• Proceedings of the PSK Conference
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• 2003.10b
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• pp.79.3-80
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• 2003

The effects of anonaine, an aporphine isoquinoline alkaloid, on dopamine biosynthesis and L-DOPA-induced neurotoxicity in PC12 cells were investigated. Treatment of PC12 cells with 0.05 ${\mu}$M anonaine showed a significant inhibition of dopamine content. The IC$\sub$50/ value of anonaine was 0.05 ${\mu}$M. Under the same conditions, 0.05 ${\mu}$M anonaine also inhibited tyrosine hydroxylase (TH) activity at 24 h (62.0% inhibition of the control level). TH mRNA levels were also decreased by the treatment with anonaine. (omitted)

• Parasites, Hosts and Diseases
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• v.55 no.3
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• pp.337-340
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• 2017

Leishmaniasis is a neglected and endemic disease that affects poorest population mainly in developing countries. A lack of adequate and definitive chemotherapeutic agents to fight against this infection has led to the investigation of numerous compounds. The aim of this study was to investigate in vitro activity of boldine against Leishmania amazonensis murine cell infection. Boldine ((S)-2,9-dihydroxy-1,10-dimethoxy-aporphine) is an aporphine alkaloid found abundantly in the leaves/bark of boldo (Peumus boldus Molina), a widely distributed tree native to Chile. The in vitro system consisted of murine macrophage infection with amastigotes of L. amazonensis treated with different concentrations from 50 to $600{\mu}g/ml$ of boldine for 24 hr. Intracellular parasite destruction was assessed by morphological examination and boldine cytotoxicity to macrophages was tested by the MTT viability assay. When cells were treated with $100{\mu}g/ml$ of boldine the reduction of parasite infection was 81% compared with untreated cultures cells. Interestingly, boldine-treatment caused a concentration-dependent decrease of macrophage infection that culminated with 96% of reduction when cells were submitted to $600{\mu}g/ml$ of boldine. Cell cultures exposed to $100{\mu}g/ml$ of boldine and $300{\mu}g/ml$ of $Glucantime^{(R)}$ during 24 hr showed a significant reduction of 50% in parasitized cells compared with cell cultures exposed just to $Glucantime^{(R)}$. The study showed that treatment with boldine produces a better effect than treatment with the reference antimonial drug, glucantime, in L. amazonensis infected macrophage. Our results suggest that boldine is a potentially useful agent for the treatment of leishmaniasis.

• Bulletin of the Korean Chemical Society
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• v.32 no.10
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• pp.3597-3602
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• 2011

A simple and rapid analytical method was developed for the determination of eight isoquinoline alkaloids in Corydalis species. Eight isoquinoline alkaloids, including 2 aporphine alkaloids (isocorydine and glaucine) and 6 protoberberine alkaloids (coptisine, palmatine, berberine, canadine, corydaline, and tetrahydrocoptisine) were used as chemical markers which have a various biological activity and determined for quality control of Corydalis (C.) species (C. ternata, C. yanhusuo, and C. decumbens). To evaluate the quality of these herbal medicines, LC chromatographic separation of alkaloids were preferentially investigated on reversed-phase C18 column with pH variation and composition of mobile phase. In addition, the separation of these alkaloids in herbal extracts was found to be significantly affected on mobile phase composition using gradient elution. Especially for C. yanhusuo extract, berberine was seriously interfered with other alkaloid extracted from sample matrix when mobile phase composition was not optimized. As results, these compounds were successfully separated within 28 min using 10 mM ammonium acetate containing 0.2% triethylamine (adjusted at pH 5.0) as a mobile phase with gradient elution. On the basis of optimized HPLC conditions, 23 different Corydalis species samples were analyzed for the determination of alkaloid levels. In addition, principal component analysis (PCA) combined with the chromatographic data could be successfully classified the different geographic origin samples.

• Natural Product Sciences
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• v.17 no.2
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• pp.108-112
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• 2011

Several isoquinoline alkaloids (1 - 18), which have basic chemical structures as protoberberine and aporphine skeletones, were evaluated for their inhibitory activities on AChE and BuChE. Among them, compounds 3, 4, 6, 8 and 12 showed the potent AchE activity with the $IC_{50}$ values ranging from $10.2{\pm}0.5\;{\mu}M$ to $24.5{\pm}1.6\;{\mu}M$, meanwhile, compound 14 - 17 exhibited strong inhibitory activity with $IC_{50}$ values from $2.1{\pm}0.2$ to $5.5{\pm}0.3\;{\mu}M$. Compounds 14 - 17 exhibited selective inhibition for AChE compared with BuChE. The isoquinoline alkaloid possesses aromatic methylenedioxy groups and quaternary nitrogen atoms are crucial for the anti-cholinesterase inhibitory activity.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.55-59
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• 2003

The effects of liriodenine, an aporphine isoquinoline alkaloid, on dopamine content in PCl2 cells were investigated. Treatment of PC12 cells with liriodenine decreased dopamine content in a dose-dependent manner (33.6% inhibition at $10\;{\mu}M$ for 12 h). The $IC_{50}$ in value of liriodenine was $8.4\;{\mu}M$. Dopamine content decreased at 3 h and reached a minimal level at 12 h after the exposure to liriodenine. Under these conditions, the activities of tyrosine hydroxylase and aromatic L-amino acid decarboxylase were also inhibited at $10\;{\mu}M$ of liriodenine by 10.1% and 20.2% relative to control, respectively. In addition, liriodenine inhibited the increase in dopamine content induced by L-DOPA Treatments $(50-100\;{\mu}M)$ in PC12 cells. These results suggest that liriodenine inhibited dopamine biosynthesis and L-DOPA-induced increase in dopamine content by reducing the activities of tyrosine hydroxylase and aromatic L- amino acid decarboxylase in PC12 cells.