• Title/Summary/Keyword: active compound

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Assessment of the Purity of Emodin by Quantitative Nuclear Magnetic Resonance Spectroscopy and Mass Balance

  • Park, Sojung;Choi, Yu-Jin;Do, Giang Hoang;Seo, Eun Kyoung;Hyun, Seunghun;Lee, Dongho
    • Natural Product Sciences
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    • v.25 no.3
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    • pp.222-227
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    • 2019
  • Quantitative nuclear magnetic resonance (qNMR) is a well-established method adopted by international pharmacopoeia for quantitative and purity analyses. Emodin is a type of anthraquinone, well known as the main active component of Fabaceae, Polygonaceae and Rhamnaceae. Purity analysis of emodin is usually performed by using the high-performance liquid chromatography (HPLC)-UV method. However, it cannot detect impurities such as salts, volatile matter, and trace elements. Using the qNMR method, it is possible to determine the compound content as well as the nature of the impurities. Several experimental parameters were optimized for the quantification, such as relaxation delay, spectral width, number of scans, temperature, pulse width, and acquisition time. The method was validated, and the results of the qNMR method were compared with those obtained by the HPLC and mass balance analysis methods. The qNMR method is specific, rapid, simple, and therefore, a valuable and reliable method for the purity analysis of emodin.

Biological Activity Analysis of Potato-derived Polar Compounds (감자 유래 극성화합물의 생리활성 분석)

  • Kim, Dae Yoon;Nam, Jung Hwan;Lee, Jae Kwon
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.10a
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    • pp.62-62
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    • 2019
  • Natural substances have various physiological activities. Substances isolated from natural substances are known to be safer and more potent than pharmaceuticals. Potatoes not only act as energy sources but also contain active ingredients such as vitamins and minerals. In particular, the potato contains a large amount of polar compounds, including the saponin in the polar compounds, and the physiological activity of the saponins, such as immunity enhancement, antioxidant and anti-inflammatory is known. In this study, the antioxidative activity of polar compounds from five potatoes was examined by chemical base anti-oxidation assay and cell based anti-oxidation assay. In the chemical base anti-oxidation assay, DPPH experiment showed activity in the order of Hongyoung, Haryung, Seohong, Sumi, and Jayoung. In the LPA experiment, IC50 was lower in the order of Jayoung, Seohong, Sumi, Hongyoung, and Haryung. In the cell based anti-oxidation assay, the smallest amount of ROS was generated when the compound was derived from Haryung and hongyoung, and strong SOD activity was observed in Sumi and Jayoung. The results of this study reveal the antioxidative effect of polar compounds extracted from various kind of potatoes, which will enable the acquisition of new bioactive candidates and the establishment of new profit generation models for farmers.

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An Isocoumarin with Hepatoprotective Activity in Hep G2 and Primary Hepatocytes from Agrimonia pilosa

  • Ko, Eun-Kyung;Park, Eun-Jeon;Kim, Mi-Hee;Jun, Jung-Yang;Park, Sung-Uk;Sohn, Dong-Hwan;Kim, Youn-Chul
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.383.1-383.1
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    • 2002
  • In connection with our studies on the isolation of hepatoprotective constituents from natural products. we have recently reported hepatoprotective compounds including phenolic bakuchiol. diarylheptanoids. furocoumarins. In the course of continuing efforts. the aqueous extract of the roots of Agrimonia pilosa Ledeb. (Rosaceae) was found to exhibit promising hepatoprotective activity. A. pilosa is a perennial herb distributed throughout South Korea. and its roots have been used as the hemostatic. antimalarial. and antidysenteric agent in oriental medicine. Chemical investigation of the aqueous extract of the roots of this plant. as guided by hepatoprotective active catechin (2). Compound 1 showed hepatoprotective effects on both tacrine-induced cytotoxicity in human level derived Hep G2 cells and tert-hydroperoxide-induced cytotoxicity in rat primary hepatocyles with $EC_{50}$ values of 66.2 $\pm$ 2.8 and 22.9 $\pm$ 2.6 $\mu\textrm{M}$ respectively.

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Isolation of a starfish myorelaxant peptide (SMP) isotype from the pyloric caeca of Patiria pectinifera

  • Kubarova, Anastasia;Go, Hye-Jin;Park, Nam Gyu
    • Fisheries and Aquatic Sciences
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    • v.24 no.4
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    • pp.163-170
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    • 2021
  • Peptides are naturally occurring biological molecules that are found in all living organisms. These biologically active peptides play a key role in various biological processes. The aim of this study is the extraction and the purification of bioactive materials that induce relaxation of an apical muscle from the pyloric caeca of Patiria pectinifera. The acidified pyloric caeca extract was partially separated by the solid phase extraction using a stepwise gradient on Sep-Pak C18 cartridge. Among the fractions, materials eluted with 60% methanol/0.1% trifluoroacetic acid was put a thorough of a series of high performance liquid chromatography (HPLC) steps to isolate a neuropeptide with relaxation activity. The purified compound was eluted at 28% acetonitrile in 0.1% trifluoroacetic acid with retention time of 25.8 min on the CAPCELL-PAK C18 reversed-phase column. To determine the molecular weight and the amino acid sequence of the purified peptide, LC-MS and Edman degradation method were used, respectively. The primary structure of the peptide was determined to be FGMGGAYDPLSAGFTD which corresponded to the amino acid sequence of a starfish myorelaxant peptide (SMP) isotype (SMPb) found in the cDNA sequence encoding SMPa and its isotypes. In this study, a muscle relaxant neuropeptide (SMPb) has been isolated from pyloric caeca of starfish P. pectinifera. This is the first report of SMPb isolation on the protein level from P. pectinifera.

Functional roles and mechanisms of ginsenosides from Panax ginseng in atherosclerosis

  • Xue, Qianqian;He, Ningning;Wang, Zhibin;Fu, Xiuxiu;Aung, Lynn Htet Htet;Liu, Yan;Li, Min;Cho, Jae Youl;Yang, Yanyan;Yu, Tao
    • Journal of Ginseng Research
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    • v.45 no.1
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    • pp.22-31
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    • 2021
  • Atherosclerosis (AS) is a leading cause of cardiovascular diseases (CVDs) and it results in a high rate of death worldwide, with an increased prevalence with age despite advances in lifestyle management and drug therapy. Atherosclerosis is a chronic progressive inflammatory process, and it mainly presents with lipid accumulation, foam cell proliferation, inflammatory response, atherosclerotic plaque formation and rupture, thrombosis, and vascular calcification. Therefore, there is a great need for reliable therapeutic drugs or remedies to cure or alleviate atherosclerosis and reduce the societal burden. Ginsenosides are natural steroid glycosides and triterpene saponins obtained mainly from the plant ginseng. Several recent studies have reported that ginsenosides have a variety of pharmacological activities against several diseases including inflammation, cancer and cardiovascular diseases. This review focuses on describing the different pharmacological functions and underlying mechanisms of various active ginsenosides (Rb1,-Rd, -F, -Rg1, -Rg2, and -Rg3, and compound K) for atherosclerosis, which could provide useful insights for developing novel and effective anti-cardiovascular drugs.

Chemical Constituents from Agrimonia pilosa with Inhibitory Activity against Interleukin 1β Production via NLRP3 and NLRC4 Inflammasomes

  • Nhoek, Piseth;Chae, Hee-Sung;An, Chae-Yeong;Pel, Pisey;Kim, Young-Mi;Chin, Young-Won
    • Natural Product Sciences
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    • v.27 no.4
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    • pp.228-233
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    • 2021
  • Bioactivity-guided fractionation by preliminary screening using interleukin-1β production in lipopolysaccharides (LPS)-induced J774A.1 cell line led to the isolation of fourteen structures including chromone, isocoumarins, flavanoids, and triterpenes from the aerial part of Agrimonia pilosa Ledeb. All structures were determined by measuring their spectroscopic data and comparing their spectroscopic data with the literatures. All the isolates were tested for their inhibitory activities against interleukin-1β production in LPS-induced J774A.1 cell. Of the tested compounds, (S)-(+)-5,7-dihydroxy-2-(1-methylpropyl)chromone (1), agrimonolide-6-O-β-D-glucopyranoside (5), agrimonolide-6-O-α-L-arabinofuranosyl-(1→6)-β-D-glucopyranoside (6), and catechin (10) were found to be active. Furthermore, compound 1 suppressed the protein expressions of NLRP3 and NLRC4 in murine macrophage.

Ginsenosides are active ingredients in Panax ginseng with immunomodulatory properties from cellular to organismal levels

  • You, Long;Cha, Seunghwa;Kim, Mi-Yeon;Cho, Jae Youl
    • Journal of Ginseng Research
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    • v.46 no.6
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    • pp.711-721
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    • 2022
  • The immune system is one of the most important parts of the human body and immunomodulation is the major function of the immune system. In response to outside pathogens or high inflammation, the immune system is stimulated or suppressed. Thus, identifying effective and potent immunostimulants or immunosuppressants is critical. Ginsenosides are a type of steroid saponin derived from ginseng. Most are harmless to the body and even have tonic effects. In this review, we mainly focus on the immunostimulatory and immunosuppressive roles of two types ginsenosides: the protopanaxadiol (PPD)-type and protopanaxatriol (PPT)-type. PPT-type ginsenosides include Rg1, Rg2, Rh4, Re and notoginsenoside R1, and PPD-type ginsenosides include Rg3, Rh2, Rb1, Rb2, Rc, Rd, compound K (CK) and PPD, which activate the immune responses. In addition, Rg1 and Rg6 belong to PPT-type ginsenosides and together with Rg3, Rb1, Rd, CK show immunosuppressive properties. Current explorations of ginsenosides in immunological areas are in the preliminary stages. Therefore, this review may provide some novel ideas to researchers who study the immunoregulatory roles of ginsenosides.

Neogambogic acid relieves myocardial injury induced by sepsis via p38 MAPK/NF-κB pathway

  • Fu, Wei;Fang, Xiaowei;Wu, Lidong;Hu, Weijuan;Yang, Tao
    • The Korean Journal of Physiology and Pharmacology
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    • v.26 no.6
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    • pp.511-518
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    • 2022
  • Sepsis-associated myocardial injury, an invertible myocardial depression, is a common complication of sepsis. Neogambogic acid is an active compound in garcinia and exerts anthelmintic, anti-inflammatory, and detoxification properties. The role of neogambogic acid in sepsis-associated myocardial injury was assessed. Firstly, mice were pretreated with neogambogic acid and then subjected to lipopolysaccharide treatment to induce sepsis. Results showed that lipopolysaccharide treatment induced up-regulation of biomarkers involved in cardiac injury, including lactate dehydrogenase (LDH), creatine kinase-MB (CK-MB), and troponin I (cTnI). However, pretreatment with neogambogic acid reduced levels of LDH, CK-MB, and cTnI, and ameliorated histopathological changes in the heart tissues of septic mice. Secondly, neogambogic acid also improved cardiac function in septic mice through reduction in left ventricular end-diastolic pressure, and enhancement of ejection fraction, fractional shortening, and left ventricular systolic mean pressure. Moreover, neogambogic acid suppressed cardiac apoptosis and inflammation in septic mice and reduced cardiac fibrosis. Lastly, protein expression of p-p38, p-JNK, and p-NF-κB in septic mice was decreased by neogambogic acid. In conclusion, neogambogic acid exerted anti-apoptotic, anti-fibrotic, and anti-inflammatory effects in septic mice through the inactivation of MAPK/NF-κB pathway.

Idiopathic infantile hypercalcemia with severe nephrocalcinosis, associated with CYP24A1 mutations: a case report

  • Yoo, Jeesun;Kang, Hee Gyung;Ahn, Yo Han
    • Childhood Kidney Diseases
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    • v.26 no.1
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    • pp.63-67
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    • 2022
  • Nephrocalcinosis often occurs in infants and is caused by excessive calcium or vitamin D supplementation, neonatal primary hyperparathyroidism, and genetic disorders. Idiopathic infantile hypercalcemia (IIH), a rare cause of nephrocalcinosis, results from genetic defects in CYP24A1 or SLC34A1. Mutations in CYP24A1, which encodes 25-hydroxyvitamin D 24-hydroxylase, disrupt active vitamin D degradation. IIH clinically manifests as failure to thrive and hypercalcemia within the first year of life and usually remits spontaneously. Herein, we present a case of IIH wih CYP24A1 mutations. An 11-month-old girl visited our hospital with incidental hypercalcemia. She showed failure to thrive, and her oral intake had decreased over time since the age of 6 months. Her initial serum parathyroid hormone level was low, 25-OH vitamin D and 1,25(OH)2 vitamin D levels were normal, and renal ultrasonography showed bilateral nephrocalcinosis. Whole-exome sequencing revealed compound heterozygous variants in CYP24A1 (NM_000782.4:c.376C>T [p.Pro126Ser] and c.1310C>A [p.Pro437His]). Although her hypercalcemia and poor oral intake spontaneously resolved in approximately 8 months, we suggested that her nephrocalcinosis and renal function be regularly checked in consideration of potential asymptomatic renal damage. Hypercalcemia caused by IIH should be suspected in infants with severe nephrocalcinosis, especially when presenting with failure to thrive.

Xanthones and 4-Phenylcoumarins from the Twigs of Mesua beccariana (Baill.) Kosterm

  • Mulyadi Tanjung;Tjitjik Srie Tjahjandarie;Muhammad Fajar Aldin;Shola Mardhiyyah;Ishomatul Maqfiroh;Ratih Dewi Saputri;Norizan Ahmat
    • Natural Product Sciences
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    • v.29 no.1
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    • pp.38-41
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    • 2023
  • Two xanthones and 4-phenylcoumarins were isolated from the twigs of Mesua beccariana (Baill.) Kosterm. Among them, one new xanthone, beccarianin A (1), along with 7-isoprenyl-jacareubin (2), mammea A/AA cyclo F (3), and mammea A/BA cyclo F (4). These structures were determined by spectrometric and spectroscopic methods, HRESIMS data, NMR, and UV spectra. Two xanthones (1-2) and two 4-phenylcoumarins (3-4) were evaluated for their cytotoxic effect on the HeLa cells. Compound 1 showed active activity (IC50 = 8.2 µM), and compounds 3-4 showed moderate activity (IC50 = 12.3 and 15.6 µM, respectively).