• Title/Summary/Keyword: Antitumor activities

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Purification and Biological Activities of MT 1155 Inducing Morphological Change of Rous Sarcoma Virus-Transformed Normal Rat Kidney Cell (Rous Sarcoma Virus에 의해 형질전환된 NRK 세포의 형태변화를 유도하는 활성물질 MT 1154의 분리와 생물학적 활성)

  • 안종석;박문수;박찬선;윤병대;민태익;안순철;오원근;이현선;윤병대
    • Microbiology and Biotechnology Letters
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    • v.21 no.1
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    • pp.59-65
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    • 1993
  • We isolated Actinomycetes strain GMT 1155 and purified the active compound, MT 1155, on the morphological reversion of ts/NRK cell from the isolate. MT 1155 was identified as toyocamycin having antifungal and antitumor activities from physico-chemical properties and UV, IR, $^1H$-NMR, $^13C$-NMR and mass spectrum. MT 1155 showed the morphologically reversional activity on ts/NRK cell and the cytotoxicity on CTLL cell at the final concentrations of 1.7 JlM and 0.2 11M, respectively and its $IC_{50}$ value on protein kinase A enzyme was 2.3 $\mu$M. Also it had strong antifungal activity against several pathogenic fungi but not antibacterial activity. And it did not inhibit both protein kinase C activity and the bleb-formation of K562 cell induced by phorbol esters.

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Cytotoxic Activity of Four Xanthones from Emericella variecolor, an Endophytic Fungus Isolated from Croton oblongifolius

  • Pornpakakul Surachai;Liangsakul Jatupol;Ngamrojanavanich Nattaya;Roengsumran Sophon;Sihanonth Prakitsin;Piapukiew Jittra;Sangvichien Ek;Puthong Songchan;Petsom Amorn
    • Archives of Pharmacal Research
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    • v.29 no.2
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    • pp.140-144
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    • 2006
  • Four xanthones were isolated from mycelia of Emericella variecolor, an endophytic fungus isolated from the leaves of Croton oblongifolius. Their structures were elucidated by spectroscopic analysis to be shamixanthone, 14-methoxytajixanthone-25-acetate, tajixanthone methanoate, and tajixanthone hydrate. All compounds were tested for cytotoxic activity against various human tumor cell lines including gastric carcinoma, colon carcinoma, breast carcinoma, human hepatocarcinoma, and lung carcinoma. The antitumor activities of these xanthones were compared with that of doxorubicin hydrochloride, a chemotherapeutic substance. All of them showed moderate activities and were selective against gastric carcinoma, colon carcinoma, and breast carcinoma. Only tajixanthone hydrate exhibited moderate activity against all cancer cell lines. Furthermore, under the test conditions it was found that 14-methoxytajixanthone-25-acetate and tajixanthone hydrate are almost as active as doxorubicin hydrochloride against gastric carcinoma (KATO3) and breast carcinoma (BT474).

Four Butenolides are Novel Cytotoxic Compounds Isolated from the Marine-Derived Bacterium, Streptoverticillium luteoverticillatum 11014

  • Li, De-Hai;Zhu, Tian-Jiao;Liu, Hong-Bing;Fang, Yu-Chun;Gu, Qian-Qun;Zhu, Wei-Ming
    • Archives of Pharmacal Research
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    • v.29 no.8
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    • pp.624-626
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    • 2006
  • Four known butenolides were isolated from the ethyl acetate extracts of the culture broth of the marine-derived bacterium, Streptoverticillium luteoverticillatum, by bioassay-guided fractionation. The structures were identified on the basis of spectral data. The absolute configuration of compound (1) was determined by CD spectrum for the first time. Compounds 1-4 showed in vitro cytotoxicity against the murine lymphoma P388 and human leukemia K562 cell lines. This is the first report on the isolation of butenolides from the marine bacterium, Streptoverticillium luteoverticillatum, and their cytotoxic activities.

Screening for Antitumor Efficacy from the Wild Plants in Korea (한국산 천연항종양성 자원의 Screening에 대하여)

  • 이상래
    • Korean Journal of Plant Resources
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    • v.5 no.2
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    • pp.85-93
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    • 1992
  • This experiment was Conducted ta screening for the anti-cancer efficacy from the wild plants which are naturally growing in the Korea. The results are as follows. The results were shown thatZea may L. nad significantly effects on mediculal efficacy anganist anti-tumor by usulg the totalpacked cell volume methods and also, severals plants, such as Sofonum nigrum, Patrinia hispidoBunge, Eragrostis, ferrugenia Beauv, Salaginela pouzolgiana Spring, Platrycarya strobilacea Bunge,Codonopsis lanceolata Benth. et Hook fil. which are collected from Giri and Mooju mountain in Koreaand Nagano in Japan were showed effects on auti-tumor. But the pharmaceologial activities ofPharbitis nil Choisy was believed to strong effec on anti - cancer tumors, while toxicity of its wasshown high that induced te kill all used mice. Extraction of Patrinia hispida Bunge, Pharbitis nilChoisy, Toilis japonica DC, Eragrostis erruginea Beauv. and Forsythia koreana Nakai showed effec-tively supressed on growth rate of cancer tumor by the below 50 percent of T/C ratio at 30mg /mlof extraction from plant. That Is strong activity while Reynouxria japonica Houtt. was observed onlymild activities. The above results many possibly suggest that Patrinia hispido Bunge and Eragrostisferrugina Beauv. inhibited the growth of cancer tumor by the both total packed cell volume methodand cytotoxicity method. Although basic research is still going on, we will find out an accurate moth-od for developing useful medicinal plant to improve pharmacological activites against anti-cancertumor, especialy, in Eragrostis ferruginea Beauv.

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Baicalein and Baicalin from the Radix of Scutellaria baicalensis Georgi Inhibits Oxidative DNA Damage and Apoptosis via its Antioxidant Activity

  • Garcia, Nellie Ann S.;Jeong, Hyung-Jin
    • Korean Journal of Plant Resources
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    • v.22 no.6
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    • pp.489-497
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    • 2009
  • In this study, we evaluated and compared the protective effects of two major constituents, baicalein and baicalin, against oxidative DNA and cell damages caused by hydroxyl radical. Antioxidant properties were evaluated using DPPH and hydroxyl radicals scavenging assays and $Fe^{2+}$ chelating assay. ${\varphi}X$ 174 RFI plasmid DNA and intracellular DNA migration assay were used to evaluate the protective effect against oxidative DNA damage. Also, MTT and lipid peroxidation assays were used to evaluate their protective effects against oxidative cell damage. Both baicalein and baicalin prevented intracellular DNA and cells from oxidative damage caused by hydroxyl radical via antioxidant activities. Baicalein demonstrated a stronger antioxidant activity in scavenging DPPH radicals and chelating $Fe^{2+}$ while baicalin scavenged hydroxyl radicals more efficiently. The differences in the level of baicalein and baicalin pose a different pathological pathway for each. The antioxidant activity of baicalin was due to its ability to scavenge hydroxyl radical whilst baicalein was a stronger $Fe^{2+}$ chelator. Further investigation to compare the molecular mechanisms of antitumor activities of baicalein and baicalin is vital to anticancer research.

Antioxidant Activity of Ethyl acetate Fraction of Oat in Caenorhabditis elegans (귀리 Ethyl acetate 분획물의 예쁜 꼬마선충 내의 항산화 효과)

  • Kwon, Kang Mu;Kim, Jun Hyeong;Yang, Jae Heon;Ki, Byeolhui;Hwang, In Hyun;Kim, Dae Keun
    • Korean Journal of Pharmacognosy
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    • v.52 no.4
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    • pp.251-256
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    • 2021
  • Oat, the seeds of Avena sativa L. (Gramineae), is an important dietary staple for people in many countries. Previous studies reported that A. sativa had various pharmacological effects such as anti-inflammatory, antitumor, neurotonic, and antispasmodic activities. In this study, Caenorhabditis elegans model system was used to investigate the antioxidant activity of methanol extract of oat. The ethyl acetate soluble fraction of the oat methanol extract showed the best DPPH radical scavenging activity. The ethyl acetate fraction was measured for the activity of superoxide dismutase (SOD), catalase, and oxidative stress tolerance by using C. elegans along with reactive oxygen species (ROS) level. In addition, to confirm that the regulation of the stress response gene is responsible for the increased stress tolerance of C. elegans treated by the ethyl acetate fraction, SOD-3 expression was measured using GFP-expressing transgenic worm. As a result, the ethyl acetate fraction increased SOD and catalase activities, and decreased ROS accumulation in a dose-dependent manner. In addition, the ethyl acetate fraction-treated CF1553 worm showed higher SOD-3::GFP intensity compared to the control.

A Pharmacological Review on Portulaca oleracea L.: Focusing on Anti-Inflammatory, Anti- Oxidant, Immuno-Modulatory and Antitumor Activities

  • Rahimi, Vafa Baradaran;Ajam, Farideh;Rakhshandeh, Hasan;Askari, Vahid Reza
    • Journal of Pharmacopuncture
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    • v.22 no.1
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    • pp.7-15
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    • 2019
  • Portulaca oleracea L. (PO) or Purslane is an annual grassy plant that is distributed in many parts of the world, especially the tropical and subtropical areas. PO has some pharmacological properties such as analgesic, antibacterial, skeletal muscle-relaxant, wound-healing, anti- inflammatory and a radical scavenger. This review article is focused on the anti-inflammatory, immuno-modulatory, anti-oxidant and anti-tumor activities of the PO. Anti-inflammatory, immuno-modulatory, anti-oxidant and Anti-tumor effects of PO were searched using various databases until the end of August 2018. The online literature was searched using PubMed, Science Direct, Scopus, Google Scholar and Web of Science. Our review showed that PO exerts its effects through anti-inflammatory properties and balancing the adaptive and innate immune system depending on situations. PO acts as immune-modulator and anti-oxidant agent in both inflammatory states by the dominance of Th2 response such as asthma, cancer and atopic dermatitis and evoked Th1 disorders including hepatitis and multiple sclerosis.

Identification of Proteins Binding to Decursinol by Chemical Proteomics

  • Kang, Hyo-Jin;Yoon, Tae-Sung;Jeong, Dae-Gwin;Kim, Yong-Mo;Chung, Jin-Woong;Ha, Jong-Seong;Park, Sung-Sup;Ryu, Seong-Eon;Kim, Sang-Hee;Bae, Kwang-Hee;Chung, Sang-J.
    • Journal of Microbiology and Biotechnology
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    • v.18 no.8
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    • pp.1427-1430
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    • 2008
  • Decursinol, found in the roots of Angelica gigas Nakai, has been traditionally used to treat anemia and other various diseases. Recently, numerous biological activities such as cytotoxic effect on leukemia cells, and antitumor, neuroprotection, and antibacterial activities have been reported for this compound. Although a number of proteins including protein kinase C, androgen receptor, and acetylcholinesterase were proposed as molecular targets responsible for the activities of decursinol, they are not enough to explain such a diverse biological activity mentioned above. In this study, we employed a chemical proteomic approach, leading to identification of seven proteins as potential proteins interacting with decursinol. Most of the proteins contain a defined ATP or nucleic acid binding domain and have been implied to be involved in the pathogenesis and progression of various human diseases including cancer, autoimmune disorders, or neurodegenerative diseases. The present results may provide clues to understand the molecular mechanism of the biological activities shown by decursinol, an anticancer natural product.

Differential Effects of Tautomycetin and Its Derivatives on Protein Phosphatase Inhibition, Immunosuppressive Function and Antitumor Activity

  • Niu, Mingshan;Sun, Yan;Liu, Bo;Tang, Li;Qiu, Rongguo
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.2
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    • pp.145-151
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    • 2012
  • In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

Anti-proliferative and Antioxidant Activities of 1-methoxy-3-methyl-8-hydroxy-anthraquinone, a Hydroxyanthraquinoid Extrolite Produced by Amycolatopsis thermoflava strain SFMA-103

  • Kumar, C. Ganesh;Mongolla, Poornima;Chandrasekhar, Cheemalamarri;Poornachandra, Yedla;Siva, Bandi;Babu, K. Suresh;Ramakrishna, Kallaganti Venkata Siva
    • Microbiology and Biotechnology Letters
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    • v.45 no.3
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    • pp.200-208
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    • 2017
  • Actinobacteria are prolific producers of a large number of natural products with diverse biological activities. In the present study, an actinobacterium isolated from sunflower rhizosphere soil sample collected from Medak, Andhra Pradesh, South India was identified as Amycolatopsis thermoflava strain SFMA-103. A pigmented secondary metabolite in culture broth was extracted by using methanol and it was further purified by silica gel column chromatography with methanol-chloroform solvent system. Structural elucidation studies based on UV-visible, 1D and 2D-NMR, FT-IR, and mass spectroscopic analyses confirmed the structure as 1-methoxy-3-methyl-8-hydroxy-anthraquinone. It showed significant in vitro anticancer activity against lung cancer and lymphoblastic leukemia cells with $IC_{50}$ values of 10.3 and $16.98{\mu}M$, respectively. In addition, 1-methoxy-3-methyl-8-hydroxy-anthraquinone showed good free radical scavenging activity by DPPH method with an $EC_{50}$ of $18.2{\mu}g/ml$. It also showed other promising superoxide radical scavenging, nitric oxide radical scavenging and inhibition of lipid peroxidation activities. This is a first report of anti-proliferative and antioxidant activities of 1-methoxy-3-methyl-8-hydroxy-anthraquinone isolated from A. thermoflava strain SFMA-103 which may find potential application in biotechnological and pharmaceutical fields.