• Title/Summary/Keyword: Anticancer drug

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Comparative Analysis of Anticancer and Antibacterial Activities among Seven Trametes Species

  • Ha Thi Kim Nguyen;Jiwon Lee;Yejin Park;Hyon Jin Park;Soon Kil Ahn;Jae Kwang Kim;Dong-Ku Kang;Minkyeong Kim;Chorong Ahn;Changmu Kim;Jaehyuk Choi
    • Mycobiology
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    • v.51 no.4
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    • pp.256-263
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    • 2023
  • Species in the genus Trametes (Basidiomycota, Polyporales) have been used in natural medicine for a long time. Many studies reported that mycelia or fruiting bodies of Trametes spp. exhibited effects of antioxidant, anti-inflammatory, anticancer, and antimicrobial activities. However, comparative analysis in this genus is scarce due to limitation of morphological identification and the sample number. In this study, the 19 strains of seven Trametes species were chosen to generate a five-gene-based phylogeny with the 31 global references. In addition, 39 culture extracts were prepared for 13 strains to test for anticancer and antibacterial activities. Strong anticancer activities were found in several extracts from T. hirsuta and T. suaveolens. Anticancer activities of T. suaveolens, T. cf. junipericola and T. trogii were first described here. The antibacterial ability of T. versicolor and T. hirsuta extracts has been confirmed. The antibacterial activities of T. suaveolens have been reported at the first time in this study. These results suggest an efficient application of the genus Trametes as the drug resources especially for anticancer agents.

Anticancer Activity and Chemical Composition of a Non-Polar Fraction from Asiasari Radix et Rhizoma (세신 비극성 분획의 항암 활성 및 성분 분석)

  • Cho, Seung-Sik;Kang, Bok Yun;Bae, Min-Suk;Shim, Jung-Hyun;Kim, Hyun Jung;Yoon, Goo
    • Korean Journal of Pharmacognosy
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    • v.51 no.4
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    • pp.264-269
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    • 2020
  • The study aimed to characterize chemical composition and anticancer property of the n-hexane fraction derived from Asiasari Radix et Rhizoma. The anticancer activity was evaluated on a panel of cancer cell lines including HN22, HSC2, HSC3, and HSC4 cells (human oral cancer), HCC827 and HCC827GR cells (human lung cancer), and KYSE30 and KYSE450 (human esophageal cancer) by MTS assay. As a result, The least polar subfraction from n-hexane-soluble layer displayed notable cytotoxicity on the tumor cell lines with IC50 ranging from 1.20 to 17.0 ㎍/ml. The chemical composition of constituents in the active subfraction was determined by gas chromatography-mass spectrometry (GC-MS). The essential oils comprised of sesquiterpenes including β-gurjunene (7.45%), γ-amorphene (6.61%), guaia-6,9-diene (6.40%), δ-guaiene (5.21%) and a phenylpropanoid, safrole (0.49%) were mainly identified in addition to long-chain hydrocarbons including n-heptadecane (24.60%), 7-hexadecene (4.44%) and a diterpenoid, ent-kaur-16-ene (6.57%).

Antioxidative Effects and Anti-proliferative Effects of MeOH, BuOH and Ethyl Acetate Fractionated from Stephania delavayi Diels (일문전(Stephania delavayi Diels.) 메탄올, 부탄올, 에틸아세테이트 분획물의 항산화 및 세포증식억제 효과)

  • Li, Yong-Chun;Kim, Kyoung-Hee;Xu, Hong-De;Park, Dae-Hun;Choi, Yeon-Shik;Hwang, Hye-Rim;Lee, Min-Jae;Choi, Jong-Jin;Kwon, Myung-Sang;Yook, Hong-Sun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.3
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    • pp.297-301
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    • 2009
  • Stephania delavayi Diels. (S. delavayi Diels.) has been used as a drug for pain-relieving and acute gastroenteritis treatment in China. Because the major therapeutic mechanism of anti-inflammatory drug is to inhibit the cyclooxygenase (COX)-2 and because COX-2 proteins inhibit apoptosis, COX-2 inhibitor has been thought as the anticancer drug candidate. For this reason, we examined S. delavayi Diels. as an anticancer drug. S. delavayi Diels. was fractionated with methanol and then partitioned with ethyl acetate, n-butanol and water. The antioxidant activity was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity and reducing power. DPPH radical scavenging activities of the crude fractions at the concentration of $1,000{\mu}g/mL$ were 75.23% (n-butanol), 68.11% (methanol), 63.58% (ethyl acetate), and 50.13% (water). The reducing power increased according to the concentration in dose-dependent manner. Also, when the antiproliferation effects of each fraction against human breast cancer cell-lines MDA-MB-231 and MCF-7 were examined, methanol extract, n-butanol fraction and ethyl acetate fraction exhibited cell proliferative inhibition effects in both cell-lines whereas water fraction did not. Among the crude fractions, the n-butanol fraction exhibited the most potent anti-proliferation effect. In conclusion, fractions from S. delavayi Diels. are promising anticancer drug candidates.

Bio-Derived Poly(${\gamma}$-Glutamic Acid) Nanogels as Controlled Anticancer Drug Delivery Carriers

  • Bae, Hee Ho;Cho, Mi Young;Hong, Ji Hyeon;Poo, Haryoung;Sung, Moon-Hee;Lim, Yong Taik
    • Journal of Microbiology and Biotechnology
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    • v.22 no.12
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    • pp.1782-1789
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    • 2012
  • We have developed a novel type of polymer nanogel loaded with anticancer drug based on bio-derived poly(${\gamma}$-glutamic acid) (${\gamma}$-PGA). ${\gamma}$-PGA is a highly anionic polymer that is synthesized naturally by microbial species, most prominently in various bacilli, and has been shown to have excellent biocompatibility. Thiolated ${\gamma}$-PGA was synthesized by covalent coupling between the carboxyl groups of ${\gamma}$-PGA and the primary amine group of cysteamine. Doxorubicin (Dox)-loaded ${\gamma}$-PGA nanogels were fabricated using the following steps: (1) an ionic nanocomplex was formed between thiolated ${\gamma}$-PGA as the negative charge component, and Dox as the positive charge component; (2) addition of poly(ethylene glycol) (PEG) induced hydrogen-bond interactions between thiol groups of thiolated ${\gamma}$-PGA and hydroxyl groups of PEG, resulting in the nanocomplex; and (3) disulfide crosslinked ${\gamma}$-PGA nanogels were fabricated by ultrasonication. The average size and surface charge of Dox-loaded disulfide cross-linked ${\gamma}$-PGA nanogels in aqueous solution were $136.3{\pm}37.6$ nm and $-32.5{\pm}5.3$ mV, respectively. The loading amount of Dox was approximately 38.7 ${\mu}g$ per mg of ${\gamma}$-PGA nanogel. The Dox-loaded disulfide cross-linked ${\gamma}$-PGA nanogels showed controlled drug release behavior in the presence of reducing agents, glutathione (GSH) (1-10 mM). Through fluorescence microscopy and FACS, the cellular uptake of ${\gamma}$-PGA nanogels into breast cancer cells (MCF-7) was analyzed. The cytotoxic effect was evaluated using the MTT assay and was determined to be dependent on both the concentration and treatment time of ${\gamma}$-PGA nanogels. The bio-derived ${\gamma}$-PGA nanogels are expected to be a well-designed delivery carrier for controlled drug delivery applications.

Enhancement of Cytotoxicity by the Combination of Anticancer Drugs in Human Lung Adenocarcinoma Cell Line (PC-14) (폐암세포주 (PC-14)에서 복합항암제 처치시 암세포살해능의 증강에 관한 연구)

  • Lee, Choon-Taek
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.3
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    • pp.525-533
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    • 1997
  • Background : No ideal combination chemotherapy for lung cancer has been established even though lots of combination anticancer chemotherapies have been tried. For the combination of anticancer drugs, the interaction of anticancer drugs is very important but unpredictable factor. In this experiment, we designed and tested new experiment to measure the interaction of two anticancer drugs using MIT assay in an attempt to predict clinical response of the combination regimen. Methods : With human lung adenocarcinoma cell line (PC-14), the cytotoxic effect of cisplatin, adriamycin, mitomycin C and etoposide were measured by in vitro chemosensitivity test (MIT assay). The combined cytotoxic effects of combination of two drugs were also measured in every combination of the drug concentrations and analyzed the interaction by Anava analysis of two way factorial design. Results : Four individual drugs showed cytotoxic effects on PC-14 by dose dependent fashion. Comparison of two drug combinations revealed that mitomycin C + cisplatin and adriamycin + cisplatin combinations showed stronger synergistic cytotoxic effects. Conclusion : From this experiment, we suggest two combinations of mitomycin C + cisplatin and adriamycin + cisplatin as chemotherapeutic regimens for unresectable non-small cell lung cancer. Furthermore, this experimental design could be applied to other types of cancer requiring combination anticancer chemotherapy.

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Cytocidal Effect of TALP-32 on Human Cervical Cancer Cell HeLa (TALP-32의 인체자궁암 세포주 HeLa에 대한 세포독성)

  • Park, Ji-Hoon;Kim, Jong-Seok;Yun, Eun-Jin;Song, Kyoung-Sub;Seo, Kang-Sik;Kim, Hoon;Jung, Yeon-Joo;Yun, Wan-Hee;Lim, Kyu;Hwang, Byoung-Doo;Park, Jong-Il
    • Toxicological Research
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    • v.22 no.4
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    • pp.315-322
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    • 2006
  • TALP-32 is highly basic protein with a molecular weight of 32 kDa purified from human term placenta. Some basic proteins such as defensins and cecropins are known to induce cell death by increasing membrane permeability and some of them are under development as an anticancer drug especially targeting multi-drug resistant cancers. Therefore, we investigated cytotoxic effect and mechanism of TALP-32 When HeLa cell was incubated with TALP-32, cytotoxicity was increased in time and dose dependent manner. As time goes by, HeLa cells became round and plasma membrane was ruptured. Increase of plasma membrane permeability was determined with LDH release assay. Also in transmission electron microscopy, typical morphology of necrotic cell death, such as cell swelling and intracellular organelle disruption was observed, but DNA fragmentation and caspase activation was not. And necrotic cell death was determined with Annexin V/Pl staining. The cytotoxicity of TALP-32 was minimal and decreased or RBC and Hep3B respectively. These data suggests that TALP-32 induces necrosis on rapidly growing cells but not on slowly growing cells implicating the possibility of its development of anticancer peptide drug.

Anticancer activity of gomisin J from Schisandra chinensis fruit

  • Samil Jung;Hyung-In Moon;Subeen Kim;Nguyen Thi Ngoc Quynh;Jimin Yu;Zolzaya Sandag;Dan-Diem Thi Le;Hyegyeong Lee;Hyojeong Lee;Myeong-Sok Lee
    • Oncology Letters
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    • v.41 no.1
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    • pp.711-717
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    • 2019
  • In attempting to identify effective anticancer drugs from natural products that are harmless to humans, we found that the gomisin J from Schisandra chinensis fruit has anticancer activity. Schisandra chinensis fruits are used in traditional herbal medicine and gomisin J is one of their chemical constituents. In the present study, we examined the anticancer activity of gomisin J in MCF7 and MDA-MB-231 breast cancer cell lines and in MCF10A normal cell line, in a time- and concentration-dependent manner. Our data revealed that gomisin J exerted a much stronger cytotoxic effect on MCF7 and MDA-MB-231 cancer cells than on MCF10A normal cells. Gomisin J suppressed the proliferation and decreased the viability of MCF7 and MDA-MB-231 cells at relatively low (<10 ㎍/ml) and high (>30 ㎍/ml) concentrations, respectively. Our data also revealed that gomisin J induced necroptosis, a programmed form of necrosis, as well as apoptosis. Notably, gomisin J predominantly induced necroptosis in MCF7 cells that are known to have high resistance to many pro-apoptotic anticancer drugs, while MDA-MB-231 exhibited a much lower level of necroptosis but instead a higher level of apoptosis. This data indicated the possibility that it may be used as a more effective anticancer drug, especially in apoptosis-resistant malignant cancer cells. In an extended study, gomisin J exhibited a strong cytotoxic effect on all tested various types of 13 cancer cell lines, indicating its potential to be used against a wide range of different types of cancer cells.

MHY2251, a New SIRT1 Inhibitor, Induces Apoptosis via JNK/p53 Pathway in HCT116 Human Colorectal Cancer Cells

  • Yong Jung Kang;Young Hoon Kwon;Jung Yoon Jang;Jun Ho Lee;Sanggwon Lee;Yujin Park;Hyung Ryong Moon;Hae Young Chung;Nam Deuk Kim
    • Biomolecules & Therapeutics
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    • v.31 no.1
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    • pp.73-81
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    • 2023
  • Sirtuins (SIRTs) belong to the nicotinamide adenine dinucleotide (NAD+)-dependent class III histone deacetylase family. They are key regulators of cellular and physiological processes, such as cell survival, senescence, differentiation, DNA damage and stress response, cellular metabolism, and aging. SIRTs also influence carcinogenesis, making them potential targets for anticancer therapeutic strategies. In this study, we investigated the anticancer properties and underlying molecular mechanisms of a novel SIRT1 inhibitor, MHY2251, in human colorectal cancer (CRC) cells. MHY2251 reduced the viability of various human CRC cell lines, especially those with wild-type TP53. MHY2251 inhibited SIRT1 activity and SIRT1/2 protein expression, while promoting p53 acetylation, which is a target of SIRT1 in HCT116 cells. MHY2251 treatment triggered apoptosis in HCT116 cells. It increased the percentage of late apoptotic cells and the sub-G1 fraction (as detected by flow cytometric analysis) and induced DNA fragmentation. In addition, MHY2251 upregulated the expression of FasL and Fas, altered the ratio of Bax/Bcl-2, downregulated the levels of pro-caspase-8, -9, and -3 proteins, and induced subsequent poly(ADP-ribose) polymerase cleavage. The induction of apoptosis by MHY2251 was related to the activation of the caspase cascade, which was significantly attenuated by pre-treatment with Z-VAD-FMK, a pan-caspase inhibitor. Furthermore, MHY2251 stimulated the phosphorylation of c-Jun N-terminal kinase (JNK), and MHY2251-triggered apoptosis was blocked by pre-treatment with SP600125, a JNK inhibitor. This finding indicated the specific involvement of JNK in MHY2251-induced apoptosis. MHY2251 shows considerable potential as a therapeutic agent for targeting human CRC via the inhibition of SIRT1 and activation of JNK/p53 pathway.