• Title/Summary/Keyword: Alkaloids

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In Vivo Antifungal Effects of Coptis japonica Root-Derived Isoquinoline Alkaloids Against Phytopathogenic Fungi

  • LEE CHI-HOON;LEE HOI-JOUNG;JEON JU-HYUN;LEE HOI-SEON
    • Journal of Microbiology and Biotechnology
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    • v.15 no.6
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    • pp.1402-1407
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    • 2005
  • The fungicidal activities of Coptis japonica (Makino) extracts and their active principles were determined against Botrytis cineria, Erysiphe graminis, Phytophthora infestans, Puccinia recondita, Pyricularia grisea, and Rhizoctonia solani using a whole plant method in vivo, and compared with natural fungicides. The responses varied according to the plant pathogen tested. At 2,000 mg/l, the chloroform and butanol fractions obtained from methanolic extracts of C. japonica exhibited strong/moderate fungicidal activities against B. cinerea, E. graminis, P. recondita, and Py. grisea. Two active constituents from the chloroform fractions and one active constituent from the butanol fractions were characterized as isoquinoline alkaloids, berberine chloride, palmatine iodide, and coptisine chloride, respectively, using spectral analysis. Berberine chloride had an apparent $LC_{50}$ value of approximately 190, 80, and 50 mg/l against B. cinerea, E. graminis, and P. recondita, respectively; coptisine chloride had an $LC_{50}$ value of 210,20, 180, and 290 mg/l against B. cinerea, E. graminis, P. recondita, and Py. grisea, respectively; and palmatine iodide had an $LC_{50}$ value of 160 mg/l against Py. grisea. The isoquinoline alkaloids were also found to be more potent than the natural fungicides, curcumin and emodin. Therefore, these compounds isolated from C. japonica may be useful leads for the development of new types of natural fungicides for controlling B. cinerea, E. graminis, P. recondita, and Py. grisea in crops.

Isoquinoline alkaloids supplementation on performance and carcass traits of feedlot bulls

  • Michels, Alex;Neumann, Mikael;Leao, Guilherme Fernando Mattos;Reck, Angela Maria;Bertagnon, Heloisa Godoi;Lopes, Leandro Samia;de Souza, Andre Martins;dos Santos, Leslei Caroline;Stadler, Edelmir Silvio Junior
    • Asian-Australasian Journal of Animal Sciences
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    • v.31 no.9
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    • pp.1474-1480
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    • 2018
  • Objective: Isoquinoline Alkaloids, derived from one plant (Macleaya cordata) can be an alternative when it is desired to increase performance in feedlot cattle. However, results on these nutritional additives in high energy diets in ruminants are still incipient in literature. In this context, the objective of this study was to evaluate performance and carcass traits of feedlot bulls supplemented with sanguinarine, the main alkaloid presents in Macleaya cordata in high energy density diets. Methods: Thirty-two crossbred Angus-Nelore bulls with mean initial body weight of $365{\pm}10kg$ and mean initial age of $11{\pm}3$ months were used. The experiment lasted 119 days, with 14 days of adaptation and 105 experimental days. Experimental diet consisted of 85% whole corn grains and 15% protein-vitamin-mineral nucleus and supplied ad libitum. Treatments consisted of a control diet (CON) and a diet with sanguinarine supplementation (SAN) at a dosage of 4 g of product sufficient to provide 6 mg of sanguinarine/d. Experimental design was completely randomized. Results: Dry matter intake, average daily gain and feed conversion were similar (p>0.05) between treatments. However, SAN group animals had higher carcass yield (p = 0.045) and were more efficient in the transformation of dry matter consumed in carcass gain (p = 0.046) than CON. In addition, haptoglobin, increased throughout feedlot duration meaning high challenge for the animals due to the diet, but this behavior was similar (p>0.05) between treatments. Conclusion: Sanguinarine produced positive results in relation to carcass yield and could be used as an additive for bulls fed diets receiving high energy density diet.

Inhibitory Effects of Phenolic Alkaloids of Menispermum Dauricum on Gastric Cancer in Vivo

  • Zhang, Hong-Feng;Wu, Di;Du, Jian-Kuo;Zhang, Yan;Su, Yun-Ming
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.24
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    • pp.10825-10830
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    • 2015
  • The present study was conducted to investigate effects and mechanisms of action of phenolic alkaloids of Menispermum dauricum (PAMD) on gastric cancer in vivo. In vitro, cell apoptosis of human gastric cancer cell line SGC-7901 was observed using fluorescence staining. In vivo, a mice model was constructed to observe tumor growth with different doses. Cell apoptosis was examined using flow cytometry and K-RAS protein expression using Western blotting. The mRNA expression of P53, BCL-2, BAX, CASPASE-3, K-RAS was examined by real-time PCR. PAMD significantly suppressed tumor growth in the xenograft model of gastric cancer in a dose-dependent manner (p<0.01). Functionally, PAMD promoted cell apoptosis of the SGC-7901 cells and significantly increased the rate of cell apoptosis of gastric tumor cells (p<0.05). Mechanically, PAMD inhibited the expression of oncogenic K-RAS both at the mRNA and protein levels. In addition, PAMD affected the mRNA expression of the cell apoptosis-related genes (P53, BCL-2, BAX, CASPASE-3). PAMD could suppress gastric tumor growth in vivo, possibly through inhibiting oncogenic K-RAS, and induce cell apoptosis possibly by targeting the cell apoptosis-related genes of P53, BCL-2, BAX, CASPASE-3.

New Azafluorenone Derivative and Antibacterial Activities of Alphonsea cylindrica Barks

  • Talip, Munirah Abdul;Azziz, Saripah Salbiah Syed Abdul;Wong, Chee Fah;Awang, Khalijah;Naz, Humera;Bakri, Yuhanis Mhd;Ahmad, Mohamad Syahrizal;Litaudon, Marc
    • Natural Product Sciences
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    • v.23 no.3
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    • pp.151-156
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    • 2017
  • A phytochemical study of Alphonsea cylindrica King (unreported) has led to the isolation of six alkaloids. The compounds were identified as kinabaline (1; azafluorenone alkaloid), muniranine (2), O-methylmoschatoline (3; oxoaporphine alkaloid), lysicamine (4), atherospermidine (5) and N-methylouregidione (6; 4, 5-dioxoaporphine alkaloid). The structures of the isolated compounds were determined based on the spectroscopic techniques and by comparison with data reported in the literature. Alkaloid 2 was isolated as a new derivative of azafluorenone while alkaloids 1, 3 - 6 were isolated for the first time from Alphonsea species. In addition, alkaloid 3 and 4 showed inhibition zone against Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus cereus in disc diffusion test. The minimum inhibition concentration (MIC) values of lysicamine (4) against S. aureus, B. cereus and P. aeruginosa were found to be smaller than O-methylmoschatoline (3). Therefore, the reported antibacterial activity showed the potential of this plant as natural antibacterial agent and supported the documented traditional use of Alphonsea sp. in the treatment of diarrhea and fever.

The Change of Catechin and Theanine Content in Green Tea during Different Storage Conditions (저장조건에 따른 녹차의 카테킨류, 테아닌의 변화)

  • Lee, Seung-Un
    • Culinary science and hospitality research
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    • v.22 no.5
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    • pp.267-276
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    • 2016
  • This study used HPLC to analyze the contents of catechins, alkaloids, and theanine of commercial green tea. Green tea samples were stored for 6 months at five different temperatures, $30^{\circ}C$, $15^{\circ}C$, $4^{\circ}C$, $-15^{\circ}C$ and $-40^{\circ}C$. Catechins change in storage temperature was $30^{\circ}C$ > $15^{\circ}C$ > $4^{\circ}C$ > $-15^{\circ}C$ > $-40^{\circ}C$ stored for 6 months. Total alkaloids content higher levels were CAF(27.49 mg/g) with lower level of TB(2.16 mg/g) and TP(0.28 mg/g). The total alkaloids content decreased in the longer storage periods, a similar case with, although CAF were almost unchanged in all storage temperatures. The results indicate that temperature and storage time are important in the storage of green tea, with refrigerated and frozen conditions as preferable to increase or preserve the chemical compounds of the green tea.

Analysis of Alkaloid Contents in Korean Plumyew [Cephalotaxus Koreana]: Variation with Location and Season (한국산 개비자 나무 [Cephalotaxus Koreana]의 알칼로이드 함량분석: 지역 및 계절에 따른 변화)

  • 김상익;최형균;송재영;김진현;이현수;홍승서
    • KSBB Journal
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    • v.15 no.5
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    • pp.434-437
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    • 2000
  • The contents and composition of alkaloids homoharringtonine, harringtonine, and cephalotaxine were determined in Korean native plumyew tree (Cephalotaxus koreana) collected from 17 different sites in Korea. The alkaloid contents of C. koreana varied with locations and plant populations from 11.8 mg/g to 195.2 mg/g of dry weight while C. koreana in southern area had higher alkaloid contents. The alkaloid compositions in C. koreana were highest with homoharringtonine (40%) and followed harringtonine (32%) and cephalotaxine (28%). Total alkaloids and homoharringtonine contents in needles were higher than those of stem by 2 fold. Alkaloid contents of C. koreana were the highest in winter, and the lowest in summer. Comparison of alkaloid contents and composition with other species of Cephalotaxus revealed that C. koreana was different to C. harringtonia, and contents of homoharringtonine were higher than other species. C. koreana could be potential source for homoharringtonine and related alkaloids.

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Embryogenic callus culture of Tribulus terrestris L. a potential source of harmaline, harmine and diosgenin

  • Nikam, T.D.;Ebrahimi, Mohammad Ali;Patil, V.A.
    • Plant Biotechnology Reports
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    • v.3 no.3
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    • pp.243-250
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    • 2009
  • In the present study, a simple one medium formulation protocol for callus culture, somatic embryogenesis and in vitro production of ${\beta}-carboline$ alkaloids and diosgenin in Tribulus terrestris L. was developed. Extensive callus induction and proliferation was obtained in leaf explant on Murashige and Skoog (MS) medium supplemented with $5.0{\mu}M$ 6 benzyl adenine (BA) and $2.5{\mu}M$ ${\alpha}-naphthaleneacetic$ acid (NAA). The embryogenic callus was maintained on subculture to fresh parental medium at 4-week intervals over a period of 28 months. The frequency of embryo formation was at a maximum ($18.1{\pm}0.9$ per g of callus) on MS medium containing $5.0{\mu}M$ BA and $2.5{\mu}M$ NAA together with $75mg\;1^{-1}$ casein hydrolysate. Globular embryo developed into torpedo stage embryo under the influence of starvation. The accumulation of ${\beta}-carboline$ alkaloids (harmaline and harmine) and steroidal saponin (diosgenin) in non-embryogenic and embryogenic callus culture derived from leaf explant was compared with root, leaf, stem, and fruit of the mother plant. The embryogenic callus accumulated equivalent amounts of harmaline ($66.4{\pm}0.5{\mu}g/g$ dry weight), harmine ($82.7{\pm}0.6{\mu}g/g$ dry weight), and diosgenin ($170.7{\pm}1.0{\mu}g/g$ dry weight) to that of the fruit of T. terrestris. The embryogenic callus culture of this species might offer a potential source for production of important pharmaceuticals.

Pharmacological Characterization of Synthetic Tetrahydroisoquinoline Alkaloids, YS 51 and YS 55, on the Cardiovascular System

  • Chang, Ki-Churl;Kang, Young-Jin;Lee, Young-Soo;Chong, Won-Seog;Choi-Yun, Hey-Sook;Lee, Duck-Hyong;Ryu, Jae-Chun
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.4
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    • pp.461-469
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethy-lamines, and many of them, especially with 6,7-disubstitution, demonstrate relatively high affinity for catecholamines. Two -OH groups at 6 and 7 positions are supposed to be essential to exert ?${\beta}-receptor$ activities. However, it is not clear whether -OH at 6,7 substitution of THIs also shows ?${\alpha}-adrenoceptor$ activities. In the present study, we investigated whether -OH or $-OCH_3$ substitutions of 6,7 position of THIs differently affect the ?1-adrenoceptor affinity. We synthesized two 1-naphthylmethyl THI alkaloids, $1-{\beta}-naphthylmethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline$ HBr (YS 51) and $1-{\beta}-naphthylmethyl-6, 7-dimethoxy-1,2,3,4-tetrahydroisoquinoline$ HCl (YS 55), and their pharmacological actions on ?${\alpha}_1-adrenoceptor$ were compared. YS 51 and YS 55, concentration-dependently relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.89{\pm}0.21$ and $5.93{\pm}0.19$, respectively. Propranolol (30 nM) did not affect the relaxation-response curves to YS 51 and YS 55. Concentration-response curves to PE were shifted to right by the pretreatment with YS 51 or YS 55. The $pA_2$ values of YS 51 and YS 55 showed $6.05{\pm}0.24$ and $5.88{\pm}0.16$, respectively. Both probes relaxed KCl (65.4 mM)-contracted aorta and inhibited $CaCl_2-induced$ contraction of PE-stimulated endothelium- denuded rat thoracic aorta in $Ca^{2+}-free$ solutions. In isolated guinea pig papillary muscle, 1 and 10 ${\mu}M$ YS 51 increased contractile force about 4- and 8- fold over the control, respectively, along with the concentration-dependent increment of cytosolic $Ca^{2+}$ ions. While, 10 ${\mu}M$ YS 55 reduced the contractile force about 50 % over the control and lowered the cytosolic $Ca^{2+}$ level, in rat brain homogenates, YS 51 and YS 55 displaced $[^3H]prazosin$ binding competitively with Ki 0.15 and 0.12 ${\mu}M$, respectively. However, both probes were ineffective on $[^3H]nitrendipine$ binding. Therefore, it is concluded that two synthetic naphthylmethyl-THI alkaloids have considerable affinity to ?1-adrenenoceptors in rat aorta and brain.

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