeo varieties. As for the chemical properties of fried brown rice, phenolic compounds increased by the frying treatment. The component of aroma after the frying treatment, it showed that aldehydes sorts of benzaldehyde, phenylmethanal had the highest content. The content of vitamin B group during parboiling treatment and frying treatment decreased as a whole than the non-treatment brown rice. The higher the content of amylose was, the more the content of vitamin $B_2$ increased. The higher the content of amylose was, the more the content of vitamin $B_6$ and mineral contents decreased. The component of mineral during frying treatment, it showed that Mg had the highest content. The higher the content of amylose increased, the more the blue value increased. The 2,2-diphenyl-$\beta$-picryl-hydrazyl (DPPH) after the frying treatment was relatively increased.

Isolation and Development of Quantification Method for Cyanidin-3-Glucoside and Cyanidin-3-Rutinoside in Mulberry Fruit by High-Performance Countercurrent Chromatography and High-Performance Liquid Chromatography

  • Choi, Soo-Jung;Jeon, Heejin;Lee, Chang Uk;Yoon, Shin Hee;Bae, Soo Kyung;Chin, Young-Won;Yoon, Kee Dong
    • Natural Product Sciences
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    • v.21 no.1
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    • pp.20-24
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    • 2015
  • Cyanidin-3-glucoside (C3G) and cyanidin-3-rutinoside (C3R) were isolated by high-performance countercurrent chromatography (HPCCC) using a two-phase solvent system composed of tert-butyl methyl ether/n-butanol/acetonitrile/water/trifluoroacetic acid (1 : 3 : 1 : 5 : 0.01, v/v) to give pure C3G (34.1 mg) and C3R (14.3 mg) from 1.5 g crude mulberry fruit extract. Using the pure C3G and C3R, a reliable high-performance liquid chromatography (HPLC) method was developed and validated to determine the C3G and C3R contents in mulberry fruit. C3G and C3R were separated simultaneously using an Eclipse XDB-C18 column ($4.6{\times}250mm$ I.D., $5{\mu}m$) coupled with a photodiode array detector (PDA). The gradient elution of the mobile phase consisting of acetonitrile (0.5% formic acid) and water (0.5% formic acid) was applied (1.0 mL/min), and the detection wavelength was 520 nm. The calibration curves of C3G and C3R showed good linearity (both with $r^2=0.9996$) in the concentration range $15.625-500{\mu}g/mL$, and the relative standard deviations (RSD%) of intra- and inter-day variability were in the ranges 2.1 - 8.2% and 4.1 - 17.1%, respectively. The accuracies were ranged 96.5 - 102.6% for C3G and C3R, respectively. The developed HPLC method was used to determine the contents of C3G and C3R in newly harvested mulberry from eight different provinces of Korea.

Development of Gradient Centrifugal Partition Chromatography Method and Its Application for the Isolation of 3,5-Dimethoxyphenanthrene-2,7-diol and Batatasin-I from Dioscorea opposita

  • Yoon, Kee-Dong;Yang, Min-Hye;Chin, Young-Won;Kim, Yoen-Jun;Kim, Hye-Ryung;Choi, Ki-Ri;Park, Ju-Hyun;Kim, Jin-Woong
    • Natural Product Sciences
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    • v.15 no.3
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    • pp.144-150
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    • 2009
  • Gradient centrifugal partition chromatography (GCPC) method was developed and applied to isolate 3,5-dimethoxyphenanthrene-2,7-diol (DMP) and batatasin-I (BA-I) from the dichloromethane soluble extract of Dioscorea opposita. In this method, the lower phase of n-hexane-methanol-water system (HMW, 10 : 9 : 1, v/v) was used as a mobile phase A (MpA) and water was used as a mobile phase B (MpB). This gradient CPC method is comparable to that of reversed-phase HPLC method in that the stationary upper-phase of HMW (10 : 9 : 1 v/v) works as if it were reversed-phase silica gel due to its hydrophobic property, while the lower phase (MpA) and water (MpB) functioned as hydrophilic mobile phases. The initial condition of the mobile phase was 20% MpA/80% MpB and maintained for 150 min to obtain DMP (1.2 mg), and then MpA was increased up to 50% to elute BA-I (1.7 mg). The purities of DMP and BA-I were 94.1% and 98.3% with the recovery yields of 83% and 86%, respectively. Similar results were obtained by linear-gradient CPC. The CPC peak fractions were identified by comparing their retention time to those of authentic samples of DMP and BA-I and their spectroscopic data ($^1$H NMR and $^{13}$C NMR) to those of literature values.