• The Korean Journal of Physiology and Pharmacology
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• v.2 no.3
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• pp.323-330
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• 1998

Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.

• Journal of Practical Agriculture & Fisheries Research
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• v.26 no.2
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• pp.31-40
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• 2024

This study was indicated that both potato leaves and stems contained certain amount of alkaloids compounds which digested in the rumen of Hanwoo steers. Three candidate plant byproducts such as potato, tomato, and eggplant were collected and dried for making feed additives. Among the candidate byproducts, potato extract was contained 2.05±0.27mg/g of α-chaconine and 0.60±0.08mg/g of α-solanine. These glycoalkaloids was potentially activated as functional compounds to skeletal muscle in beef cattle. However, tomato and eggplant byproducts were not detected any alkaloids compounds. After potato byproducts collected and dried for 24 hours, dry matter of potato byproduct were used as feeding study for evaluating active dose titrations. For evaluating dietary rate of rumen microbes, potato dry matter were treated with in situ hybridization for 72 hours using annulated Hanwoo steers. The glycoalkaloids contained potato dry matter were digested until 12 hours after treatment. Blood concentration of glycoalkaloids were not detected after 24 hours treatment of potato dry matter. These data indicated that potato byproduct were digested with rumen microbes for 24 hours after treatments.

• Journal of the Korean Chemical Society
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• v.54 no.1
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• pp.65-70
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• 2010

We describe the immune stimulatory effects of compounds determined by means of activity-monitored extraction and isolation techniques. As a result, 4-carboethoxy-6-methoxy-2-quinolone (1) and 4-carboethoxy-6-hydroxy-2-quinolone (2) were isolated from the ethyl acetate-soluble fraction of the Oryza sativa cv. Heugnambyeo bran, and were determined to exert significant inhibitory effects in macrophage cell line (murine RAW 264.7) and murine splenocytes. The structures were elucidated on the basis of spectroscopic evidence, particularly the results obtained via hetero nuclear multiple-bond connectivity and high-resolution MS spectroscopy. Up to date, compound (1) was isolated as natural sources for the first time.

• 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.

• CELLMED
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• v.10 no.2
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• pp.11.1-11.14
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• 2020

Nigella sativa commonly known as Black seed, Black cumin or Kalonji (Family Ranunculaceae) is a widely used for its miraculous healing power. Use of N. sativa seeds and oil has splendid historical past in diverse traditional systems of medicine and food. In Tibb-e-Nabwi (Prophetic Medicine), it is considered as one of the greatest forms of healing medicine. Phytochemically; it contains fixed oil, protein, alkaloids saponin and essential oil. Therapeutic properties of this plant are due to the presence of thymoquinone which is one of major active component and has different beneficial properties. In Unani System of Medicine the diseases are treated with nontoxic herbal drugs. As per Unani classical literature N. sativa perform various pharmacological actions like carminative, anti-inflammatory, analgesic, diuretic, emmenagogue, galactagogue, expectorant etc. Ample of phytochemical, pharmacological and clinical researches has been executed on N. sativa., which may include antidiabetic, anticancer, immunomodulator, analgesic, antimicrobial, anti-inflammatory, bronchodilator, hepato-protective, renal protective, gastro-protective, antioxidant properties, etc. This review is an effort to summarize the literature on scientific researches of pharmacognostical characteristics, chemical composition and pharmacological activities of the kalonji seeds

• Korean Journal of Medicinal Crop Science
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• v.13 no.5
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• pp.237-241
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• 2005

Scopolamine and hyoscyamine are important anticholinergic compounds obtained from Hyoscyamus niger. Adventitious roots induced from rhizome of H. niger and roots were cultured in SH medium supplemented with 3% (w/v) sucrose and 0.5 mg/L IBA. Roots were grown rapidly after 10 days of cultures. Scopolamine production was increased 7 times and hyoscyamine production was increased 12 times after 10 day of cultures. SH medium was best in root growth. But, highest scopolamine productivity was observed in WPM medium, followed White medium and best hyoscyamine productivity was resulted in MS medium. Sucrose was increased scopolamine and hyoscyamine production were increased the medium supplemented by sucrose comparing to than those by other carbon sources.

• Korean Journal of Medicinal Crop Science
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• v.12 no.2
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• pp.135-140
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• 2004

Total RNAs were isolated from cultured roots of Scopolia parviflora, $poly(A)^+$ RNA was obtained through the mRNA purification, cDNA library of Hnh6h was constructed. Recombinant baculoviruses in Spodoptera frugiperda (Sf) cells were constructed by use of the transfer vector pBacPAK, which has the AcNPV sequence under the polyhedrin promoter. The expression vector carrying Hnh6h gene was transferred to S. parviflora and obtained transgenic hairy root lines. Our results confirmed the over expression of the H6H protein was used by anti-pBacPAK about cDNAs of S. parviflora. This study will served for production of tropane alkaloids by metabolic engineering.

• 한국생물공학회:학술대회논문집
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• 2003.04a
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• pp.321-323
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• 2003

Hyoscyamine and scopolamine are the pharmaceutically valuable anticholinergic drugs. The aim of our study is to increase the contents of both hyoscyamine and scopolamine by means of elicitation. Various biotic elicitors derived from 3 fungi and 1 yeast were inoculated to the hairy root cultures. When homogenate and supernatant of elicitors treated with hairy root cultures, that of yeast elicitor was only increased scopolamine production. However, all of the fungal elicitors did not influenced the productions of scopolamine and hyoscyamine. Our results will contribute to mass production of tropane alkaloids by hairy root cultures of Scopolia parviflora.

• Korean Journal of Pharmacognosy
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• v.22 no.1
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• pp.26-32
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• 1991

The study aimed to confirm transformation, morphology, steroid alkaloidal TLC pattern and growth rate of hairy roots. The Solanum nigrum plantlets were inoculated with Agrobacterium rhizogenes strain 15834. Hairy roots were induced by plasmid. Agropine and mannopine were detected in the hairy roots. The organization of hairy roots on the transactional morphology was undifferentiated. Culture on the medium containing hormone(IBA 2, kinetin 0.1mg/l) altered hairy roots into callus. The growth rate of hairy roots on the NN30 liquid medium was 52 times heavier than in the original state and this was higher than on the other media. The results of TLC analysis indicated that the hairy roots produced steroidal alkaloids resembling those of normal roots.

• Korean Journal of Plant Tissue Culture
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• v.27 no.4
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• pp.269-282
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• 2000

Benzylisoquinoline alkaloids are a diverse group of natural products that include many pharmacologically active compounds produced in a limited number of plant families. Despite their complexity, intensive biochemical research has extended our knowledge of the chemistry and enzymology of many important benzylisoquinoline alkaloid pathways, such as those leading to the analgesic drugs morphine and codeine, and the antibiotics sanguinarine and berberine. The use of cultured plant cells as an experimental system has facilitated the identification and characterization of more than 30 benzylisoquinoline alkaloid biosynthetic enzymes, and the molecular cloning of the genes that encode at least 8 of these enzymes. The recent expansion of biochemical and molecular technologies has creat-ed unique opportunities to dissect the mechanisms involved in the regulation of benzylisoquinoline alkaloid biosynthesis in plants. Research has suggested that product accumulation is controlled by the developmental and inducible regulation of several benzylisoquinoline alkaloid biosynthetic genes, and by the subcellular compartmentation of biosynthetic enzymes and the intracellular localization and trafficking of pathway intermediates. In this paper, we review our current understanding of the biochemistry, cell biology, and molecular regulation of benzylisoquinoline alkaloid biosynthesis in plants. We also summarize our own research activities, especially those related to the establishment of protocols for the genetic transformation of benzylisoquinoline alkaloid-producing species, and the development of metabolic engineering strategies in these plants.