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Therapeutic effects of dihydroartemisinin and transferrin against glioblastoma

  • Kim, Suk Hee;Kang, Seong Hee;Kang, Bo Sun
    • Nutrition Research and Practice
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    • v.10 no.4
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    • pp.393-397
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    • 2016
  • BACKGROUND/OBJECFTIVES: Artemisinin, a natural product isolated from Gaeddongssuk (artemisia annua L.) and its main active derivative, dihydroartemisinin (DHA), have long been used as antimalarial drugs. Recent studies reported that artemisinin is efficacious for curing diseases, including cancers, and for improving the immune system. Many researchers have shown the therapeutic effects of artemisinin on tumors such as breast cancer, liver cancer and kidney cancer, but there is still insufficient data regarding glioblastoma (GBM). Glioblastoma accounts for 12-15% of brain cancer, and the median survival is less than a year, despite medical treatments such as surgery, radiation therapy, and chemotherapy. In this study, we investigated the anti-cancer effects of DHA and transferrin against glioblastoma (glioblastoma multiforme, GBM). MATERIALS/METHODS: This study was performed through in vitro experiments using C6 cells. The toxicity dependence of DHA and transferrin (TF) on time and concentration was analyzed by MTT assay and cell cycle assay. Observations of cellular morphology were recorded with an optical microscope and color digital camera. The anti-cancer mechanism of DHA and TF against GBM were studied by flow cytometry with Annexin V and caspase 3/7. RESULTS: MTT assay revealed that TF enhanced the cytotoxicity of DHA against C6 cells. An Annexin V immune-precipitation assay showed that the percentages of apoptosis of cells treated with TF, DHA alone, DHA in combination with TF, and the control group were $7.15{\pm}4.15%$, $34.3{\pm}5.15%$, $66.42{\pm}5.98%$, and $1.2{\pm}0.15%$, respectively. The results of the Annexin V assay were consistent with those of the MTT assay. DHA induced apoptosis in C6 cells through DNA damage, and TF enhanced the effects of DHA. CONCLUSION: The results of this study demonstrated that DHA, the derivative of the active ingredient in Gaeddongssuk, is effective against GBM, apparently via inhibition of cancer cell proliferation by a pharmacological effect. The role of transferrin as an allosteric activator in the GBM therapeutic efficacy of DHA was also confirmed.

Cytotoxicity of Methanol Extracts from Cudrania tricuspidata Bureau (꾸지뽕나무 메탄올 추출물의 세포독성)

  • Choi, So-Ra;You, Dong-Hyun;Jang, Ik;Ahn, Min-Sil;Song, Eun-Ju;Seo, Sang-Young;Choi, Min-Kyung;Kim, Young-Sun;Kim, Myung-Kon;Choi, Dong-Geun
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.3
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    • pp.153-158
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    • 2012
  • In order to develop as a natural source of anticancer materials of Cudrania tricuspidata, the cytotoxicity of methanol extracts by harvesting parts and times against 8 cell lines including 293 (normal kidney cells) and A-431 (epidermoid carcinoma cells) were investigated using MTT assay. All harvesting parts had hardly cytotoxicity against 293. And methanol extracts of stem bark and root bark showed very high cytotoxicities against 7 cancer cell lines. The cytotoxicity was the highest against HeLa (cervix adenocarcinoma cells) and followed by MCF-7 (breast adenocarcinoma cells), AGS (stomach adenocarcinoma cells), HT-29 (colon adenocarcinoma cells), HepG2 (hepatoblastoma cells), A549 (lung carcinoma cells) and A-431. By the way, leaf extract had a cytotoxicity against only AGS and ripe fruit extract had no cytotoxicity. Among harvesting times, the cytotoxicity of root bark were high from April to September but that of stem bark showed a little difference. These results showed that anticancer activities of Cudrania tricuspidata extracts were eventful changes by harvesting parts and times.

Screening of Antiviral Activity from Natural Plants against Feline Calicivirus (Feline calicivirus에서 항바이러스 활성을 가지는 천연식물자원 탐색)

  • Kim, Kyoung-Lan;Kim, Young-Mog;Lee, Eun-Woo;Lee, Dae-Sung;Lee, Myung-Suk
    • Journal of Life Science
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    • v.19 no.7
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    • pp.928-933
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    • 2009
  • In an effort to discover an antiviral substance against noroviruse (NV), which causes gastroenteritis illness world-wide, several plants including spices and herbs were evaluated for their antiviral activities against feline calicivirus (FCV) as a surrogate for NV. Among them, methanolic extract of green tea (Camellia sinensis L.) exhibited significant antiviral activity against FCV. After treatment with green tea extract (3.13 mg/ml) for 1 hr, FCV was completely inactivated. The antiviral activity of green tea extract against FCV was also determined to be dose and time- dependent. The results obtained in this study suggested that green tea will be effective in the prevention of food-borne diseases caused by NV.

Multi-Function of a New Bioactive Secondary Metabolite Derived from Endophytic Fungus Colletotrichum acutatum of Angelica sinensis

  • Ramy S. Yehia
    • Journal of Microbiology and Biotechnology
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    • v.33 no.6
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    • pp.806-822
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    • 2023
  • In the current study we assessed a new crystallized compound, 5-(1-hydroxybutyl)-4-methoxy-3-methyl-2H-pyran-2-one (C-HMMP), from the endophytic fungus Colletotrichum acutatum residing in the medicinal plant Angelica sinensis for its in vitro antimicrobial, antibiofilm, antioxidant, antimalarial, and anti-proliferative properties. The promising compound was identified as C-HMMP through antimicrobial-guided fraction. The structure of C-HMMP was unambiguously confirmed by 2D NMR and HIRS spectroscopic analysis. Antimicrobial property testing of C-HMMP showed it to be effective against a variety of pathogenic bacteria and fungi with MICs ranging from 3.9 to 31.25 ㎍/ml. The compound displayed excellent antibiofilm activity against C. albicans, S. aureus, and K. pneumonia. Furthermore, the antimalarial and radical scavenging activities of C-HMMP were clearly dosedependent, with IC50 values of 0.15 and 131.2 ㎍/ml. The anti-proliferative activity of C-HMMP against the HepG-2, HeLa, and MCF-7 cell lines in vitro was investigated by MTT assay, revealing notable anti-proliferative activity with IC50 values of 114.1, 90, and 133.6 ㎍/ml, respectively. Moreover, CHMMP successfully targets topoisomerase I and demonstrated beneficial anti-mutagenicity in the Ames test against the reactive carcinogenic mutagen, 2-aminofluorene (2-AF). Finally, the compound inhibited the activity of α-glucosidase and α-amylase with IC50 values of 144.7 and 118.6 ㎍/ml, respectively. To the best of our knowledge, the identified compound C-HMMP was obtained for the first time from C. acutatum of A. sinensis, and this study demonstrated that C-HMMP has relevant biological significance and could provide better therapeutic targets against disease.

New Aminothiazolyl Cephalosporins. Synthesis and Biological Evaluation of 7-[Alkoxyiminomethyl(2-aminothiazol-4-yl)acetamido]ceph-3-em-4-carboxylic Acids

  • Koh, Hun-Yeong;Kang, Han-Young;Choi, Kyung-Il;Chang, Moon-Ho
    • Bulletin of the Korean Chemical Society
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    • v.11 no.6
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    • pp.538-542
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    • 1990
  • New aminothiazolyl cephalosporins with alkoxyiminomethyl(2-aminothiazol-4-yl)acetyl substituents at 7-position of cephems were synthesized starting from (2-aminothiazol-4-yl)acetate via one carbon homologation followed by acylation with 7-aminoceph-3-em-4-carboxylic acid derivatives. These new aminothiazolyl cephalosporins exhibit promising in vitro activities against various strains including Gram positive bacteria.

Hepatoprotective Effects of Saururus chinensis Baill against 2,3,7,8-tetrachlorodibenzo- p-dioxin (TCDD) Induced Toxicity

  • Lee, Sang-Hun;Kim, Hee-Jin;Lee, Jin-Young;Ha, Bae-Jin
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.211.2-211.2
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    • 2003
  • Saururus Chinensis Baill (Saururaceae) has been used as folk medicine for analgesics, beriberi, edema, hepatitis, and icterus, etc. Hepatoprotective effects of Saururus chinensis Baill (SCB) administration on function of the biochemical parameters in liver of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) treated rats were investigated. After 7 days from TCDD(1$\mu\textrm{g}$/kg) injection, SCB(200mg/kg) was administered into rats intraperitoneally for 4 week.s We examined the antioxidative enzymatic activity by measuring the level of AST and ALT in serum and SOD, Catalase, GPx, GSH and GSSG in liver tissue of rats. (omitted)

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Antimicrobial Activity of Nano Materials against Acidovorax citrulli and Other Plant Pathogens (나노 화합물을 이용한 Acidovorax citrulli 및 식물병원성 미생물의 항균활성 효과 검정)

  • Kim, Sang Woo;Adhikari, Mahesh;Yadav, Dil Raj;Lee, Hyun Goo;Um, Young Hyun;Kim, Hyun Seung;Lee, Youn Su
    • Research in Plant Disease
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    • v.21 no.1
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    • pp.12-19
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    • 2015
  • Antimicrobial activities of nano-materials were tested against several plant pathogens. Twelve different nano-materials were used to observe the antagonistic activity against three kinds of mold and sixteen different kinds of watermelon fruit rot pathogens (Acidovorax citrulli). According to the results, no antagonism have been found against the pathogen, Cylindrocarpon destructans. However in the case of Pythium ultimum, combination of Brass/Glucose 1,000 ppm confirmed the mycelial growth reduction by 94%. In addition, little effect was found against Rhizoctonia solani by Ag/Glucose 3,000 ppm. The remaining other nano-materials have different antimicrobial effect depending on the strains of A. citrulli. But in the case of lime (Cu/Salt 1,000 ppm) highest antimicrobial activity was observed with 97%. Moreover growth of five different strains of A. citrulli was checked by 99% with the combination of Ag/Glucose 1,000 ppm. 92% reduction of A. citrulli growth was observed with $Brass/CaCO_3$ 3,000 ppm. Tested nano-materials against different plant pathogens in this study showed the antimicrobial activity at the range of 24-70%.

Evaluation of Insecticidal Activity of Plant Extracts against the Diamondback Moth, Plutella xylostella (Lepidoptera: Plutellidae) on Vegetable Plant (배추좀나방(Plutella xylostella)에 대한 식물추출물의 살충력 평가)

  • Choi, I-Jin;Kwon, Hyuk-Hyun;Lee, Han-Ho;Son, Hyoung-Gi;Hong, Sang-Kil;Kang, Jong-Woon;Park, Yu-Soon
    • Korean Journal of Plant Resources
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    • v.26 no.1
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    • pp.19-25
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    • 2013
  • This study focused on the usefulness of plant extracts for a city organic farm. Insecticidal activity of 8 plant species, plants crude extracts by ethanol and water, against third instar larvae (susceptible strain) of Plutella xylostella was evaluated in this study. Ethanol(25%) extracts of plant materials had better insecticidal activity than water extracts at the room temperature. Insecticidal activity were investigated by leaf disc spray method. Five plant extracts (Capsicum annuum, Chelidoniun majus, Leonurus sibiricus, Coptis japonica, Mentha piperascens) showed over 50% insecticidal activity to P. xylostella at the concentration of $1500mg{\cdot}L^{-1}$. Extract of C. annuum showed the highest insecticidal activity (83.3%) against P. xylostella. Phytotoxicity was not observed on Raphanus sativus and Brassica campestris with spray application. Seed germination and growth of two plants were not affected. Extract of C. japonica revealed 73.3% control efficacy against P. xylostella of R. sativus and showed 70% control efficacy against those of B. campestris, respectively, in plastic house. Insecticidal activity against various insects was observed in C. japonica extract as 87.4% for R. sativus and 74.3% for B. campestris in the field. These results suggested that extracts of C. annuum, C. japonica showed the highest insecticidal activity, and could be used as city farm insecticides for organic farming.

Bioactive Metabolites Produced by Pseudonocardia endophytica VUK-10 from Mangrove Sediments: Isolation, Chemical Structure Determination and Bioactivity

  • Mangamuri, Usha Kiranmayi;Vijayalakshmi, Muvva;Poda, Sudhakar;Manavathi, Bramanandam;Bhujangarao, Ch.;Venkateswarlu, Y.
    • Journal of Microbiology and Biotechnology
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    • v.25 no.5
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    • pp.629-636
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    • 2015
  • Chemical investigation of the actinobacterial isolate Pseudonocardia endophytica VUK-10 has led to the segregation of two known bioactive compounds, namely 4-(2-acetamidoethyl) phenyl acetate and 4-((1, 4-dioxooctahydropyrrolo [1, 2-a] pyrazin-3-yl) methyl) phenyl acetate. The strain was isolated from a sediment sample of the Nizampatnam mangrove ecosystem, south coastal Andhra Pradesh, India. The chemical structure of the active compounds was established on the basis of spectroscopic analysis, including 1H NMR and 13C NMR spectroscopies, FTIR, and EIMS. The antimicrobial and cytotoxic activities of the bioactive compounds produced by the strain were tested against opportunistic and pathogenic bacteria and fungi and on MDA-MB-231, OAW, HeLa, and MCF-7 cell lines. The compounds exhibited antimicrobial activities against gram-positive and gram-negative bacteria and fungi and also showed potent cytotoxic activity against MDA-MB-231, OAW, HeLa, and MCF-7 cell lines. This is the first example for this class of bioactive compounds isolated from Pseudonocardia of mangrove origin.