• Journal of Applied Biological Chemistry
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• 제62권1호
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• pp.31-38
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• 2019

Scutellaria baicalensis Georgi (Scutellariae Radix)는 이뇨제, 고지혈증, 항박테리아, 항알레르기, 항염증제 및 항암제와 같은 건강보조식 및 전통 생약으로도 널리 사용되어 왔다. 본 연구에서 복잡한 S. baicalensis 추출물에서 지표 물질 또는 유효화합물들을 분리하는 것은 신원 확인 및 생리활성 평가를 위한 필수적인 단계다. 8개의 성분들로 구성된 타겟 분획물을 두개의 gradient elution를 사용하여 고성능 액체 크로마토 그래피에서 분석하였다. 중압 액체크로마토그래피 및 개방형칼럼으로 분취를 시뮬레이션함으로 예비실험에서 충분히 분리가 되도록 용리 조건을 결정할 수 있었다. 최적 분취방법으로 확보된 표준유효분획물로부터 8개의 지표성분들이 포함된 것을 확인하였다. 또한, 분획물은 UPLC-QTof-MS 비교 분석으로 MS, UV, HRESIMS 결과를 확인할 수 있었다. 따라서, 스케일 업 실험법은 S. baicalensis 추출물에 성공적으로 적용될 수 있었다.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Signal transduction in Toxicology
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• pp.9-13
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• 2001

Genistein, a natural isoflavonoid phytoestrogen, is a strong inhibitor of protein tyrosine kinase and DNA topoisomerase II activities. Genistein has been shown to have anticancer proliferation, differentiation and chemopreventive effects. In the present study, we have addressed the mechanism of action by which genistein suppressed the proliferation of p53-null human prostate carcinoma cells.(omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.75-78
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• 2003

Polyketides are a class of structurally diverse natural products which possess a wide range of biological activities. These compounds are used throughout medicine and agriculture as antimicrobials, immunosuppressants, antiparasitics, and anticancer agents. While structurally diverse, polyketides are assembled by a common mechanism of decarboxylative condensations of simple malonate derivatives by polyketide synthases (PKSs) in a manner very similar to fatty acid biosynthesis (Fig 1). (omitted)

• Journal of Ginseng Research
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• 제44권5호
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• pp.704-716
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• 2020

Background: Ginsenoside Rh2 (GRh2) is a characterized component in red ginseng widely used in Korea and China. GRh2 exhibits a wide range of pharmacological activities, such as anti-inflammatory, antioxidant, and anticancer properties. However, its effects on Toxoplasma gondii (T. gondii) infection have not been clarified yet. Methods: The effect of GRh2 against T. gondii was assessed under in vitro and in vivo experiments. The BV2 cells were infected with tachyzoites of T. gondii RH strain, and the effects of GRh2 were evaluated by MTT assay, morphological observations, immunofluorescence staining, a trypan blue exclusion assay, reverse transcription PCR, and Western blot analyses. The in vivo experiment was conducted with BALB/c mice inoculated with lethal amounts of tachyzoites with or without GRh2 treatment. Results and conclusion: The GRh2 treatment significantly inhibited the proliferation of T. gondii under in vitro and in vivo studies. Furthermore, GRh2 blocked the activation of microglia and specifically decreased the release of inflammatory mediators in response to T. gondii infection through TLR4/NF-κB signaling pathway. In mice, GRh2 conferred modest protection from a lethal dose of T. gondii. After the treatment, the proliferation of tachyzoites in the peritoneal cavity of infected mice markedly decreased. Moreover, GRh2 also significantly decreased the T. gondii burden in mouse brain tissues. These findings indicate that GRh2 exhibits an antieT. gondii effect and inhibits the microglial activation through TLR4/NF-κB signaling pathway, providing the basic pharmacological basis for the development of new drugs to treat toxoplasmic encephalitis.

• 통합자연과학논문집
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• 제9권3호
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• pp.161-165
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• 2016

The p21-activated kinase-1 (PAK1) has emerged as a potential target for anticancer therapy. It is overexpressed in ovarian, breast and bladder cancers. This suggests that PAK1 may contribute to tumorigenesis. 4-azaindole derivatives are reported as potent PAK1 inhibitors. The present work deals with the molecular docking studies of 4-azaindoles with PAK1. Probable binding mode of these inhibitors has been identified by molecular modeling. Docking results indicated that hydrogen bonding interactions with Glu345 and Leu347 are responsible for governing inhibitor potency of the compounds. Additionally, Val284, Val328, Met344 and Leu396 were found to be accountable for hydrophobic interactions inside the active site of PAK1.

• International Journal of Oral Biology
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• 제46권2호
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• pp.85-93
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• 2021

Asarum sieboldii Miq. (Aristolochiaceae) is a perennial herbaceous plant and has been used as traditional medicine for treating diseases, cold, fever, phlegm, allergies, chronic gastritis, and acute toothaches. Also, it has various biological activities, such as antiallergic, antiinflammatory, antinociceptive, and antifungal. However, the anticancer effect of A. sieboldii have been rarely reported, except anticancer effect on lung cancer cell (A549) of water extracts of A. sieboldii. This study investigated the anticancer activity of methanol extracts of A. sieboldii (MeAS) and the underlying mechanism in human FaDu hypopharyngeal squamous carcinoma cells. MeAS inhibited FaDu cells grown dose-dependently without affecting normal cells (L929), as determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and live and dead assay. In addition, concentration of MeAS without cytotoxicity (0.05 and 0.1 mg/mL) inhibited migration and colony formation. Moreover, MeAS treatment significantly induced apoptosis through the proteolytic cleavage of caspase-3, -7, -9, poly (ADP-ribose) polymerase, and downregulation of Bcl-2 and upregulation of Bax in FaDu cells, as determined by fluorescence-activated cell sorting analysis, 4'6-diamidino-2-phenylindole stain, and western blotting. Altogether, these results suggest that MeAS exhibits strong anticancer effects by suppressing the growth of oral cancer cells and the migration and colony formation via caspase- and mitochondrial-dependent apoptotic pathways in human FaDu hypopharyngeal squamous carcinoma cells. Therefore, MeAS can serve as a natural chemotherapeutic for human oral cancer.

• Asian Pacific Journal of Cancer Prevention
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• 제16권14호
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• pp.6117-6121
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• 2015

Background: Most northeast Thai vegetables may play roles in human health by acting as antioxidant and anticancer agents. Recent study showed that Cratoxylum formosum subsp. pruniflorum (Kurz.) Gogel. (Teawdang) could inhibit growth of liver cancer cell lines. Cervical cancer, which has human papilloma virus as its main cause, is found at high incidence in Thailand. Due to increasing drug resistance, searches for potential anticancer compounds from natural source are required. Therefore, our purpose was to evaluate the cytotoxicity of Teawdang extracts in cervical cancer cell lines. Materials and Methods: Teawdang edible parts, purchased from Khon Kaen market during July-October 2013 was extracted with organic solvent. Phenolic profiles of crude hexane (CHE), ethyl acetate (CEE), methanol (CME) and water (CWE) extracts were performed by high performance liquid chromatographic (HPLC) techniques. Their cytotoxic effects on cervical cancer cells were investigated with HPV-non infected (C-33A) and HPV-infected (HeLa and SiHa) cell lines. Results: HPLC profiles showed that all crude extracts contained caffeine, ferulic acid and resveratrol. CME and CEE had high contents of gallic acid and quercetin. Catechin was found only in CWE. Cytotoxicity test showed that CEE had the lowest IC50 on HeLa ($143.18{\pm}13.35 {\mu}g/mL$) and SiHa cells ($106.45{\pm}15.73{\mu}g/mL$). C-33A cells were inhibited by CWE ($IC50=130.95{\pm}3.83{\mu}g/mL$). Conclusions: There were several phenolic compounds in Teawdang extracts which may have cytotoxic effects on cervical cancer cell lines. Investigation of these bioactive compounds as new sources of anticancer agents is recommended.

• 생약학회지
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• 제18권2호
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• pp.127-135
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• 1987

In vitro sensitivity testing was performed for 21 kinds putative anticancer drugs selected from references and information. Cellular damage of P815 mastocytoma cells following exposure to water extracts of drugs was evaluated by colony formation assay. Highly effective drugs with more than 50% inhibition of colony formation were seven (Houttuyniae Herba, Sanguisorbae Radix, Nepetae Herba, Manitis Squama, Lonicerae Flos, Amomi Semen, Polyporus), though not more effective than BCNU. According to the results of $^3H-thymidine$ incorporation assay for determination of selective cytotoxicity, 3 of these drugs (Houttuyniae Herba, Polyporus, Manitis Squama) were found to be low cytotoxic to normal mouse lymphoid cells. These findings suggest that the above 3 drugs may be used for effective anticancer drugs in vivo.

• 생명과학회지
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• 제23권4호
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• pp.518-528
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• 2013

꿀풀과(Labiatae)에 속하는 황금(黃芩, S. baicalensis)은 한국, 중국, 몽골 및 시베리아 동부 등지에 분포하는 여러해살이 초본식물로서 예로부터 민간처방 약재로 사용되었으며, 한방에서는 뿌리 말린 것을 이질, 발열 및 황달의 치료제로 사용되고 있다. 또한 최근 연구에 따르면 황금 추출물은 항염증, 항당뇨, 항균, 항알레르기, 항바이러스, 항고혈압, 항산화 및 항암 효능을 가지는 것으로 알려져 있으나 신세포암에서의 항암효능 및 분자생물학적 기전에 대해서는 명확히 밝혀져 있지 않다. 본 연구에서는 인체 신세포암 Caki-1 세포에서 황금 에탄올 추출물(ethanol extract of S. baicalensis, EESB)이 유발하는 항암효과 및 항암기전을 조사하였다. 본 연구의 결과에 의하면 EESB 처리에 의한 Caki-1 세포의 증식억제는 apoptosis 유발과 밀접한 연관이 있었으며, 이는 DR4 Fas ligand 및 Bax 단백질의 발현 증가와 Bid, XIAP 및 cIAP-1의 발현 억제와 관련이 있었다. EESB는 또한 미토콘드리아의 기능 손상과 caspase-3의 기질단백질인 PARP, ${\beta}$-catenin 및 $PLC{\gamma}$-1 단백질의 단편화를 유발하였다. 그러나 EESB 처리에 의하여 유발되었던 apoptosis가 pan-caspases inhibitor인 z-VED-fmk를 이용하여 caspases의 활성을 억제하였을 경우 현저하게 감소되어, EESB에 의한 apoptosis 과정에 caspase의 활성 증대가 중요한 역할을 한다는 것을 알 수 있었다. 이러한 결과들은 황금의 항암작용을 이해하는데 중요한 자료가 될 것이고 나아가 향후 수행될 추가 실험을 위한 기초 자료로서 그 가치가 매우 높을 것으로 생각된다.

• 생약학회지
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• 제18권2호
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• pp.118-126
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• 1987

Natural Killer cells are considerd to play an important role in antitumor immune surveilance mechanism. In this study, 21 putative anticancer drugs selected from reference were assessed by evaluating the effect on rat Natural Killer cell activity (NKCA). All 21 herb drugs were extracted in boiling water, lyophilized, autoclaved, and then used for experiment. Culture supernatant of concanavalin-A (Con-A)-stimulated rat spleen cells as a source of lymphokine was also used as a control of comparison. Rat spleen cells were used as effector and NKCA was measured in 4hr $^{51}Cr-release$ assay against Yac-1 mouse lymphoma cell line. In order to determine the optimal conditions for NKCA augmentation, effector cells were treated with 3 different concentrations of each drug for 24, or 48 hrs before testing of NKCA, In optimal conditions determined from previous results, the effect of herb drugs on NKCA were assessed in 3 to 5experiments. NKCA was significantly enhanced by treatment with 4 herb drugs(Ponciri Fructus, Houttuyniae Herba, Aurantii Pericarpium, Nepetae Herba). Culture supernatant of Con-A-stimulated spleen cells also augmented the rat NKCA more significantly. The results show that 4 of the herb medicines supposed to display anticancer effect may have activity as a biological response modifier through augmentation of NKCA.