• Title/Summary/Keyword: alkaloids$

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Screening of novel alkaloid inhibitors for vascular endothelial growth factor in cancer cells: an integrated computational approach

  • Shahik, Shah Md.;Salauddin, Asma;Hossain, Md. Shakhawat;Noyon, Sajjad Hossain;Moin, Abu Tayab;Mizan, Shagufta;Raza, Md. Thosif
    • Genomics & Informatics
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    • v.19 no.1
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    • pp.6.1-6.10
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    • 2021
  • Vascular endothelial growth factor (VEGF) is expressed at elevated levels by most cancer cells, which can stimulate vascular endothelial cell growth, survival, proliferation as well as trigger angiogenesis modulated by VEGF and VEGFR (a tyrosine kinase receptor) signaling. The angiogenic effects of the VEGF family are thought to be primarily mediated through the interaction of VEGF with VEGFR-2. Targeting this signaling molecule and its receptor is a novel approach for blocking angiogenesis. In recent years virtual high throughput screening has emerged as a widely accepted powerful technique in the identification of novel and diverse leads. The high resolution X-ray structure of VEGF has paved the way to introduce new small molecular inhibitors by structure-based virtual screening. In this study using different alkaloid molecules as potential novel inhibitors of VEGF, we proposed three alkaloid candidates for inhibiting VEGF and VEGFR mediated angiogenesis. As these three alkaloid compounds exhibited high scoring functions, which also highlights their high binding ability, it is evident that these alkaloids can be taken to further drug development pipelines for use as novel lead compounds to design new and effective drugs against cancer.

Discrimination of biological and artificial nicotine in e-liquid

  • Hyoung-Joon Park;Heesung Moon;Min Kyoung Lee;Min Soo Kim;Seok Heo;Chang-Yong Yoon;Sunyoung Baek
    • Analytical Science and Technology
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    • v.36 no.1
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    • pp.22-31
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    • 2023
  • As the use of e-liquid cigarettes is rapidly increasing worldwide, it multiplies the potential risk undisclosed to the health of non- and smokers. To reduce the hazard, each country has its own set of regulations for controlling e-liquids. In Korea, the narrow definition of tobacco makes it difficult and have been steadily occurring tax evasion exploiting the difference in natural and artificial nicotine. Therefore, it is very important to distinguish source of nicotine for their regulation. To find biochemical discriminant markers, this study established analysis methods based on high-performance liquid chromatography coupled with diode array detector (HPLC-DAD) and high-performance liquid chromatography coupled with triple Quadrupole mass spectrometry (HPLC-MS/MS) for nicotine enantiomers and tobacco alkaloids targeted using the difference in pathways of nicotine biosynthesis and chemical synthesis. The method was validated by experimenting linearity (R2 > 0.999), recovery (80.99-108.41 %), accuracy (94.11-109.73 %) and precision (0.04-8.27 %). Then, the results for discrimination of the nicotine obtained from analysis of 65 commercial e-liquid products available in Korean market was evaluated. The method successfully applied to the e-liquids and one sample labelled 'synthetic nicotine' for tax exemption was found to contain a natural nicotine product. This method can be used to determine whether an e-liquid product uses natural or artificial nicotine and monitor non-taxable e-liquid products. The method is more scientific than the existing one, which relies only on field evidence.

Pathogen, Insect and Weed Control Effects of Secondary Metabolites from Plants (식물유래 2차 대사물질의 병충해 및 잡초 방제효과)

  • Kim, Jong-Bum
    • Applied Biological Chemistry
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    • v.48 no.1
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    • pp.1-15
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    • 2005
  • Pathogens, insects and weeds have significantly reduced agricultural productivity. Thus, to increase the productivity, synthetic agricultural chemicals have been overused. However, these synthetic compounds that are different from natural products cannot be broken down easily in natural systems, causing the destruction of soil quality and agricultural environments and the gradually difficulty in continuous agriculture. Now agriculture is faced with the various problems of minimizing the damage in agricultural environments, securing the safety of human health, while simultaneously increasing agricultural productivity. Meanwhile, plants produce secondary metabolites to protect themselves from external invaders and to secure their region for survival. Plants infected with pathogens produce antibiotics phytoalexin; monocotyledonous plants produce flavonoids and diterpenoids phytoalexins, and dicotylodoneous plant, despite of infected pathogens, produce family-specific phytoalexin such as flavonoids in Leguminosae, indole derivatives in Cruciferae, sesquitepenoids in Solanaceae, coumarins in Umbelliferae, making the plant resistant to specific pathogen. Growth inhibitor or antifeedant substances to insects are terpenoids pyrethrin, azadirachtin, limonin, cedrelanoid, toosendanin and fraxinellone/dictamnine, and terpenoid-alkaloid mixed compounds sesquiterpene pyridine and norditerpenoids, and azepine-, amide-, loline-, stemofoline-, pyrrolizidine-alkaloids and so on. Also plants produces the substances to inhibit other plant growths to secure the regions for plant itself, which is including terpenoids essential oil and sesquiterpene lactone, and additionally, benzoxazinoids, glucosinolate, quassinoid, cyanogenic glycoside, saponin, sorgolennone, juglone and lots of other different of secondary metabolites. Hence, phytoalexin, an antibiotic compound produced by plants infected with pathogens, can be employed for pathogen control. Terpenoids and alkaloids inhibiting insect growth can be utilized for insect control. Allelochemicals, a compound released from a certain plant to hinder the growth of other plants for their survival, can be also used directly as a herbicides for weed control as well. Therefore, the use of the natural secondary metabolites for pest control might be one of the alternatives for environmentally friendly agriculture. However, the natural substances are destroyed easily causing low the pest-control efficacy, and also there is the limitation to producing the substances using plant cell. In the future, effects should be made to try to find the secondary metabolites with good pest-control effect and no harmful to human health. Also the biosynthetic pathways of secondary metabolites have to be elucidated continuously, and the metabolic engineering should be applied to improve transgenics having the resistance to specific pest.

Development of Analytical Method for Ergot Alkaloids in Foods Using Liquid Chromatoraphy-Tandem Mass Spectrometry (LC-MS/MS를 이용한 식품 중 맥각 알칼로이드 시험법 개발)

  • Chun, So Young;Chong, Euna;Lee, Bomnae;Kwon, Jin-Wook;Park, Hye Young;Kim, Sheenhee;Gang, Giljin
    • Journal of Food Hygiene and Safety
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    • v.34 no.2
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    • pp.158-169
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    • 2019
  • Ergot alkaloids are mycotoxin produced by fungi of the Claviceps genus, mainly by Claviceps purpurea in EU. Recently obtained informations indicates necessity for control the ergot in imported grains. Recent occurrence data of ergot alkaloids from EU countries indicate the necessities of management and control these toxins from the imported grains like rye, wheat, oat etc. The aim of this study is to optimize the liquid chromatography-tandem mass spectrometry method for determination of ergot alkaloids (ergometrine, ergosine, ergotamine, ergocornine, ergocryptine, ergocristine and their epimers (-inines) from grain and grain-based food. The test method was optimized by extracting the sample with acetonitrile containing 2 mM ammonium carbonate, purification with Mycosep cartridge, and instrumental analysis by LC-MS/MS using Syncronis C18 column. The standard calibration curves showed linearity with correlation coefficents; $R^2$ >0.99. Mean recoveries ranged from 72.0 to 111.3% at three different fortified levels (20, 50, and $100{\mu}g/kg$). The correlation coefficient expressed as precision was within the range of 1.9-12.9%. The limit or quantifications (LOQ) ranged from 0.012 to $0.058{\mu}g/kg$. The developed analytical method met the criteria of AOAC Int. and CAC validation parameters like accuracy and sensitivity. As a result, it was confirmed that the test method developed in this study is suitable for the simultaneous analysis of six species of ergot alkaloid from grains and grain products.

Monoamine Oxidase Inhibitor from Uncaria rhynchophylla

  • Hong, Seong-Su;Han, Xiang Hua;Park, So-Young;Choi, Woo-Hoi;Lee, Myung-Koo;Hur, Jae-Doo;Hwang, Bang-Yeon;Ro, Jai-Seup
    • Natural Product Sciences
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    • v.11 no.3
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    • pp.145-149
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    • 2005
  • A methanol soluble extract from the dried hooks and stems of Uncaria rhynchophylla showed a strong inhibitory activity against monoamine oxidase in mouse brain. Using a bioassay-guided purification of this extract, a known ${\beta}-carboline$ type alkaloid, harman (1), was obtained as an active constituent. In addition, five known indole alkaloids, isocorynoxeine (2), isorhynchophylline (3), corynoxeine (4), cadambine (5), and $3{\alpha}-dihydrocadambine$ (6), were isolated and found to be weakly active or inactive.

Studies on the Change of Chemical Components of Flue-cured Tobacco with Maturity (황색종 잎담배의 숙도에 따른 화학성분의 변화연구)

  • Hwang, Geon-Jung;Kim, Jeong-Hwan;Kim, Chan-Ho
    • Journal of the Korean Society of Tobacco Science
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    • v.3 no.1
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    • pp.20-24
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    • 1981
  • This experiment was carried out to determine the relationships between maturity and content of the chemical components in flue-cured tobacco. The results were as follows : 1) Among the chemical components, the contents of total nitrogen, ammonia nitrogen, total alkaloids, nicotine, total volatile base, petroleum-ether extract, crude fiber, crude ash, water soluble ash, and chlorine decreased significantly, and those of total sugar, reducing sugar, and starch increased as leaf maturity progressed until the stage of ripeness, but, afterwards, a reverse tendency appeared. 2) There was a significant relationship between maturity and the contents of chemical components, such as total nitrogen, protein nitrogen, ammonia nitrogen, total volatile base, and the correlation coefficients of them were -0.743, -0.789, -0.797, and -0.642, respectively.

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A Study on Antimicrobial Activity of Veratri Herba (여로의 항균작용에 관한 연구)

  • Chi Gyoo Yong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.16 no.1
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    • pp.95-98
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    • 2002
  • This study was carried out to investigate the efficacy of antifungal and antibacterial activity of Veratri Herba, which was used as insecticide in the clinical part of oriental dermatology for a long time. Sample herb was selected with Veratrum maackii in the middle of 5 veratrum species. The experimental results of this herb were as follows. Crude extract showed various relative inhibitory rates from 68.9% to 95.6% in 2mg/disc against Fusarium oxysporum, Botrytis cineria, Saccharomyces cerevisiae, Escherichiae coli, and Bacillus subtilis on the basis of inhibitory range against B. cineria, and the inhibitory effect was decreased depending on density. In the extract of various organic solvent, chloroform and ethyl acetate fraction show the various size of dear zone against all microbes. And in the subfraction assay from ethyl acetate fraction, crude alkaloids show the antibacterial and antifungal effect significantly.

Asymmetric Michael Reaction of Malonate Derivatives with α, β-Unsaturated Ketones

  • Cho, Min-Je;Cho, Myoung-Gi;Huh, Sun-Chul;Kim, Sung-Min;Lee, Kil-sung;Koh, Kwang-Oh;Mang, Joo-Yang;Kim, Dae-Young
    • Bulletin of the Korean Chemical Society
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    • v.27 no.6
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    • pp.857-862
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    • 2006
  • The catalytic enantioselective Michael reaction promoted by quaternary ammonium salts from Cinchona alkaloids as a phase-transfer catalyst is described. Treatment of malonates with $\alpha$,$\beta$-unsaturated ketones under mild reaction conditions afforded the corresponding Michael adducts in good yields with good to moderate enantiomeric excesses.

Enhancing Activity of Anticancer Drugs in Multidrug Resistant Tumors by Modulating P-Glycoprotein through Dietary Nutraceuticals

  • Khan, Muhammad;Maryam, Amara;Mehmood, Tahir;Zhang, Yaofang;Ma, Tonghui
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.16
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    • pp.6831-6839
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    • 2015
  • Multidrug resistance is a principal mechanism by which tumors become resistant to structurally and functionally unrelated anticancer drugs. Resistance to chemotherapy has been correlated with overexpression of p-glycoprotein (p-gp), a member of the ATP-binding cassette (ABC) superfamily of membrane transporters. P-gp mediates resistance to a broad-spectrum of anticancer drugs including doxorubicin, taxol, and vinca alkaloids by actively expelling the drugs from cells. Use of specific inhibitors/blocker of p-gp in combination with clinically important anticancer drugs has emerged as a new paradigm for overcoming multidrug resistance. The aim of this paper is to review p-gp regulation by dietary nutraceuticals and to correlate this dietary nutraceutical induced-modulation of p-gp with activity of anticancer drugs.

Analysis of Alkaloids in Uncaria Hooks (조구등 중의 알칼로이드 분석)

  • Park, Man Ki;Park, Jeong Hill;Kim, Jong Moon;Han, Sang Bum;Han, Bang Hee;Kang, Jong Seong
    • Analytical Science and Technology
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    • v.6 no.4
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    • pp.395-399
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    • 1993
  • Corynoxeine, rhynchophylline, isocorynoxeine, isorhychophylline were isolated from Uncaria hooks and determined by HPLC. Their contents were : isocorynoxeine 0.21%, isorhynchophylline 0.16%, corynoxeine 0.28%, rhynchophylline 0.23%, respectively. Corynoxeine and isocorynoxeine, rhynchophylline and isorhychophylline were interconverted each other by heat treatment.

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