• Title/Summary/Keyword: isoquinoline alkaloids

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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.

Protective effect of Macleaya cordata isoquinoline alkaloids on lipopolysaccharide-induced liver injury in broilers

  • Jiaxin Chen;Weiren Yang;Hua Liu;Jiaxing Niu;Yang Liu;Qun Cheng
    • Animal Bioscience
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    • v.37 no.1
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    • pp.131-141
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    • 2024
  • Objective: This experiment aimed to explore the protective action of dietary supplementation with isoquinoline alkaloids (IA) from Macleaya cordata on lipopolysaccharide (LPS)-induced liver injury in broilers. Methods: Total 216 healthy broilers were selected in a 21-d trial and assigned randomly to the following 3 treatments: control (CON) group, LPS group, and LPS+IA group. The CON and LPS groups were provided with a basal diet, whereas the LPS+IA group received the basal diet supplemented with 0.6 mg/kg Macleaya cordata IA. Broilers in LPS and LPS+IA groups were intraperitoneally injected with LPS (1 mg/kg body weight) at 17, 19, and 21 days of age, while those in CON group were injected with equivalent amount of saline solution. Results: Results showed LPS injection caused systemic and liver inflammation in broilers, inhibited immune function, and ultimately lead to liver injury. By contrast, supplementation of IA ameliorated LPS-induced adverse change in serum parameters, boosted immunity in LPS+IA group. Furthermore, IA suppressed the elevation of hepatic inflammatory cytokines and caspases levels induced by LPS, as well as the expressions of genes related to the toll-like receptor 4 (TLR4)/myeloid differentiation primary response 88 (MyD88)/nuclear factor-kappa B (NF-κB) pathway. Conclusion: Dietary inclusion of 0.6 mg/kg Macleaya cordata IA could enhance immune function of body and inhibit liver damage via inactivating TLR4/MyD88/NF-κB signaling pathway in broilers.

Aldose Reductase Inhibitory Alkaloids from Corydalis ternata

  • Seo, Wonse;Jung, Sang Hoon;Shim, Sang Hee
    • Natural Product Sciences
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    • v.22 no.2
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    • pp.102-106
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    • 2016
  • A methanolic extract of Corydalis ternata having aldose reductase inhibitory activity was examined as a possible aldose reductase (ALR2) inhibitor, a key enzyme involved in diabetic complications. Seven alkaloids, tetrahydrocoptisine (1), corydaline (2), tetrahydropalmatine (3), isocorybulbine (4), corybulbine (5), dehydrocorydaline (6), and N-methyltetrahydroberbinium (7) were isolated from $CHCl_3$ fraction of C. ternata methanol extract. Among them, compounds 1, 5, and 7 exhibited $5.04{\pm}1.97%$, $5.00{\pm}1.26%$, and $1.80{\pm}2.33%$ inhibitions, respectively at $40{\mu}M$. The activities of the single compounds were not comparable to that of the whole extract, suggesting that the whole combination of each single compound was responsible for the activity of the extract as shown in many cases of natural medicines. Even though this is the second report on aldose reductase inhibition activity of C. ternata, recombinant human aldose reductase was employed in this study unlike in the previous report. Furthermore, the aldose reductase inhibitory activities of isocorybulbine, corybulbine, and N-methyltetrahydroberbinium, to the best of our knowledge, were evaluated for the first time in this study. These results suggest a use of the extract of C. ternata for ameliorating diabetic complications.

Human Neutrophil Elastase Inhibitory Alkaloids from Chelidonium majus L.

  • Kim, Jeong Yoon;Lee, Ji Hye;Song, Yeong Hun;Jeong, Won Min;Tan, Xuefei;Uddin, Zia;Park, Ki Hun
    • Journal of Applied Biological Chemistry
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    • v.58 no.3
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    • pp.281-285
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    • 2015
  • Human neutrophil elastase (HNE) represents a good therapeutic target for the treatment of inflammatory diseases as well as invasion of microorganism. The methanol extract of a aerial part of Chelidonium majus L. showed high activity against the neutrophil elastase with an $IC_{50}$ value of $100{\mu}g/mL$. Due to its potency, subsequent bioactivity-guided fractionation of methanol extract led to six alkaloids (1-6), which were identified as dihydrosanguinarine (1), (s)-stylopine (2), arnottianamide (3), (+)-chelidonine (4), spallidamine (5), and N-trans-feruloyltyramine (6). Among of them, three alkaloids (2, 5, and 6) inhibited HNE in a dose-dependent manner with $IC_{50}$ ranging between 11.6 and $51.0{\mu}M$. Lineweaver-Burk and Dixon plots, and their secondary replots showed that alkaloids (2, 5, and 6) were mixed inhibitors of HNE. The analysis of $K_I$ and $K_{IS}$ value proved that all inhibitors (2, 5, and 6) had reversible mixed type I mechanism.

Protoberberine Alkaloids and their Reversal Activity of P-gp Expressed Multidrug Resistance (MDR) from the Rhizome of Coptis japonica Makino

  • Min, Yong-Deuk;Yang, Min-Cheol;Lee, Kyu-Ha;Kim, Kyung-Ran;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • v.29 no.9
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    • pp.757-761
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    • 2006
  • Six protoberberine alkaloids were isolated from the chloroform layer of the rhizome of Coptis japonica Makino (Ranunculaceae). The structures of the isolated compounds were determined to be 6-([1,3]dioxolo[4,5-g]isoquinoline-5-carbonyl)-2,3-dimethoxy-benzoic acid methyl ester (1), oxyberberine (2), 8-oxo-epiberberine (3), 8-oxocoptisine (4), berberine (5) and palmatine (6) by physicochemical and spectroscopic methods. The compound 3 (8-oxo-epiberberine) was first isolated from natural sources. The compounds were tested for cytotoxicity against five tumor cell lines in vitro by SRB method, and also tested for the MDR reversal activities. Compound 4 was of significant P-gp MDR inhibition activity with ED50 value $0.018\;{\mu}g/mL$ in MES-SA/DX5 cell and $0.0005\;{\mu}g/mL$ in HCT15 cell, respectively.

Allelopathic Potential and Substances from Cork Tree (Pbellodendron amurense Rupr.)

  • Park, Young-Goo;Choi, Myung-Suk;Yang, Jae-Kyung;Paik, Ki-Hyon
    • Journal of the Korean Wood Science and Technology
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    • v.29 no.3
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    • pp.92-98
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    • 2001
  • Allelopathic effects of the cork tree (Phellodendron amurense Rupr.) on several crops and soil miro-organisms were assessed using germination bioassay and antimicrobial assay, and allelochemicals were identified. In a germination bioassay, extract of cork tree inhibited at high concentration on germination of several crop seeds such as cabbage, lettuce, and cucumber. However, aqueous extracts inhibited powerfully growth of test organisms such as Streptococus aureus, S. aureus, S. typhimurium, and E. coli as bacteria, and Candida albicans as yeast, and Botrytis cineria and Alternata alternaria as fungi.. The cork tree extract showed strong antimicrobial activities against isolated soil fungi. The allelochemicals were separated using Silica gel, Sephadex LH-20 gel column chromatography and HPLC. The substances were analyzed by UV spectrometry and EI-mass spectrometry. The active allelochemicals were identified as isoquinoline alkaloids, berberine and palmatine.

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Effects of Aporphine Compounds on Dopamine Biosynthesis in PC12 Cells

  • Jin, Chun-Mei;Lee, Jae-Joon;Yin, Shou-Yu;Kim, Yu-Mi;Lee, Myung-Koo;Ryu, Si-Yong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.254.1-254.1
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    • 2002
  • The effects of aporplline isoquinoline alkaloids such as liriodenine. anonaine and asimilobine on dopamine biosynthesis in PC12 cells were investigated. Treatment of PC12 cells with liriodenine (10 ${\mu}$M), anonaine (0.05 ${\mu}$M) and asimilobine (0.15 ${\mu}$M) showed 33.6%, 37.7% and 35.1 % inhibition of dopamine content for 12 h. The IC$\sub$50/ values of liriodenine. anonaine and asimilobine were 8.4 ${\mu}$M. 0.05 ${\mu}$M and 0.13 ${\mu}$M. respectively. (omitted)

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Influence of Quaternary Benzophenantridine and Protopine Alkaloids on Growth Performance, Dietary Energy, Carcass Traits, Visceral Mass, and Rumen Health in Finishing Ewes under Conditions of Severe Temperature-humidity Index

  • Estrada-Angulo, A.;Aguilar-Hernandez, A.;Osuna-Perez, M.;Nunez-Benitez, V.H.;Castro-Perez, B.I.;Silva-Hidalgo, G.;Contreras-Perez, G.;Barreras, A.;Plascencia, A.;Zinn, R.A.
    • Asian-Australasian Journal of Animal Sciences
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    • v.29 no.5
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    • pp.652-658
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    • 2016
  • Twenty $Pelibuey{\times}Katahdin$ ewes ($35{\pm}2.3kg$) were used to determine the effects of the consumption of standardized plant extract containing a mixture of quaternary benzophenanthridine alkaloids and protopine alkaloids (QBA+PA) on growth performance, dietary energetics, visceral mass, and ruminal epithelial health in heat-stressed ewes fed with a high-energy corn-based diet. The basal diet (13.9% crude protein and 2.09 Mcal of net energy [NE] of maintenance/kg of dry matter) contained 49.7% starch and 15.3% neutral detergent fiber. Source of QBA+PA was Sangrovit RS (SANG) which contains 3 g of quaternary benzophenathridine and protopine alkaloids per kg of product. Treatments consisted of a daily consumption of 0 or 0.5 g SANG/ewe. Ewes were grouped by weight and assigned to 10 pens (5 pens/treatment), with two ewes per pen. The experimental period lasted 70 days. The mean temperature humidity index during the course of this experiment was $81.7{\pm}1.0$ (severe heat stress). There were no treatment effects on water intake. Dry matter intake was not affected (p = 0.70) by treatments, but the group fed SANG had a numerically (11.2%) higher gain in comparison to the control group, SANG improved gain efficiency (8.3%, p = 0.04), dietary NE (5.2%, p<0.01) and the observed-to-expected NE (5.9%, p<0.01). Supplemental SANG did not affect ($p{\geq}0.12$) carcass characteristics, chemical composition of shoulder, and organ weights (g/kg empty body weight) of stomach complex, intestines, and heart/lung. Supplemental SANG decreased liver weight (10.3%, p = 0.02) and increased visceral fat (16.9%, p = 0.02). Rumen epithelium of ewes fed SANG had lower scores for cellular dropsical degeneration (2.08 vs 2.34, p = 0.02), parakeratosis (1.30 vs 1.82, p = 0.03) and neutrophil infiltration (2.08 vs 2.86, p = 0.05) than controls. It is concluded that SANG supplementation helped ameliorate the negative effects of severe heat on growth performance of feedlot ewes fed high-energy corn-based diets. Improvement in energetic efficiency may have been mediated, in part, by anti-inflammatory effects of supplemental SANG and corresponding enhancement of nutrient uptake.

Effects of Berberine on 6-hydroxydopamine-induced Parkinsonism in Rats (Berberine이 백서의 6-hydroxydopamine-유도 파킨슨병 모델에 미치는 영향)

  • Kwon, Ik-Hyun;Choi, Hyun-Sook;Shin, Kun-Seong;Hwang, Bang-Yeon;Lee, Myung-Koo
    • Korean Journal of Pharmacognosy
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    • v.40 no.4
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    • pp.351-356
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    • 2009
  • Many isoquinoline alkaloids including berberine lower dopamine content by reducing tyrosine hydroxylase (TH) activity and aggravate L-DOPA-induced cytotoxicity in PC12 cells. In this study, the effects of berberine on 6-hydroxydopamine (6-OHDA)-induced cytotoxicity in PC12 cells and on unilateral 6-OHDA-lesioned rat models were investigated. Berberine at 10-30 ${\mu}M$ did not affect cell viability in PC12 cells. However, berberine at concentrations higher than $50{\mu}M$ caused cytotoxicity at 24 h. Berberine (10-50 ${\mu}M$) also enhanced 6-OHDA (10-50 ${\mu}M$)-induced cytotoxicity at 24 h compared to 6-OHDA alone with an apoptotic process. In addition, treatment with berberine (5 and 30 mg/kg, i.p.) for three weeks showed a dopaminergic cell loss in substantia nigra of 6-OHDA-lesioned rats: 30 mg/kg berberine was more intensive cytotoxic. The levels of dopamine were also decreased by berberine (5 and 30 mg/kg) in the ipsilateral substantia nigra of 6-OHDA-lesioned rats. These results suggest that berberine aggravated 6-OHDA-induced cytotoxicity in PC12 cells and treatment with berberine (5 and 30 mg/kg) in 6-OHDA-lesioned rats also enhanced the degeneration of dopaminergic cell death and the decrease in dopamine levels in substantia nigra. Therefore, the long-term L-DOPA therapeutic patients with isoquinoline compounds including berberine may need to be checked for the adverse symptoms.

DNA Binding Mode of the Isoquinoline Alkaloid Berberine with the Deoxyoligonucleotide d(GCCGTCGTTTTACA)2

  • Park, Hye-Seo;Kim, Eun-Hee;Sung, Yoon-Hui;Kang, Mi-Ran;Chung, In-Kwon;Cheong, Chae-Joon;Lee, Weon-Tae
    • Bulletin of the Korean Chemical Society
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    • v.25 no.4
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    • pp.539-544
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    • 2004
  • The ability of protoberberine alkaloids, berberine and berberrubine, to act as topoisomerase II poisons is linked to the anti-cancer activity. Minor alterations in structure have a significant effect on their relative activity. Berberine, which has methoxy group at the 19-position, is significantly less potent than berberrubine. Several observations support non-specific binding to HP14 by the berberine: (i) nonspecific upfield changes in $^1H$ chemical shift for protons of the berberine; (ii) the broadening of imino protons of HP14 upon binding of the berberine; (iii) very small increases in duplex melting temperature in the presence of the berberine. Our results reveal that substitution of a hydroxyl group to a methoxy group on the 19-position, thereby converting the berberrubine to the berberine is associated with a non-specific DNA binding affinity and a reduced topoisomerase II poisoning. The presence of a bulky 19-methoxy substituent decreases intercalating properties of berberine and makes it inactive as topoisomerase II poison.