• Title/Summary/Keyword: antineoplastic activity

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The synthesis and antineoplastic activity of alkyl thiosulfates and diaryl disulfides

  • Chae, Dong-Kyu;Chung, Won-Keun;Lee, Nam-Bock
    • YAKHAK HOEJI
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    • v.16 no.3
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    • pp.149-154
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    • 1972
  • Seven alkylthiosulfates and three diaryl thiosulfates were synthesized as potential antineoplastic agents, and subjected to antineoplastic activity test against Ehrlich ascites carcinoma, SN-36 Leukemia and Sarcoma 180. Allyl thiosulfate, n-propylthiosulfate and ${\beta}$-hydroxyethylthiosulfate were found as to be active against experimental tumors.

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Synthesis of Novel 4-Substituted Phenazone Derivatives as Potential Antibacterial and Antineoplastic Agents

  • Girges, M.M.;El-Zahab, Abou M.M.;Hanna, M.A.
    • Archives of Pharmacal Research
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    • v.11 no.3
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    • pp.169-174
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    • 1988
  • A new series of substituted phenazone derivatives has been prepared through a series of reactions that are illustrated in Scheme I. The antibacterial and antineoplastic activities of the prepared compounds were evaluated. While none of the synthesized products showed marked antibacterial activity, all of them possessed a significant antitumor effect.

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Pharmacokinetic Study on BR-28702-2, a New Anticancer Drug, in Rats (흰쥐에서의 신규 항암제 BR-28702-2의 체내동태)

  • 용철순;이신웅;전철수;채희상;신원섭;백우현
    • Biomolecules & Therapeutics
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    • v.3 no.2
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    • pp.97-103
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    • 1995
  • The purpose of this study was to determine pharmacokinetic parameters of BR-28702-2, a new antineoplastic agent which is the conjugate of nucleotide and phospholipid, and to compare them with those of ara-C. Male rats were cannulated in the left femoral vein and received a single i.v. bolus dose of either BR-28702-2 or ara-C. BR-28702-2 was also administered i.p. and plasma samples were analyzed by reversedphase HPLC. The t$_{1}$2($\beta$)/ of ara-C(1.22 hr.) was significantly smaller than that of BR-28702-2(4.420 hr.). The absolute bioavailability of BR-28702-2 after i.p. injection was 1.125%. This lower bioavailability, together with previous reports that marked antineoplastic activity was observed when given i.p., indicates that BR-28702-2 would act as a depot system to release active moieties. Further works, therefore, need to be done to characterize active metabolites.

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Antineoplastic Effect of Extracts from Traditional Medicinal Plants and Various Plants (III) (전통 약용식물 및 각종 식물의 항암 효과에 대한 연구 (III))

  • Hyun, Jin-Won;Lim, Kyoung-Hwa;Sung, Min-Sook;Kang, Sam-Sik;Paik, Woo-Hyun;Bae, Kun-Woo;Cho, Hyun;Kim, Hyoung-Ja;Woo, Eun-Rhan;Park, Ho-Koon;Park, Jae-Gahb;Yang, Yong-Man
    • Korean Journal of Pharmacognosy
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    • v.27 no.2
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    • pp.105-110
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    • 1996
  • Antineoplastic activity against human gastric and colon carcinoma cell lines was tested in eighty-three species of Korean plants including Korean medicinal plants which have been frequently used in oriental herb prescriptions. The plant materials were extracted with methanol and the cytotoxic activity was tested using a calorimetric tetrazolium assay (MTT assay). Twenty-six plant extracts against gastric carcinoma cell line, eighteen extracts against colon carcinoma cell line and fourteen plant extracts against both carcinoma cell lines showed antineoplastic activity at the concentration of less than $100{\mu}g/ml$. The effective components from four species have been isolated and reported.

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Antineoplastic Activity of Crude Saponin Mixture from the Roots of Luffa tuberosa (Roxb.) in Ehrlich Ascites Carcinoma Bearing Mice

  • Yeligar Veerendra C.;K. Murugesh;Dash Deepak;Nayak Siva S.;Maiti Bhim C.;Maity Tapan K.
    • Natural Product Sciences
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    • v.12 no.4
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    • pp.247-253
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    • 2006
  • The antitumor activity of crude saponin mixture obtained from Luffa tuberosa (Roxb.) (Fam; Cucurbitaceae) hairy roots (CSLT) in mice transplanted with Ehrlich ascites carcinoma (EAC) was investigated. The EAC-bearing mice receiving 150 and $300{\mu}g/kg$ body weight, (i.p) of CSLT have shown a dose dependent elevation in tumor-tree survival and a highest number of survivors were observed after administration of CSLT $(300{\mu}g/kg)$, which was considered as an optimum dose for its antineoplastic action. The mean survival time (MST) for this dose was approximately $47.1{\pm}0.74d$, when compared with $19.0{\pm}0.36d$ of untreated control. Administration of $300{\mu}g/kg$ CSLT resulted in 130% long-term increased survival time. The measurement of body weight, tumor volume, packed cell volume, viable and non-viable count indicated the efficacy of CSLT in tumor-bearing mice, there was a significant recovery in hematological profiles, and there was depletion in lipid peroxidation levels, and the antioxidant enzyme activities such as GSH, SOD and CAT were restored to near the normal levels. The CSLT was found to be devoid of conspicuous short-term toxicity in the mice when animals were intraperitoneally injected with 250, 500, 750 and $1000{\mu}g/kg$ bodyweight. The treated mice showed conspicuous toxic symptoms only at a dose of $1500{\mu}g/kg$. Mortality of the animals was monitored up to 14 d post drug treatment, $1/7^{th}$ of the $LD_{50}$ dose has been considered for the optimal antineoplastic activity.

Isolation and Identification of Squalene and Antineoplastic Activity of Its Residue Extract in Amaranth (Amaranth의 Squalene 동정과 잔사 추출물의 항암 작용 검색)

  • Lee, Jae-Hak;Moon, Hyung-In;Lee, Jung-Il;Kang, Chul-Whan;Lee, Seung-Taek
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.41 no.4
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    • pp.450-455
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    • 1996
  • In this study isolation and identification of squalene from amaranth and antineoplastic activity of its residue extract except squalene were determined to examine the utilization of grain amaranth in Korea. The content of squalene in amaranth grain was about 0.43%. The isolated squalene showed 99% pureness containing the identical molecular weight and structure provisionally in comparison with that of animal squalene from Sigma Co. by means of GC /Mass spectrum. Antineoplastic activity against human gastric and colon carcinoma cell line was measured in extract (except squalene) from Amaranth using MTT method. Extract from remaining plant good showed significant cytotoxic effect at the concentration of less than 230$\mu\textrm{g}$/ml.

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Studies on Anti-cancerous Substances from Higher Plane in East Asian Region

  • Takeya, Koichi
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 1999.10a
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    • pp.1-45
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    • 1999
  • To date many kinds of compounds have been obtained from plants kingdom as antineoplastic and anti-cancerous agents. However, there is no special type of compounds for ncancer therapy. Various types of substances are effective for various types of cancers and tumors: for instance, alkaloids, lignans, terpenes and steroids etc. Curcumol obtained from Curcuma aromatica was tested and noticed to be effective against cancer of the uterine cervix clinically Oridonin isolated from Rabdosia ssp.is now investigated for clinical trials in China. Moreover, camptothecine isolated from Camptotheca acuminata is also antineoplastic alkaloid, but is very toxic. Chemical modification has been tried to decrease its toxicity. This compound is now using as clinical agent. Harringtonin was investigated as an anticancerous drug in China. Taxol, a compound with a taxane ring isolated from the bark of Taxus brevifolia, has been demonstrated to have substantial anticancer activity in patients with solid tumors refractory standard chemotherapy. Supply of this drug has severely limited full exploration of its antineoplastic potential. Some efforts are continued in National Cancer Institute NCI) Washington for surveying various Taxus species for optimal taxol content, improvement in semi-synthesis from baccatin III, improvement in method of extraction, and development of alternative renewable resources. Further, there are many compounds which have been reported as antineoplastic agents. On the other hand, we have screened on higher plants collected in Japan, China, Korea, Southeast Asia and South America for antineoplastic activity, which has been done using Sarcoma 180 ascites in mice, P388 Iymphocytic leukemia in mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma (KB) cells in our laboratory, as primary screening. In this meeting, I will present on antitumor and cytotoxic substances of the higher plants (Rubia cordifolia, Ailanfhus Vilmoriniana, Aster tataricus, Taxus cuspidata var. nana, Cephalotaxus harringtonia var drupacea, etc.) selected from above screening tests.

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Studies on Anti-Cancerous Substances from Higher Plants in East Asian Region

  • Takeya, Koichi
    • Plant Resources
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    • v.3 no.1
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    • pp.1-45
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    • 2000
  • To date many kinds of compounds have been obtained from plants kingdom as antineoplastic and anti-cancerous agents. However, there is no special type of compounds for cancer therapy. Various types of substances are effective for various types of cancers and tumors: for instance, alkaloids. lignans, terpenes and steroids etc. Curcumol obtained from Curcuma aromatica was tested and noticed to be effective against cancer of the uterine cervix clinically. Oridonin isolated from Rabdosia ssp. is now investigate for clinical trials in China. Moreover camptothecine isolated from Camptotheca acuminata is also antineoplastic alkaloid, but is very toxic. Chemical modification has been tried to decrease its toxicity This compound is now using as clinical agent. Harringtonin was investigated as an anticancerous drug in China. Taxol, a compound with a taxane ring isolated from the bark of Taxus brevifotia. has been demonstrated to have substantial anticancer activity in patients with solid tumors refractory standard chemotherapy. Supply of this drug has severely limited full exploration of its antineoplastic potential Some efforts are continued in National Cancer Institute(NCI) Washington for surveying various Taxus species for optimal taxol content, improvement in semi-synthesis from baccatin 111, improvement in method of extraction, and development of alternative renewable resources. Further, there are many compounds which have been reported as antineoplastic agents. On the other hand, we have screened on higher plants collected In Japan, China, Korea. Southeast Asia and South America for antineoplastic activity, which has been done using Sarcoma 180 ascites in mice, P388 Iymphocytic leukemia In mice, Chinese hamster lung V-79 cells, P388 cells and nasopharynx carcinoma(KB) cells in our laboratory, as primary screening. In this meeting, 1 will present on antitumor and cytotoxic substances of the higher plants(Rubis cordifolia, Ailanthus vilmoriniana, Aster tataricus, Taxus cuspidata var. nana, Cephalotaxus harringtonia var. drupacea, etc.) selected from above screening tests.

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Studies on Antitumor Components of Cultured Basidiomycetes - Purification and Chemical Analysis of Antineoplastic Constituents of Cultured Mycelia of Laccaria laccata - (애기졸각버섯 배양(培養) 균사(菌絲)의 항암(抗癌) 성분(成分)의 정제(精製) 및 화학(化學) 분석(分析))

  • Kim, Yoo-Jin;Lee, Chong-Ock;Shim, Mi-Ja;Kim, Sung-Won;Choi, Eung-Chil;Kim, Byong-Kak
    • The Korean Journal of Mycology
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    • v.12 no.1
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    • pp.35-43
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    • 1984
  • To produce and characterize antineoplastic constituents in the submerged cultured­mycelia of Laccaria laccata, the mycelia were extracted with distilled water. Purification of the extract was carried out by acetone precipitation, by ion exchange chromatography using DEAE­Sephadex A-50, CM-Sephadex C-25 resins, and by gel filtration chromatography on Sephadex G-200. Each fraction obtained during the purification was examined for antineoplastic activity against sarcoma 180 in ICR mice. As the purification proceeded, the antineoplastic activity was markedly increased. The highly purified Fraction E showed 75% tumor inhibition ratio at a dose of 10mg/kg/day and contained 81% polysaccharide and 4% protein. The antitumor component of Fraction E stimulated an accumulation of peritoneal exudate cells including peritoneal macrophages, and is named laccaran.

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