• 농약과학회지
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• 제5권1호
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• pp.24-29
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• 2001

은행잎함유 살충성분인 bilobalide의 활성부위를 조사하기 위해 bilobalide를 가수분해 및 산화를 시킨 후 구조를 확인하고 살충활성을 검정하였다. 분해물의 분석 결과, 염기에 의한 가수분해물은 cyclopentenone 계열의 화합물로 밝혀졌고, 산화물은 trilactone 형태를 유지한 sesquiterpene 구조로써 dehydration된 형태로 추정되었다. 분해물의 살충활성을 검정한 결과, 살충력의 크기는 bilobalide, monoacetyl 유도체, ginkgolide C, 산화분해물, diacetyl 유도체, 가수분해물의 순으로 감소하여 bilobalide의 살충력을 나타내는데에는 trilactone의 구조를 유지하는 것이 중요한 것으로 나타났다.

• International Journal of Oral Biology
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• 제45권1호
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• pp.8-14
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• 2020

Bilobalide isolated from the leaves of Ginkgo biloba has several pharmacological activities such as neuroprotective, anti-inflammatory, and anticonvulsant. However, the effect of bilobalide on cancer has not been clearly established. The main purpose of this study was to investigate the effect of bilobalide on cell growth and apoptosis induction in FaDu human pharyngeal squamous cell carcinoma. This was examined by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay, nuclear 4′,6-diamidino-2-phenylindole dihydrochloride staining, DNA fragmentation analysis, and immunoblotting. Bilobalide inhibited the growth of FaDu cells in dose- and time-dependent manners. Treatment with bilobalide resulted in nuclear condensation and DNA fragmentation in FaDu cells. Furthermore, it promoted the proteolytic cleavage of procaspase-3/-7/-8/-9 with increase in the amount of cleaved caspase-3/-7/-8/-9. Bilobalide-induced apoptosis in FaDu cells was mediated by the expression of Fas and the activation of caspase-8, caspase-3, and poly (ADP-ribose) polymerase. Immunoblotting revealed that the antiapoptotic mitochondrial protein Bcl-2 was downregulated, but the proapoptotic protein Bax was upregulated by bilobalide in FaDu cells. Bilobalide significantly increased Bax/Bcl-2 ratio. These results suggest that bilobalide inhibits cell proliferation and induces apoptosis in FaDu human pharyngeal squamous cell carcinoma via both the death receptor-mediated extrinsic apoptotic pathway and the mitochondrial-mediated intrinsic apoptotic pathway.

• Biotechnology and Bioprocess Engineering:BBE
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• 제9권1호
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• pp.35-40
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• 2004

Ginkgolides (GK) and bilobalide are valuable compounds that belong to the lactone terpene. The contents of these metabolites were determined by HPLC from female and male tree of Ginkgo biloba L. The productivity of G. biloba cells was also compared with the corresponding individual trees. High variations in the ginkgolides and bilobalide were observed from different individuals, plant parts, and cultured cells. The ginkgolides and bilobalide contents were different depending on the plant parts. Callus was obtained from various plant tissues, and NAA was better at callogenesis than 2,4-D in both the female and male trees. The plants and their corresponding cells showed considerable variation in their ginkgolides and bilobalide concentrations. The ginkgolides and bilobalide contents were not correlated with the production between dominant trees and their corresponding cells. Light irradiation enhanced the production of GK-A and GK-B, however, the concentration of bilobalide decreased under dark conditions.

• 약학회지
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• 제41권1호
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• pp.111-116
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• 1997

The neurotoxicity induced by L-glutamate in primary cultures of rat cortical cells could be attenuated by sesquiterpene constituent of Ginkgo biloba leaves, bilobalide. At the c oncentration of 100 nM, Bilobalide elevated the combined levels of reduced/oxidized glutathione in rat cortical cells exposed to 100 ${\mu}$M glutamate. Furthermore, bilobalide promoted a reduction in superoxide dismutase activity in glutamate-treated cells. Finally, bilobalide markedly inhibited the production of malondialdehyde. a measure of lipid peroxidation, in glutamate-treated rat cortical cells.

• Biotechnology and Bioprocess Engineering:BBE
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• 제9권1호
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• pp.41-46
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• 2004

The influence of various culture conditions on growth and ginkgolides (GKA and GKB), and bilobalide formation in callus and suspension cultures of Ginkgo biloba were investigated. Callus induced from the leaf petioles exhibited distinct morphological and physiological responses. The cell biomass and ginkgolides content varied among the cell lines; brownish callus lines produced high levels of ginkgolides and bilobalide in spite of poor cell growth. Among the culture media used, MS medium showed significant effect on cell growth and ginkgolides production. Low concentration of sucrose (3%) improved cell growth, while higher sucrose levels (5 and 7%) improved ginkgolides production. Cultivation of callus cultures above 28$^{\circ}C$ dramatically reduced their growth rate; however the cell lines grown at 36$^{\circ}C$ showed increased levels of bilobalide content. A 2.5-L balloon type bubble bioreactor (BTBB) was successfully developed for the cell growth and ginkgolides production.

• KSBB Journal
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• 제25권2호
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• pp.173-178
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• 2010

Antifungal effect of Ginkgo biloba leaves extracts conducted for Pityrosporum ovale. Antifungal effect verified by diffusion test, optical density test and colony counting test under various concentration. Extract of ginkgo biloba leaves performed with 40% ethanol and 60% water solution at $60^{\circ}C$ and major components analyzed by HPLC. The concentrated extract have bilobalide and ginkgolide A and ginkgolide B and their concentration were 153.0 mg/L, 8403.5 mg/L and 2723.0 mg/L respectively. Ginkgo biloba leaves extracts gave 99.1% of antifungal effect for Pityrosporum ovale examined by colony counting method.

• Applied Biological Chemistry
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• 제48권2호
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• pp.150-154
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• 2005

천연식물자원으로부터 생물농약을 개발하기 위하여 점박이응애(Tetranichus urticae), 목화진딧물(Aphis gossypii)과 복숭아혹진딧물(Myzus persicae)에 대해 푸른은행잎 추출물(GG-W80)과 노란은행잎 추출물(YG-W80)의 살충효과와 기피효과를 leaf disk법과 유묘검정법에 의해 조사하였다. 점박이응애에 대한 살충효과는 GG-W80이 98.3%로 YG-W80의 20.0%보다 우수하였다. 점박이응애에 강한 살충효과를 보이는 생리활성물질은 high performance liquid chromatography(HPLC)를 이용해 동정하였다. 푸른은행잎 추출물에서는 각각 bilobalide $611\;{\mu}g/kg$, ginkgolide A $37\;{\mu}g/kg$와 ginkgolide B $243\;{\mu}g/kg$이 동정되었으며, 노란은행잎 추출물에서는 bilobalide $214\;{\mu}g/kg$와 ginkgolide B $46\;{\mu}g/kg$이 동정되었으나 ginkgolide A는 확인되지 않았다. 이상의 결과는 은행잎에 존재하는 terpene계 화합물인 bilobalide와 ginkgolide A, B가 점박이응애에 살충력을 갖고 있음을 알수 있으며, 이들 성분을 포함한 은행잎 추출물이 점박이응애에 대한 생물학적 방제 가능성을 가지고 있음을 시사하였다.

• 대한본초학회지
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• 제30권1호
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• pp.85-93
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• 2015

Objectives : Bilobalide (BIL) is a predominant sesquiterpene trilactone constituent that accounts for a partial portion of the standardized Ginkgonis Folium extract, which has been widely used to treat a variety of neurological disorders involving cerebral ischemia and neurodegeneration. In this study, it was tested whether BIL exhibits anti-inflammatory activities on inflammation response, or not. Methods : To elucidate the molecular mechanisms of BIL on pharmacological and biochemical actions in inflammation, we examined the effect of BIL on pro-inflammatory mediators in lipopolysaccharide (LPS)-stimulated macrophages. The investigation was focused on how BIL affect on inflammation-related mediators including various signals such as nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$), inducible NO synthase(iNOS), cyclooxygenase-2(COX-2), interleukin-6(IL-6), tumor necrosis $factor-{\alpha}$ ($TNF-{\alpha}$), mitogen-activated protein kinases(MAPKs) and nuclear factor kappa-light-chain-enhancer of activated B cells ($NF-{\kappa}B$) in LPS-stimulated RAW 264.7 cells. Results : We found that BIL inhibited LPS-induced NO, $PGE_2$, IL-6 and $TNF-{\alpha}$ productions as well as the expressions of iNOS and COX-2. Furthermore, BIL suppressed the LPS-induced phosphorylation for MAPK activation. Conclusions : These results suggest that BIL has inhibitory effects on LPS-induced $PGE_2$, NO, IL-6 and $TNF-{\alpha}$ production, as well as the expressions of iNOS and COX-2 in the murine macrophage. It seems that these inhibitory effects occur by blocking the phosphorylation of MAPKs for activation. Then, BIL suppressed the activation of nuclear factor $NF-{\kappa}B$ in nucleus. These observations suggest that BIL has anti-inflammatory effect by inhibiting.

• Bulletin of the Korean Chemical Society
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• 제32권9호
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• pp.3261-3266
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• 2011

The interaction of bilobalide (BB) and ginkgolides B (GB) with bovine serum albumin (BSA) was investigated by fluorescent technique and UV/vis absorption spectroscopy. The results showed that BB and GB could intensively quench the fluorescence of BSA through a static quenching procedure. The binding constants (Ka) and the average binding distance between the donor (BSA) and the acceptor (ginkgolides) were obtained ($r_{BB}$ = 5.33 nm and $r_{GB}$ = 4.20 nm) by the theory of non-radiation energy transfer, and then the thermodynamic parameters such as ${\Delta}S^0$ (0.17-0.32 kJ/mol), ${\Delta}G^0$ (-20.76 ~ -17.79 kJ/mol) and ${\Delta}H^0$ (32.47-76.52 kJ/mol) could be calculated, respectively. All these results revealed that the interaction of BB and GB with BSA were driven mainly by hydrophobie force. The synchronous fluorescence spectroscopy was applied to examine the effect of two ginkgolides on the configuration of BSA. The configuration alteration of BSA could be induced by the hydrophobicitv environment of tyrosine with the increase of the drug concentration.

• KSBB Journal
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• 제21권4호
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• pp.312-316
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• 2006

본 연구에서는 은행잎 추출물의 Staphylococcus aureus에 대한 항균효과를 검증하기 위해 먼저 에탄올 농도별로 bilobalide와 ginkgolide A, B의 성분을 분석한 결과 40% 에탄올 용매를 최적 활성농도로 결정하였다. Disc diffusion test, Optical density test을 통한 S. aureus 항균실험 결과 에탄올 추출농도가 증가할수록 항균효과가 증가하나 40% 에탄올 이상에서는 항균활성에 큰 차이가 없었다. 주사전자현미경을 통하여 은행잎 에탄올 40% 추출물 16배 농축액을 처리한 균의 세포표면을 확인한 결과 심하게 손상되었음을 확인할 수 있었다. 투과전자현미경을 이용하여 관찰한 결과 은행잎 추출물로 처리한 균주에서는 세포벽이 관찰되지 않았으며, 이는 은행잎 추출물의 주성분인 bilobalide와 ginkgolide A, B가 세포벽 합성을 저해하는 것으로 보여진다.