• Biomolecules & Therapeutics
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• v.16 no.3
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• pp.261-269
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• 2008

This experiment was performed to investigate the anxiolytic-like effects of cyclopeptide fraction alkaloids of Zizyphi Spinosi Semen (CFAZ), by using the experimental paradigms of anxiety, and compared with those of a known anxiolytic, diazepam. CFAZ (8.0 mg/kg, p.o.) increased the percentage of time spent on the open arms and the number of open arms entries in the elevated plus-maze test, increased the number of head dips in the hole-board test, and increased the percentage of center zone ambulatory time in the open-field box. However, CFAZ has no effect on the locomotor activity, while diazepam (2.0 mg/kg, p.o.) significantly reduced locomotor activity. CFAZ did not influence the grip force in the grip strength meter test, either. From the molecular experiments, CFAZ increased chloride influx in cultured cerebellar granule cells. In addition, $GABA_A$ receptors $\gamma$-subunit were over-expressed by CFAZ in cultured cerebellar granule cells. It is concluded that CFAZ may have anxiolytic-like effects, and these effects may be mediated by $GABA_A$ receptors.

• Korean Journal of Pharmacognosy
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• v.27 no.4
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• pp.289-294
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• 1996

In previous paper, we described the induced callus of Corydalis remota contains a significant amount of alkaloids. This study describes an optimal condition to maximize alkaloid production. The suspension cultures maintained alkaloid production ability after fifth subculture and a small amount of alkaloid seemed to be released out of cells. The yields of alkaloid by cultured cells was varied depending on the concentrations of NAA, carbon sources and phosphate ion and depending on the vitamin combinations and concentrations. Biosynthetic precursor and an elicitor treatment also affected the total alkaloid yield of the cultures. The optimal conditions for alkaloid production were as follows: 1) MS basal salt containing 30 g/l of glucose, 1.0 mg/l of NAA, and vitamins of LS medium should be used. 2) The culture should be treated with tyrosine 20 mg/l, and yeast extract 1.5 ml/l after the culture reached a stationary phase of growth. Five alkaloids were isolated from the cultures and they were characterized. The spectral data unambiguously revealed that the isolated compounds were dihydrosanguinarine, protopine. tetrahydropalmatine, allocyptopine and ambinine, respectively.

• Korean Journal of Medicinal Crop Science
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• v.12 no.5
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• pp.372-377
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• 2004

Scopolia parviflora Nakai, a rare and endangered species, is the sole plant producing tropane alkaloids (TA) among the Korean native species. In order to enhance TA productivity the SP72 root line was selected by screening 100 of root line, and the optimal culture media for root growth and TA production were investigated with the SP72 roots. Based on the several media, SH and 2B5 medium were determined as growth medium and White and NN medium as production medium. Among the four combinations of two-stage culture, 2BN (2B5 as growth medium plus NN as production medium) showed more enhanced root growth and TA production as compared with production media of White and NN medium and growth media of SH and 2B5 medium, respectively. However, bubble column bioreactor (BCB) cultures applying two-stage culture did not reveal the effective results despite of the each successful operation of two-stage culture in conical flasks and BCB cultures.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.32 no.3
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• pp.347-352
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• 1987

This studies were carried out to investigate the effects of nitrogen fertilizer rates and methods of its application on maturity of leaves, total nitrogen and total alkaloids concentration in burley tobacco leaves. Nitrogen rate ranged from 17.5 to 40.5kg/10a and applied through basic fertilization and sidedressing. The filling capacity of cured leaves was decreased with increasing levels of nitrogen fertilizer. As the rate of nitrogen fertilization was increased or sidedressing, the maturity of leaves was delayed and total alkaloids and total nitrogen concentration were increased. Total alkaloids concentration in leaves was gradually increased, especially more in upper leaves from 60 to no days after tratnsplanting, but total nitrogen concentration was decreased.

• Biomolecules & Therapeutics
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• v.12 no.3
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• pp.138-144
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• 2004

Therapeutic effect of a Kampo medicine, Choto-san, in patients with vascular dementia was demonstrated by a double-blind and placebo-controlled clinical trial. To clarify the therapeutic efficacy of Choto-san, anti-ischemic effect in mice, hypotensive effect in spontaneously hypertensive rats (SHR), anti-oxidative effects in vitro, and N-methyl-D-aspartate (NMDA) receptor-blocking activity using Xenopus oocytes were studied. (1) Pretreatment with Choto-san (0.75-6.O g/kg, P.O.) or a component herb Chotoko (Uncaria genus: 75 - 600 mg/kg, P.O.) prevented ischemia-induced impairment of spatial learning behaviour in mice. Indole alkaloids- and phenolic fractions extracted from Chotoko also improved significantly the learning deficit. (2) Subchronic administration of Choto-san (0.5 g/kg, p.o.) caused a significant hypotensive effects in SHR. (3) Choto-san, Chotoko, and the phenolic constituent, (-) epicatechin, significantly protected the NG108-15 cell injury induced by $H_20_2$ exposure in vitro and also inhibited lipid peroxidation in the brain homogenate. (4) Indole alkaloids, rhynchophylline and isorhynchophylline (1-100 uM), reversibly reduced NMDA-induced current in the receptor-expressed Xenopus oocytes. These results suggest that anti-vascular dementia effects of Choto-san are mainly due to the effect of Chotoko. From these results, it is possible to make a novel dietary supplement through several extraction steps from Chotoko.

• 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.

• Archives of Pharmacal Research
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• v.26 no.2
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• pp.114-119
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• 2003

A high performance liquid chromatographic (HPLC) method was developed for the qualitative and quantitative determination of benzophenanthridine alkaloids from the methanol extracts of Hylomecon hylomeconoides and H. vernale (Papaveraceae). Achiral and chiral methods were adapted for the separation of 6-methoxydihydrosanguinarine (1), 6-acetonyldihydrosanguinarine (2) and dihydrosanguinarine (3). The achiral reversed phase HPLC method made it possible the simultaneous separation and determination of 1, 2 and 3 within 20 min on ODS column using acetonitrile-phosphate buffer (50 mM, pH 7.0) (50 : 50, v/v). The separation and determination of 1 and 2 enantiomers was available using chiral columns. The same amount of (+) and (-)-enantiomers of 1 was found from the methanol extract of specimen, indicated that 1 could be the artifact produced by the reaction of sanguinarine with methanol. H. hylomeconoides showed higher level of 1 and 3 in compared with H. vernale, especially in root samples permitting the possibility of chemical discrimination between two species.

• YAKHAK HOEJI
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• v.41 no.5
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• pp.554-558
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• 1997

Two alkaloidal components were isolated from the ether soluble part of the MeOH extract of the root bark of Euonymus japonica. Their structures were elucidated by the spe ctroscopic analylses as the sesquiterpene pyridine alkaloids derived from polyester sesquiterpenes which are characteristically detected in Celastraceae plants. These include macrocycle formed by two ester linkages between dihydro-${\beta}$-agarofuran nucleus and pyridinic dibasic acid(compound 1:evoninic acid, compound 2:wilfordic acid). The structure of compound $1[C_{47}H_{50}N_2O_{17},\;mp\;161{\sim}163^{circ}C$. $[{\alpha}]_D^{28}=+31.6^{\circ}$(c, 0.1 in EtOH)] was determined as novel structure named as euojaponine N, and compound $2[C_{48}H_{57}NO_{18},\;mp\;142{\sim}145^{circ}C,\;[{\alpha}_D^{27}=+27.0^{\circ}$(c, 0.1 in EtOH)] was identified as ebenifoline W-I reported from Maytenus ebenifolia.

• 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.

• Journal of Plant Biotechnology
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• v.29 no.3
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• pp.199-207
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• 2002

The tropane alkaloids hyoscyamine (its racemic form being atropine) and scopolamine are used medicinally as anticholinergic agents that act on the parasympathetic nerve system. Because they differ in their actions on the central nervous system, currently there is a 10-fold higher commercial demand for scopolamine, in the N-butylbromide form, than there is for hyoscyamine and atropine combined. Several solanaceous species have been used as the commercial sources of these alkaloids, but the scopolamine contents in these plants often are much lower than those of hyoscyamine. For this reason there has been long-standing interest in increasing the scopolamine contents of cultivated medicinal plants. Naturally occurring and artificial interspecific hybrids of Duboisia have high scopolamine contents and are cultivated as a commercial source of scopolamine in Australia and other countries. Anther culture combined with conventional interspecific hybridization also has been used to breed high scopolamine-containing plants in the genera Datura and Hyoscyamus, but without much success. The use of recombinant DNA technology for the manipulation of metabolic processes in cells promises to provide important contributions to basic science, agriculture, and medicine. In this review, I introduce on the enzymes and genes involved in tropane alkaloid biosynthesis and current progress in metabolic engineering approaches for tropane alkaloid, especially scopolamine, production.