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20(R)-Ginsenoside Rg3와 20(S)-Ginsenoside Rg3의 HaCaT 세포 이동성과 침윤성에 대한 효과
김상원(Sang-Won Kim),노영찬(Young-Chan Noh),박소연(So-Yeon Park),이미진(Mijin Lee),최희지(Hui-Ji Choi),송규용(Gyu-Yong Song),김항건(Hangun Kim) 대한약학회 2021 약학회지 Vol.65 No.2
Wound healing in the skin is a complex process involving several steps. First is the inflammation stage, in which the wound causes constriction of damaged blood vessels and the aggregation of platelets, aiding neutrophils and macrophages in removing the damaged tissue and preventing infection. This is followed by the proliferation stage involving keratinocytes and fibroblasts. Finally, in the tissue remodeling stage, the wound healing process is completed through contraction of the wound area, which promotes the growth of new tissue. In particular, the migration of keratinocytes and fibroblasts during the proliferation stage to the wound site and penetration of these cells into the surrounding tissues promote the wound healing process. In this study, we performed MTT assays to evaluate the toxicity of 20(R)-Rg3 and 20(S)-Rg3, stereoisomers of ginsenoside Rg3, an active ingredient of Korean ginseng, on the keratinocytes and fibroblasts involved in the proliferation stage. Migration assays, invasion assays, and quantitative reverse transcription polymerase chain reaction (qRT-PCR) were used to assess the expression of genes related to wound healing. We observed that 20(R)-Rg3 was non-toxic and promoted the expression of COL1A2 and ACTC1, genes related to wound healing, thereby increasing the mobility and invasiveness of keratinocytes. In addition, we confirmed that 20(R)-Rg3 increased the initial rate of wound healing in vivo in BALB/c mice. The positive effect of 20(R)-Rg3 on wound healing can be assessed by separating this isomer from 20(S)-Rg3, which has moderate toxicity against keratinocytes and reduces mobility and invasiveness. Thus, 20(R)-Rg3 optical isomers could be potential candidates for the development of effective wound healing medicines.
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비소세포폐암에서 Gefitinib 내성 극복을 위한 효과적인 화합물 합성 및 항암 활성 평가
김광일(Kwang Il Kim),박소연(So-Yeon Park),최대옥(Daeock Choi),김항건(Hangun Kim) 대한약학회 2024 약학회지 Vol.68 No.2
Lung cancer remains a leading cause of global cancer-related mortality, emphasizing the need for innovative strategies to combat resistance to the first-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs), Gefitinib. This study aimed to discover and evaluate small molecule compounds selectively inhibiting Gefitinib resistance. A compound library was screened against adenocarcinoma (A549), EGFR-mutant NSCLC (H1975 and PC9), and Gefitinib-resistant NSCLC (PC9GR) cell lines. The study identified W1 as a promising lead compound, and its derivative, compound W3, exhibited excellent efficacy in PC9 and PC9GR cells. These findings underscore the potential of W3, an 4-anilinopyrimidine derivative, as an inhibitor of Gefitinib resistance in NSCLC. This research contributes valuable insights to the ongoing efforts in developing effective and sustainable treatment options for lung cancer patients facing EGFR-TKI resistance.
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동소이식 유방암 근적외선 이미징을 이용한 우스닉산 칼륨염의 항암 효능 평가
손예선(Yeseon Son),이창욱(Changwook Lee),유인탁(In Tag Yu),이미진(Mijin Lee),김항건(Hangun Kim) 대한약학회 2022 약학회지 Vol.66 No.5
Mouse cancer models are useful tools for evaluating in vivo tumor growth and metastasis, providing valuable information for preclinical testing. In this process, optical imaging enables the mouse models to easily identify the progress of disease in a non-invasive way. Here, we established an experimental bioimaging animal model of near-infrared (NIR) fluorescence by using a fluorescence-labeled organism bioimaging instrument (FOBI) and evaluated the anti-cancer effect of potassium usnate (KU) in an orthotopic breast cancer model. The cell viability assay revealed that KU had cytotoxicity with half maximal inhibitory concentration of approximately 138.57, 167.69, and 144.17 μM in 4T1-Fluc-Neo/iRFP-Puro (4T1-iRFP), MDA-MB-231, and MCF-7 cells, respectively. The measurement of NIR fluorescence from the 4T1-iRFP cells in a microtube via FOBI exhibited a strong correlation between cell number and fluorescence intensity, and the minimal detection limit was 10⁵ cells. Accordingly, NIR imaging was performed on the orthotopic breast cancer mouse model by using FOBI, and regression of tumor progression through intraperitoneal KU administration was successfully monitored. Our results demonstrated the establishment of NIR imaging in the orthotopic breast cancer animal model for evaluating the anti-cancer effect of KU.
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