• 제목/요약/키워드: Chemotherapeutics

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Comparative antiplasmodial activity, cytotoxicity, and phytochemical contents of Warburgia ugandensis stem bark against Aspilia africana wild and in vitro regenerated tissues

  • Denis Okello;Jeremiah Gathirwa;Alice Wanyoko;Richard Komakech;Yuseong Chung;Roggers Gang;Francis Omujal;Youngmin Kang
    • Journal of Plant Biotechnology
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    • 제50권
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    • pp.97-107
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    • 2023
  • Malaria remains to be one of the most severe global public health concerns. Traditionally, Aspilia Africana and Warburgia ugandensis have been used to treat malaria in several African countries for millennia. In the current study, A. africana calli (AaC), A. africana in vitro roots (AaIR), A. africana wild leaf (AaWL), and W. ugandensis stem bark (WuSB) were dried and pulverized. Fourier transform near-infrared spectroscopy was used to analyze the powdered samples, while 80% ethanolic extracts of each sample were assayed for antiplasmodial activity (against Plasmodium falciparum strains DD2 (chloroquine-resistant) and 3D7 (chloroquine-sensitive)) and cytotoxicity. WuSB showed the highest antiplasmodial activity (IC50 = 1.57 ± 0.210 ㎍/ml and 8.92 ± 0.365 ㎍/ml against P. falciparum 3D7 and DD2, respectively) and selectivity indices (43.90 ± 7.914 and 7.543 ± 0.051 for P. falciparum 3D7 and DD2, respectively). The highest total polyphenolic contents (total phenolic and flavonoid contents of 367.9 ± 3.55 mg GAE/g and 203.9 ± 1.43 mg RUE/g, respectively) were recorded for WuSB and the lowest were recorded for AaC. The antiplasmodial activities of the tested plant tissues correlated positively with total polyphenolic content. The high selectivity indices of WuSB justify its traditional applications in treating malaria and present it as a good candidate for discovering new antimalarial compounds. We recommend elicitation treatment for AaIR, which showed moderate antiplasmodial activity against P. falciparum DD2, to increase its secondary metabolite production for optimal antimalarial activity.

Characteristic Features of Cytotoxic Activity of Flavonoids on Human Cervical Cancer Cells

  • Sak, Katrin
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권19호
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    • pp.8007-8018
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    • 2014
  • Cervical cancer is the most common gynecologic malignancy worldwide and development of new therapeutic strategies and anticancer agents is an urgent priority. Plants have remained an important source in the search for novel cytotoxic compounds and several polyphenolic flavonoids possess antitumor properties. In this review article, data about potential anticarcinogenic activity of common natural flavonoids on various human cervical cancer cell lines are compiled and analyzed showing perspectives for the use of these secondary metabolites in the treatment of cervical carcinoma as well as in the development of novel chemotherapeutic drugs. Such anticancer effects of flavonoids seem to differentially depend on the cellular type and origin of cervical carcinoma creating possibilities for specific targeting in the future. Besides the cytotoxic activity per se, several flavonoids can also contribute to the increase in efficacy of conventional therapies rendering tumor cells more sensitive to standard chemotherapeutics and irradiation. Although the current knowledge is still rather scarce and further studies are certainly needed, it is clear that natural flavonoids may have a great potential to benefit cervical cancer patients.

Photocleavage of DNA by 4′-Bromoacetophenone- Pyrrole Carboxamides

  • Jeon, Raok
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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    • pp.79-79
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    • 2001
  • Genotoxic chemotherapeutics are irreversible DNA targeting agents, which can act as anticancer and antiviral drugs. Natural antibacterial and anticancer enediynes function through the formation of free radicals formed by Bergman-type cycloaromatization and being capable of cleavage of DNA strand. They have been focused primarily on the design and syntheses of simple enediyne structures, which can be mimic their mechanistic feature. Recently. I have been reported the possible application of 4'-bromoacetophenone as a simple photoactivatable DNA cleaving agent, which could be readily prepared and exhibit potent and selective DNA cleaving activity. Herein, we further investigated the activity of 4'-bromoacetophenone-pyrrolecarboxamides, which consist of both DNA cleaving element and recognition unit under various conditions in order to get more understanding of the mechanism of the action and find a broad spectrum of application.

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Anticancer Therapy for Breast Cancer Patients with Skin Metastases Refractory to Conventional Treatments

  • Varol, Umut;Yildiz, Ibrahim;Alacacioglu, Ahmet;Uslu, Ruchan
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권4호
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    • pp.1885-1887
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    • 2014
  • Skin metastases of breast cancer are usually late events in the course of tumor progression and signify a poor prognosis. They may remain as a therapeutic challenge especially after failure of standard treatments. Topical interventions, together with or without radiotherapy, may only palliate the symptoms temporarily. However, there may be alternative treatment modalities for unresectable breast cancer skin metastases resistant to chemotherapy and radiotherapy. There are various genetic alterations in tumors and therapeutic potential of expression patterns for factors like epidermal growth factor receptor may have important clinical implications in case of disease refractory to the conventional treatments. Here, we clarified the therapeutic options and genetic alterations in skin metastatic breast cancer patients refractory to standard chemotherapeutics.

The Effect of Abraxane on Cell Kinetic Parameters of HeLa Cells

  • Gurses, Nurcan;Topcul, Mehmet
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권7호
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    • pp.4229-4233
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    • 2013
  • Abraxane (nab-paclitaxel) is a member of the group of nano chemotherapeutics. It is approved for metastatic breast cancer and non small cell lung cancer. Trials for several cancer types including gynecological cancers, head and neck, and prostatic cancer are being studied. In this study, the antiproliferative and apoptotic effect of abraxane was evaluated on HeLa cell line originated from human cervix carcinoma. Three different doses ($D_1$=10 nM, $D_2$=50 nM, $D_3$=100 nM) were administered to HeLa cells for 24, 48 and 72 h. The 50 nM dose of abraxane decreased DNA synthesis from 4.62-0.08%, mitosis from 3.36-1.89% and increased apoptosis from 10.6-30% at 72 h. Additionally, tripolar metaphase plates were seen in mitosis preparations. In this study, abraxane effected cell kinetic parameters significantly. This results are consistent with other studies in the literature.

폐 Aspergillosis (Pulmonary aspergillosis 10 cases report)

  • 김범식
    • Journal of Chest Surgery
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    • 제19권3호
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    • pp.381-384
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    • 1986
  • Pulmonary aspergillosis is a relatively rare disease in Korea. Immune suppressive patients, resulting from misuse or long term therapy of antibiotics, steroid and anticancer chemotherapeutics tend to be vulnerable to pulmonary aspergillosis. This study is made to illustrate the clinical features, preoperative diagnosis and surgical role in the management is this diseases. In retrospective study of operative cases from May 1980 through July 1986, 10 cases were analysis. Hemoptysis and blood tinged sputum were the most common chief complaints. Major underlying pathology was cavitary lesion or bronchiectasis caused by pulmonary tuberculosis [5 cases]. 2 cases were disseminated form due to immune suppression. Anatomic location of lesion was in the upper lobe in half case. Systemic antifungal agent is helpful for invasive aspergillosis and Resection is the treatment of choice for localized fungus balls and symptomatic localized forms.

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The Cytotoxic Action of New Ag-Porphyrin as a Potential Chemotherapeutic Agent

  • Nelli, Babayan;Artak, Tovmasyan;Ani, Gevorkyan;Gennadi, Gasparyan;Rouben, Aroutiounian
    • 환경생물
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    • 제26권2호
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    • pp.115-120
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    • 2008
  • Earlier we have described new water-soluble Ag- and Zn-derivatives of tetrachloride meso-tetra (4-N-oxiethylpyridyl) porphyrin (TOEtPyP) as potential anticancer drugs. In this work the effect of one of these metal porphyrins, TOEtPyP Ag, on the cell population kinetics was studied in vitro using morphological and biochemical techniques. The results suggested that TOEtPyP Ag action consisted in the simultaneous suppression of the cell growth and activation of the cell death. About 40% of the cells were shown to die via apoptotic pathway. So, the porphyrin studied may be attributed to inducers of both necrotic and apoptotic processes. The results obtained support our previous assertion that TOEtPyP Ag may be considered as a potential chemotherapeutic agent.

Effect of Epigallocatechin Gallate on Viability of Kudoa septempunctata

  • Shin, Sang Phil;Hong, Hyun Ki;Jin, Chang Nam;Sohn, Hanchang;Choi, Kwang Sik;Lee, Jehee
    • Parasites, Hosts and Diseases
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    • 제58권5호
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    • pp.593-597
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    • 2020
  • Kudoa septempunctata have been reported as a causative agent for acute transient gastrointestinal troubles after eating raw olive flounder (Paralichthys olivaceus). It raised public health concerns and quarantine control in several countries. Quantitative evaluation on viability of K. septempunctata is crucial to develop effective chemotherapeutics against it. A cytometry using fluorescent stains was employed to assess effect of three compounds on viability of K. septempunctata. Epigallocatechin gallate reduced markedly viability of K. septempunctata at 0.5 mM or more, and damaged K. septempunctata spores by producing cracks.

Synthesis of New 3-Arylisoquinolinamines: Effect on Topoisomerase I Inhibition and Cytotoxicity

  • Cho, Won-Jae;Min, Sun-Young;Le, Thanh-Nguyen;Kim, Tae-Sung
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.180.1-180.1
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    • 2003
  • Eukaryotic DNA topoisomerase I (top I) is an essential enzyme that act to relax supercoiled DNA during the transcription, replication and mitosis. Intracellular levels of top I are elevated in a number of human solid tumors, relative to the respective normal tissues, suggesting that controlling the topI level is important to treat cancer. Top I poisons show their antitumor activities by stabilizing the cleavable ternary complex consisting of top I enzyme, DNA, and drug. Thus, top I is a promising target for the development of new cancer chemotherapeutics against a number of solid tumors. (omitted)

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DNA Damage Induced by New Pophyrins of Different Chemical Structure

  • Galina Hovhannisyan;Samvel Haroutiunian;Kristina Margaryan;Robert Ghazaryan;Rouben Aroutiounian
    • 환경생물
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    • 제23권4호
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    • pp.379-382
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    • 2005
  • The new cationic meso-substituted N-quarternized 4-pyridylporphyrins and their metal derivatives were synthesized as novel chemotherapeutics. The level of DNA damage induced by porphyrins TOBut4PyP, TOBut4PyP, TOEt4PyPMn and TOBut4PyPMn and its dependence on the chemical structure of compounds were analyzed by the Comet-assay. On the base of data obtained, the investigated porphyrins may be arranged by their genotoxic activity in the following order: TOEt4PyP>TOEt4PyPMn>TOBut4PyP>TOBut4PyPMn. Thus, i) the genotoxicity of the Mn-derivatives of TOEt4PyP and TOBut4PyP is higher than the original porphyrins and ii) the genotoxicity of TOEt4PyP and TOEt4PyPMn is increased after substitution of a butyl radical for ethyl one. The applied Comet-assay permits to reveal the dependence of DNA damage induction on the chemical structure of porphyrins.