• Archives of Pharmacal Research
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• v.24 no.4
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• pp.270-275
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• 2001

Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (birding assay) for NMDA receptor glycine site.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.34-37
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• 1998

Combinatorial chemistry is one of the most interested topics in the area of drug discovery. One of the most important points is how to find a lead compound that gives the seed structure for designing of a combinatorial library. Natural products is suitable for searching a new bioactive compound with new structure. We have carried out systematic screening works to find natural products possessing the effects on inter-and intra-cellular signaling. Two hundreds extracts of medical plants and two thousands microbial culture broth samples have been tested for the induction and inhibition of IL-2 or IL-6 production (Fig. 1). ELISA is an efficient method for screenings from such a large number of samples. Now, we apply this method to search prion- binding agents.

• CELLMED
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• v.2 no.2
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• pp.14.1-14.7
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• 2012

Cordycepin, a nucleoside derivative, was extracted from $Cordyceps$ $sinensis$, and then proved to be a bioactive compound present in traditional Chinese medicine Cordyceps. Early investigations revealed cordycepin possessed anti-microbial activity mainly by inhibiting nucleic acid synthesis. Although cordycepin is not used as antibacterial agents in clinic, its other pharmacological effects and possible mechanisms have gradually been deeply studied. This review serves to summarize the research progress of cordycepin.

• Archives of Pharmacal Research
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• v.24 no.4
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• pp.300-306
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• 2001

A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.

• Journal of Microbiology
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• v.39 no.4
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• pp.254-264
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• 2001

Sponges are host organisms for various symbiotic microorganisms such as archaea, bacteria, cyano-bacteria and microalgae. Sponges are also sources of a wide variety of useful natural products like cyto-toxins. antifouling agents, antibiotics, and anti-inflammatory and antiviral compounds, Symbiotic microorganisms is sponges can be sources of various natural products, because metabolites previously ascribed to sponges have recently been demonstrated to be biosynthesized by symbionts. If a symbiotic microorganisms from which some natural products are derived can be cultured, the microorganism could be used in a mass production of the bioactive comopounds. We summarize recent research on iso-lation and cultivation of sponge-symbiotic microorganisms and the symbiotic relationship.

• Journal of Pharmacopuncture
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• v.19 no.3
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• pp.246-252
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• 2016

Objectives: The purpose of this study was to obtain a natural antibiotic from Phenol-rich compounds; for the dressing and the treatment of chronic wounds. Methods: The Phenol-rich compound sweet gel was prepared by blending four natural herbal extracts, Acacia catechu (L.F.), Momia (Shilajit), Castanea sativa, and Ephedra sinica stapf, with combination of a sweet gel medium, including honey, maple saps, Phoenix dactylifera L. (date), pomegranate extract and Azadirachta indica gum as a stabilizer. The combinations were screened by using a well-diffusion assay with cloxacillin as a control. Pseudomonas spp. was tested with our novel antimicrobial compound. The zones of inhibition in agar culture were measured for each individual component and for the compound, and the results were compared with those of the control group which had been treated with cloxacillin. Data were expressed as means ${\pm}$ standard deviations. Quantitative analyses were performed using the paired t-test. Results: The antibiotic effect of the Phenol-rich compound sweet gel was statistically shown to be more significant than that of cloxacillin against Pseudomonas aeruginosa (P < 0.05). Conclusion: Our novel approach to fighting the antibiotic resistance of Pseudomonas proved to be successful. The Phenol-rich compound sweet gel was found to be suitable for use as an alternative medicine and bioactive dressing material, for the treatment of patients with various types of wounds, including burns, venous leg ulcers, ulcers of various etiologies, leg ulcers on the feet of diabetic, unhealed graft sampling sites, abscesses, boils, surgical wounds, necrotic process, post-operative and neonatal wound infection, and should be considered as an alternative to the usual methods of cure.

• Natural Product Sciences
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• v.24 no.2
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• pp.79-81
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• 2018

Norcolensoic acid (1) was isolated from both the fruiting bodies and the liquid culture of Lachnum virgineum. The structures of 1 was determined using spectroscopic methods. Compound 1 was isolated for the first time from this fungus. Compound 1 showed moderate antibacterial and phytotoxic activities.

• Journal of Ginseng Research
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• v.46 no.2
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• pp.304-314
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• 2022

Background: Ginsenosides are biologically active components of ginseng and have various functions. In this study, we investigated the immunomodulatory activity of a ginseng product generated from ginseng powder (GP) via enzymatic bioconversion. This product, General Bio compound K-10 mg solution (GBCK10S), exhibited increased levels of minor ginsenosides, including ginsenoside-F1, compound K, and compound Y. Methods: The immunomodulatory properties of GBCK10S were confirmed using mice and a human natural killer (NK) cell line. We monitored the expression of molecules involved in immune responses via enzyme-linked immunosorbent assay, flow cytometry, NK cell-targeted cell destruction, quantitative reverse-transcription real-time polymerase chain reaction, and Western blot analyses. Results: Oral administration of GBCK10S significantly increased serum immunoglobulin M levels and primed splenocytes to express pro-inflammatory cytokines such as interleukin-6, tumor necrosis factor-α, and interferon-γ. Oral administration of GBCK10S also activated NK cells in mice. Furthermore, GBCK10S treatment stimulated a human NK cell line in vitro, thereby increasing granzyme B gene expression and activating STAT5. Conclusion: GBCK10S may have potent immunostimulatory properties and can activate immune responses mediated by B cells, Th1-type T cells, and NK cells.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.781-785
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• 2002

A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

• Korean Journal of Food Science and Technology
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• v.52 no.5
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• pp.503-509
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• 2020

The present study investigated the effects of dry and moist heat treatments on total phenols, total anthocyanins, and antioxidant activity levels in black chokeberry (Aronia melanocarpa) fruits. Lyophilized chokeberry powder samples were heated in a drying oven at 60, 100, 160, 180, and 200℃ for 20, 40, or 60 min. Finely ground fresh chokeberry fruits were heated in water at 60, 80, and 100℃ for 20 min, and bioactive compound and antioxidant activity levels were measured. The bioactive compounds and antioxidant activity decreased with increasing temperature and treatment duration. Antioxidant activity was preserved at 160℃ or lower without significant loss for dry heating, whereas moist heat treatment increased both bioactive compounds and antioxidant activity with increasing temperature.