• Natural Product Sciences
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• v.11 no.3
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• pp.145-149
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• 2005

A methanol soluble extract from the dried hooks and stems of Uncaria rhynchophylla showed a strong inhibitory activity against monoamine oxidase in mouse brain. Using a bioassay-guided purification of this extract, a known ${\beta}-carboline$ type alkaloid, harman (1), was obtained as an active constituent. In addition, five known indole alkaloids, isocorynoxeine (2), isorhynchophylline (3), corynoxeine (4), cadambine (5), and $3{\alpha}-dihydrocadambine$ (6), were isolated and found to be weakly active or inactive.

• Bulletin of the Korean Chemical Society
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• v.26 no.12
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• pp.1975-1980
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• 2005

A series of substituted rutaecarpines were prepared by employing Fischer indole synthesis as key step and their inhibitory activities on COX-1 and 2 as well as selectivity on COX-2 were evaluated. The compounds with a methanesulfonyl and a bromo group at C10 showed promising inhibitory activity ($IC_{50}$ = 0.27, 0.35 $\mu$M, respectively) with selectivity.

• Journal of Microbiology and Biotechnology
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• v.25 no.2
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• pp.174-177
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• 2015

A potent α-glucosidase inhibitor (compound I) was isolated from coffee brews by activity-based fractionation and identified as a β-carboline alkaloid norharman (9H-pyrido[3.4-b]indole) on the basis of mass spectroscopy and nuclear magnetic resonance spectra (¹H NMR, ¹³C NMR, and COSY). The norharman showed potent inhibition against α-glucosidase enzyme in a concentration-dependent manner, with an IC₅₀ value of 0.27 mM for maltase and 0.41 mM for sucrase. A Lineweaver-Burk plot revealed that norharman inhibited α-glucosidase enzyme uncompetitively, with a K_i value of 0.13 mM.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.247.2-247.2
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• 2002

A synthetic naphthoquinone alkaloid. 2-amino-3-ethoxycarbonyl-l-methyl pyrolo (3,2-b) naphtho-4,9-dione (compound 1), showed a potent cytotoxicity in a panel of cancer cell lines with an IC50 ranged from 0.1 to 0.3 microgram/mL. Prompted by a potent cytotoxic activity, the mechanism action study was performed with cultured A549 of human lung cancer cells. Flow cytometric G2-M cell cycle arrest and microscopic investigation was also characterized with apoptotic morphological features. (omitted)

• Korean Journal of Microbiology
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• v.52 no.4
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• pp.415-420
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• 2016

Chemical study of an Arctic bacterium, Pseudomonas aeruginosa (Pseudomonadaceae) led to the isolation of two diketopiperazines 1 and 2, two phenazine alkaloids 3 and 4, and an indole carbaldehyde 5, along with a benzoic acid derivative 6. The structures of the compounds were confirmed by 1D and 2D NMR, and MS experiments, as well as by comparison of their data with published values. Among the isolates, compounds 5 and 6 were isolated for the first time from P. aeruginosa of the seawater of Arctic Chuckchi Sea. Antimicrobial activities of compounds 1‒6 against a Staphylococcus aureus and Candida albicans were evaluated.

• Applied Biological Chemistry
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• v.48 no.1
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• pp.1-15
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• 2005

Pathogens, insects and weeds have significantly reduced agricultural productivity. Thus, to increase the productivity, synthetic agricultural chemicals have been overused. However, these synthetic compounds that are different from natural products cannot be broken down easily in natural systems, causing the destruction of soil quality and agricultural environments and the gradually difficulty in continuous agriculture. Now agriculture is faced with the various problems of minimizing the damage in agricultural environments, securing the safety of human health, while simultaneously increasing agricultural productivity. Meanwhile, plants produce secondary metabolites to protect themselves from external invaders and to secure their region for survival. Plants infected with pathogens produce antibiotics phytoalexin; monocotyledonous plants produce flavonoids and diterpenoids phytoalexins, and dicotylodoneous plant, despite of infected pathogens, produce family-specific phytoalexin such as flavonoids in Leguminosae, indole derivatives in Cruciferae, sesquitepenoids in Solanaceae, coumarins in Umbelliferae, making the plant resistant to specific pathogen. Growth inhibitor or antifeedant substances to insects are terpenoids pyrethrin, azadirachtin, limonin, cedrelanoid, toosendanin and fraxinellone/dictamnine, and terpenoid-alkaloid mixed compounds sesquiterpene pyridine and norditerpenoids, and azepine-, amide-, loline-, stemofoline-, pyrrolizidine-alkaloids and so on. Also plants produces the substances to inhibit other plant growths to secure the regions for plant itself, which is including terpenoids essential oil and sesquiterpene lactone, and additionally, benzoxazinoids, glucosinolate, quassinoid, cyanogenic glycoside, saponin, sorgolennone, juglone and lots of other different of secondary metabolites. Hence, phytoalexin, an antibiotic compound produced by plants infected with pathogens, can be employed for pathogen control. Terpenoids and alkaloids inhibiting insect growth can be utilized for insect control. Allelochemicals, a compound released from a certain plant to hinder the growth of other plants for their survival, can be also used directly as a herbicides for weed control as well. Therefore, the use of the natural secondary metabolites for pest control might be one of the alternatives for environmentally friendly agriculture. However, the natural substances are destroyed easily causing low the pest-control efficacy, and also there is the limitation to producing the substances using plant cell. In the future, effects should be made to try to find the secondary metabolites with good pest-control effect and no harmful to human health. Also the biosynthetic pathways of secondary metabolites have to be elucidated continuously, and the metabolic engineering should be applied to improve transgenics having the resistance to specific pest.

• KSBB Journal
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• v.15 no.6
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• pp.609-614
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• 2000

Suspension cultures of Camptotheca acuminata, which is known to produce the anticancer indole alkaloid camptothecin and its derivatives, were made to increase camptothecin production. The capability of camptothecin production in suspended cells is decreased by repeated subculturein. Aggregated cells produced more camptothecin than single cells. Optimal cell aggregation was achieved in hybrid medium supplemented with 4% sucrose. Aggregated cells in hybrid medium with 4% sucrose produced $18.04{\times}10^{-4} mg/L$ of camptothecin. The control of shaking speeds was effective at inducing cell aggregation and camptothecin production. A shaking speed of 100 rpm was found optimum to increase the cell aggregation with a camptothecin production of $19.4{\times}10^{-4} mg/L$.

• Korean Journal of Medicinal Crop Science
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• v.17 no.3
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• pp.192-197
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• 2009

Camptotheca acuminata, a native of South China is a well known natural source of monoterpene-indole alkaloid camptothecin(CPT), one of the most promising anti-tumoural compounds. This study was conducted to optimize plant growth regulators and culture conditions on plantlets regeneration through organogenesis from callus of Camptotheca acuminta. Callus were induced from various explants of in vitro germinated plantlets of C. acuminta using WPM medium containing 0.2 ㎎/L 2,4-D. Hypocotyl segments were exhibited higher embryogenic callus than the other explants. Shoot buds formation from embryogenic callus was affected by plant growth regulators, pre-treated dark condition and liquid culture. Organogenesis was optimal in WPM liquid medium containing 0.5 ㎎/L BA. The dark pre-treatment for 2 weeks before the solid culture was effective for organogenesis. The regenerated shoots were rooted in WPM medium with 0.2 ㎎/L NAA and successfully acclimated in green-house conditions.

• KSBB Journal
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• v.15 no.5
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• pp.428-433
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• 2000

Cell cultures of Camptotheca acuminata, which is known to produce the anticancer indole alkaloid camptothecin and its dervatives, were made to enhance the productivity of camptothecin. In suspension cultures, the maximum cell growth rate in exponential growth phase was $0.269day^{-1}$ which was correlated to 2.58days of cell doubling time. The production of camptothecin was non-growth associated. The camptothecin production was the highest at 11th day form inoculation and then it decreased. Various elicitors were applied to enhance the production of camptothecin. Both of jasmonic acid and cellulase increased the production of camptothecin. The optimal dosing time of elicitor was the beginning of the cultures. The combination of two elicitors was more effective to produce camptothecin than single applications. $20.42{\times}10^{-3}mg/\ell$ of camptothecin was obtained with combined application of two elicitors in two days.

• The Korean Journal of Physiology and Pharmacology
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• v.23 no.3
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• pp.161-169
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• 2019

Fumigaclavine C (FC), an active indole alkaloid, is obtained from endophytic Aspergillus terreus (strain No. FC118) by the root of Rhizophora stylosa (Rhizophoraceae). This study is designed to evaluate whether FC has anti-adipogenic effects in 3T3-L1 adipocytes and whether it ameliorates lipid accumulation in high-fat diet (HFD)-induced obese mice. FC notably increased the levels of glycerol in the culture supernatants and markedly reduced lipid accumulation in 3T3-L1 adipocytes. FC differentially inhibited the expressions of adipogenesis-related genes, including the peroxisome proliferator-activated receptor proteins, CCAAT/enhancer-binding proteins, and sterol regulatory element-binding proteins. FC markedly reduced the expressions of lipid synthesis-related genes, such as the fatty acid binding protein, lipoprotein lipase, and fatty acid synthase. Furthermore, FC significantly increased the expressions of lipolysis-related genes, such as the hormone-sensitive lipase, Aquaporin-7, and adipose triglyceride lipase. In HFD-induced obese mice, intraperitoneal injections of FC decreased both the body weight and visceral adipose tissue weight. FC administration significantly reduced lipid accumulation. Moreover, FC could dose-dependently and differentially regulate the expressions of lipid metabolism-related transcription factors. All these data indicated that FC exhibited anti-obesity effects through modulating adipogenesis and lipolysis.