• Title, Summary, Keyword: antiangiogenic

Search Result 77, Processing Time 0.035 seconds

Lupane Derivatives-I: Synthesis and Cytotoxic Activity (루판 유도체의 합성 및 세포독성-I)

  • You, Young-Jae;Kim, Yong;Ahn, Byung-Zun
    • YAKHAK HOEJI
    • /
    • v.46 no.5
    • /
    • pp.295-300
    • /
    • 2002
  • To observe the structure-activity relationship of lupane derivatives both on cytotoxic and antiangiogenic activity, twelve lupane derivatives were prepared; their antiangiogenic and cytotoxic activities were evaluated. Among them, four compounds were more cytotoxic than betulinic acid. Carboxylic acid at C28 seemed to be essential for cytotoxic activity. But, a selective cytotoxicity toward SK-MEL-2 was not observed. As for antiangiogenic activity, none of the compounds except lupeol showed antiangiogenic activity at 30 $\mu\textrm{g}$/mL.

A New Potent Angiogenesis Inhibitor, FR-118487

  • Otsuka, Takanao;Ohkawa, Takehiko;Shibata, Toshihiro;Oku, Teruo;Okuhara, Masakuni;Terano, Hiroshi;Kohsaka, Masanobu;Imanaka, Hiroshi
    • Journal of Microbiology and Biotechnology
    • /
    • v.1 no.3
    • /
    • pp.163-168
    • /
    • 1991
  • A new angiogenesis inhibitor, FR-118487 was obtained by chemical modification of FR-111142 which was isolated from the fermentation products of Scolecobasidium arenarium F-2015. The antiangiogenic activity of FR-118487 was compared with that of the parent compound, FR-111142. In the endothelial cell proliferation test in vitro and the angiogenesis in the chick embryo chorioal-lantoic membrane assay, FR-118487 had about 5∼10 times stronger antiangiogenic activities than FR-111142. In addition, FR-118487 inhibited the angiogenesis in the rabbit corneal assay and suppressed the solid tumor growth in mice. These findings showed that FR-118487 would be a unique antiangiogenic agent with promising antitumor activity.

  • PDF

ANTI-TUMOR AND ANTI-ANGIOGENIC EFFECT OF THALIDOMIDE ON ORAL SQUAMOUS CELL CARCINOMA XENOGRAFTS IN NUDE MICE (누드마우스에 이종이식된 구강편평상피세포암종에 대한 thalidomide의 항암효과와 혈관형성억제에 관한 연구)

  • Kim, Su-Gon;Myoung, Hoon;Kim, Myung-Jin
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
    • /
    • v.27 no.4
    • /
    • pp.330-336
    • /
    • 2001
  • Angiogenesis is an essential process for the growth, invasion and metastasis of cancer. However, it is uncertain that antiangiogenic effects can be a major treatment strategy of oral cancer. The aim of this study was to investigate whether thalidomide, which is known to be a potent inhibitor of angiogenesis, have inhibitory effect on the growth and antiangiogenic effects of oral squamous cell carcinoma(OSCC) xenografted in nude mice and whether antiangiogenesis of thalidomide can be included as a major treatment strategy of oral cancer. After human oral squamous cell carcinoma strain KB was subcutaneously implanted in 20 nude mice, the volume of tumor was measured every three days. When the tumor mass reached $75{\sim}100mm^3$, thalidomide(200mg/kg/d) was administered into 10 experimental nude mice and the same volume of distilled water was administered into 10 control nude mice and the tumor volume was measured every three days. The excised tumor masses on the 30th day after administration were frozen and processed for immunohistochemistry using vascular endothelial growth factor(VEGF) and CD31. We evaluated microvessel density and VEGF expression. The results were as follows ; 1. Thalidomide retarded the growth of human OSCC as compared with the control group, but it was not statistically significant. 2. A statistically significant lower microvessel density was observed in the thalidomide-treated group than in the control group(p<0.01) and thalidomide significantly reduced VEGF expression (p<0.01). Thalidomide exhibited significantly antiangiogenic effect, but did not inhibit the growth of human OSCC effectively. Antiangiogenic therapy of thalidomide alone is not likely to be effective in the treatment of human OSCC, but might be regarded as adjuvant chemotherapeutic strategy.

  • PDF

Changes of Serum VEGF and b-FGF in 26 Patients with Breast Cancer after Treatment with Hang-Am-Dan (HAD), an Antiangiogenic Botanical Prescription

  • Yoo Hwa Seung;Lee Nam Heon;Cho Jung Hyo;Lee Yeon Weol;Son Chang Gue;Kang Wee Chang;Cho Chong Kwan
    • The Journal of Korean Medicine
    • /
    • v.26 no.4
    • /
    • pp.22-30
    • /
    • 2005
  • Objectives: Recently, angiogenesis has gained an increasing interest as a prognostic factor in breast cancer. In this study we aimed to assess the anti angiogenic effects of HAD, a botanical anticancer remedy which has been prescribed in Daejeon University Oriental Hospital in Korea, on patients with breast carcinoma by measuring the serum vascular endothelial growth factor (VEGF), basic fibroblast growth factor (b-FGF) and platelets levels. Methods: The study included 26 consecutive breast cancer patients (mean age$\pm$standard deviation: 47.5$\pm$8.7 years) with stage II to IV disease who were treated with HAD (mean duration $\pm$ standard deviation: 264.5$\pm$121.6 days). In addition to routine laboratory and staging procedures, serum VEGF, b-FGF levels and platelet counts were determined as antiangiogenic markers. The antiangiogenic effects of HAD were evaluated by analyzing the differences between the values of the antiangiogenic markers before and after the treatment with HAD. Results: Serum b-FGF concentrations were significantly reduced after the treatment with HAD (P=0.042). Serum VEGF concentrations were found to have a somewhat decreasing change, though the change was not statistically significant (P=0.229). Platelet counts had little changes (P=O.80). Conclusions: It is supposed that HAD has effects on decreasing the serum b-FGF levels related with the clinical outcome of breast cancer patients.

  • PDF

Biological Screening of Novel Derivatives of Valproic Acid for Anticancer and Antiangiogenic Properties

  • Farooq, Muhammad;El-Faham, Ayman;Khattab, Sherine N.;Elkayal, Ahmed M.;Ibrahim, Mahmoud F.;Taha, Nael Abu;Baabbad, Almohannad;Wadaan, Mohammad A.M.;Hamed, Ezaat A.
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.18
    • /
    • pp.7785-7792
    • /
    • 2014
  • Background: Valproic acid (VPA) is a potent anticancer and antiangiogenic agent. However, design and synthesis of chemical derivatives with improved antiangiogenic and anticancer activities are still necessary. In this study a library of novel derivatives of VPA was synthesized and tested. Methods: A human liver cancer cell line (HepG2) and a human normal embryonic kidney cell line (HEK 293) were exposed to various concentrations of VPA derivatives for 24 hours and cell viability was checked by MTT colorimetric assay. Anti-angiogenic properties were evaluated in transgenic zebrafish embryos. Results: N-valproylglycine derivatives suppressed survival almost 70% (p value 0.001) in HepG2 cells but only 10-12% in HEK 293 cells (p value 0.133). They also suppressed angiogenic blood vessel formation by 80% when used between $2-20{\mu}M$ in zebrafish embryos. Valproic acid hydrazides showed moderate level of anticancer activity by affecting 30-50% (p value 0.001) of cell viability in HepG2 cells and 8-10% in HEK293 cells (p value 0.034). Conclusion: The majority of compounds in this study showed potent and stronger antiangiogenic and anticancer activity than VPA. They proved selectively toxic to cancer cells and safer for normal cells. Moreover, these compounds inhibited developmental angiogenesis in zebrafish embryos. Based on the fact that liver is a highly vascularized organ, in case of liver carcinoma these compounds have the potential to target the pathological angiogenesis and could be an effective strategy to treat hepatocellular carcinoma.

Antiangiogenic Activity of the Lipophilic Antimicrobial Peptides from an Endophytic Bacterial Strain Isolated from Red Pepper Leaf

  • Jung, Hye Jin;Kim, Yonghyo;Lee, Hyang Burm;Kwon, Ho Jeong
    • Molecules and Cells
    • /
    • v.38 no.3
    • /
    • pp.273-278
    • /
    • 2015
  • The induction of angiogenesis is a crucial step in tumor progression, and therefore, efficient inhibition of angiogenesis is considered a powerful strategy for the treatment of cancer. In the present study, we report that the lipophilic antimicrobial peptides from EML-CAP3, a new endophytic bacterial strain isolated from red pepper leaf (Capsicum annuum L.), exhibit potent antiangiogenic activity both in vitro and in vivo. The newly obtained antimicrobial peptides effectively inhibited the proliferation of human umbilical vein endothelial cells at subtoxic doses. Furthermore, the peptides suppressed the in vitro characteristics of angiogenesis such as endothelial cell invasion and tube formation stimulated by vascular endothelial growth factor, as well as neovascularization of the chorioallantoic membrane of growing chick embryos in vivo without showing cytotoxicity. Notably, the angiostatic peptides blocked tumor cell-induced angiogenesis by suppressing the expression levels of hypoxia-inducible $factor-1{\alpha}$ and its target gene, vascular endothelial growth factor (VEGF). To our knowledge, our findings demonstrate for the first time that the antimicrobial peptides from EML-CAP3 possess antiangiogenic potential and may thus be used for the treatment of hypervascularized tumors.

Screening of angiogenesis inhibitors from Korean plants (I) (한국산 식물자원으로부터 신생혈관 억제제 검색 (I))

  • You, Young-Jae;Park, Jin-Young;An, Ren-Bo;Kim, Young-Ho;Kang, Jong-Seong;Ahn, Byung-Zun;Bae, Ki-Hwan
    • Korean Journal of Pharmacognosy
    • /
    • v.31 no.3
    • /
    • pp.320-324
    • /
    • 2000
  • Methanol extracts of 94 Korean plants were screened for angiogenesis inhibitors using the tube-like formation assay of HUVEC (Human Umbilical Vein Endothelial Cell) and evaluated for growth inhibitory activity on A549 cells, human lung cancer cells. Extracts of Euphorbia sieboldiana, Adonis amurensis, and Anthriscus sylvestris showed antiangiogenic and growth inhibitory activity at $50\;{mu}g/ml$. Aristolochia manshuriens and Styrax obassia expressed antiangiogenic activity without growth inhibitory action.

  • PDF

Antiangiogenic Activity of Bupleurum longiradiatum on human umbilical venous endothelial cells

  • You, Young-Jae;Lee, Im-Seon;Kim, Yong;Bae, Ki-Hwan;Ahn, Byung-Zun
    • Archives of Pharmacal Research
    • /
    • v.25 no.5
    • /
    • pp.640-642
    • /
    • 2002
  • The ethyl acetate fraction of Bupleurum longiradiatum was found to have an inhibitory effect on the tube-like formation of human umbilical venous endothelial (HUVE) cells. The active compounds, isolated from the fraction, were identified as acetylbupleurotoxin (P1) and bupleurotoxin (P2). The compounds P1 and P2 completely inhibited the tube-like formation of HUVE cells at 30 ${\mu}g$/ml, below the cytotoxic concentration. But, they did not exhibit antitumor activity on BDF1 mice bearing Lewis lung carcinoma cells despite their antiangiogenic activity.