RESUMO
Compounds bearing an acyl group of a various size at 1'-OH of shikonin were synthesized as acyl analogues of shikonin, which was isolated from the root of Lithospermum erythrorhizon, and evaluated for inhibitory effect on topoisomerase-I activity. A selective acylation at 1'-OH of shikonin in the presence of dicyclohexylcarbodiimide and 4-(dimethylamino)pyridine gave rise to a good yield of corresponding acylshikonin derivatives. In general, analogues with an acyl group of shorter chain lengths (C2-C6) exerted a stronger inhibitory action than those with longer chain lengths (C7-C20). While the halogen substitution at C-2 of the acetyl moiety failed to increase the inhibitory potency, the placement of double bonds in the acyl group (C5-C7) augmented the potency remarkably. Of the 32 derivatives evaluated, 15 compounds exhibited a higher inhibitory effect than shikonin. Noteworthy, the inhibitory potency of acetylshikonin, propanoylshikonin, and 4-pentenoylshikonin was approximately 4-fold greater than that of camptothecin. All these data suggest that the size of acyl moiety is important for the enhancement of potency, and the presence of olefinic double bonds is also beneficial.
Assuntos
Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/farmacologia , Naftoquinonas/síntese química , Naftoquinonas/farmacologia , Inibidores da Topoisomerase I , Acetilação , DNA Topoisomerases Tipo I/metabolismo , DNA Super-Helicoidal/metabolismo , Células HeLa , Humanos , Extratos Vegetais/farmacologia , Raízes de Plantas/químicaRESUMO
2- or 6-(1-hydroxyiminoalkyl)-5,8-dimethoxy-1, 4-naphthoquinone(2- or 6-hyim-DMNQ) derived from the roots of Lithospermum erythrorhizon was synthesized for the evaluation of antitumor activities. Among those derivatives, 2-hyim-DMNQ-S33 was found to be a potent anticancer agent. This compound suppressed the proliferation of Radiation Induced Fibrosarcoma (RIF) cells in a dose-dependent manner. 2-hyim-DMNQ-S33 significantly prolonged the survival time by 239% as compared with Sarcoma 180 tumor-bearing control mice in vivo. We found that the compound significantly suppressed phosphorylation of extracellular signal-regulated kinase (pERK) and activated c-jun-N-terminal kinase (JNK) and protein kinase C (PKC)-alpha following 4 h-treatment. These findings indicate that 2-hyim-DMSQ-S33 exerts antitumor activities by regulating pERK, JNK and PKC-alpha.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Animais , Divisão Celular/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos ICR , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Naftoquinonas/farmacologia , Neoplasias Experimentais/tratamento farmacológico , Proteína Quinase C/metabolismoRESUMO
Novel twelve esters of chlorambucil with 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone were synthesized and tested for their antitumor activity in mice bearing S-180 ascitic cells as well as cytotoxic activity against L1210 cells. Eight of them were highly cytotoxic on L1210 cells (ED(50), <6 microg mL(-1)) and derivatives 1 and 12 (T/C, 200 and 205%) appeared more active in vivo than chlorambucil (T/C, 168%).
Assuntos
Antraquinonas/química , Antraquinonas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Clorambucila/química , Animais , Clorambucila/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Leucemia L1210 , Masculino , Camundongos , Camundongos Endogâmicos ICR , Sarcoma Experimental/tratamento farmacológico , Sarcoma Experimental/mortalidade , Relação Estrutura-AtividadeRESUMO
Some 2- or 6-acyl-5,8-dimethoxy-1,4-naphthoquinone (DMNQ) derivatives were synthesized and evaluated for inhibition of DNA topoisomerase I and cytotoxicity against L1210 cells. Compared with 2-acyl-DMNQ derivatives, 6-acyl-DMNQ compounds, bearing a higher electrophilic quinone moiety, showed a higher potency in the inhibition of DNA topoisomerase I and the cytotoxicity, implying the possible participation of electrophilic arylation in their bioactivities. Time and temperature dependence of the enzyme inhibition suggests that the arylation occurs irreversibly. Among the 6-acyl-DMNQ derivatives, the ones possessing an acyl group of an intermediate size (C(5)-C(9)) showed higher potency in their bioactivities than other derivatives. Furthermore, for the effective inhibition of DNA topoisomerase I, the size of acyl moiety of 6-acylated derivatives seems to be limited to < 12 carbon atoms.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Naftoquinonas/síntese química , Naftoquinonas/farmacologia , Inibidores da Topoisomerase I , Animais , Técnicas In Vitro , Leucemia L1210/tratamento farmacológico , Camundongos , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/enzimologia , Oxirredução , Consumo de Oxigênio/efeitos dos fármacos , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
Thirty six 5,8-dimethoxy-1,4-naphthoquinone derivatives, which bear unsaturated alkyl side chain with ester bond, were synthesized and tested cytotoxic activity on L1210 cells and antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R1 being methyl and propyl (IV1-24) were not enhanced by replacing the alkanoyls with alkenoyls. In contrast, the introduction of the alkenoyl moieties on the compounds with R1 = hexyl (IV25-36) resulted in the enhancement of their cytotoxicities. Replacement of alkanoyl group with an alkenoyl group generally increased the T/C value of the mice bearing S-180 cells.
Assuntos
Antineoplásicos , Antineoplásicos/farmacologia , Naftoquinonas/farmacologia , Animais , Antineoplásicos/síntese química , Avaliação de Medicamentos , Técnicas In Vitro , Leucemia L1210/tratamento farmacológico , Camundongos , Camundongos Endogâmicos ICR , Naftoquinonas/síntese química , Sarcoma 180/tratamento farmacológico , Células Tumorais CultivadasRESUMO
1-Polyoxyphenyl-3-(2,6-dioxyphenyl)propane-1,3-diones have been synthesized as intermediates for flavone synthesis by condensation of 2-(2,6-dioxybenzoyloxy)polyoxyacetophenone in the presence of phase transfer catalyst. The average yields of 1-polyoxyphenyl-3-phenylpropane-1,3- diones, 1-polyoxyphenyl-3-(2-benzyloxyphenyl)propane-1,3-diones and 1-polyoxy-3-(2,6-dibenzyloxyphenyl)propane-1,3-diones were 79%, 74% and 71%, respectively. The bulkiness of the benzyloxy groups or methoxy groups exerted steric hindrance and reduced the yield. Nevertheless, the yields were higher than the previously reported ones.
Assuntos
Benzoatos/síntese química , Flavonoides/síntese química , Metano/análogos & derivados , Metano/síntese química , Benzoatos/química , Metano/químicaRESUMO
An HPLC method was developed to resolve the enantiomers of shikonin derivatives of the Lithospermi Radix. The optimum mobile phase on a Chiracel AD column was 5% isopropanol in n-hexane with flow rate of 1 ml/min. Establishment of this method made possible to determine the ratios of shikonin/acetylshikonin or alkanin/acetylalkanin in the same root. The correlation of the ratios of these substance pairs appeared characteristic for the country where they were originated from. All of the Korean species showed significantly higher ratios of shikonin/acetylshikonin and alkanin/acetylalkanin than the Chinese ones. This method would be useful to determine the origin of Lithospermi Radix.
Assuntos
Anti-Inflamatórios não Esteroides/química , Naftoquinonas/química , Plantas Medicinais/química , 2-Propanol , Acetilação , Calibragem , Cromatografia Líquida de Alta Pressão , Coreia (Geográfico) , Raízes de Plantas/química , Solventes , EstereoisomerismoRESUMO
The rate of the GSH conjugate formation, the inhibition of DNA topoisomerase-I and the cytotoxic activity against L1210 cells of the naphthoquinones showed the same order; 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) > 6-(1-hydroxyethyl)-DMNQ > 2-(1-hydroxyethyl)-DMNQ; the steric hindrance of the substituents, particularly 2-substutuent, in reacting with cellular nucleophiles must be the main cause for lowering the bioactivities. Acetylation of 2-(1-hydroxyethyl)-DMNQ producing 2-(acetyloxyethyl)-DMNQ potentiated the bioactivities; 2-(1-hydroxyethyl)-DMNQ did not react with GSH and the enzyme, and showed ED50 of 0.680 microgram/ml, whereas the values of 2-(1-acetyloxyethyl)-DMNQ were the conjugate formation of 0.14 microM, IC50 value of 81 microM for the enzyme inhibition and ED50 of 0.146 microgram/ml for the cytotoxcity. Furthermore, the acetylation 2-(1-hydroxyethyl)-DMNQ (T/C, 119%) enhanced the T/C values for the mice bearing S-180 tumor [T/C of 2-(1-acetyloxyethyl)-DMNQ, 276%]. It was assumed that the difference in bioactivities ensued by acetylation was based on the mechanism of the so-called bioreductive alkylation.
Assuntos
Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/farmacologia , Naftoquinonas/síntese química , Naftoquinonas/farmacologia , Acetilação , Animais , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacologia , Glutationa/química , Leucemia L1210/tratamento farmacológico , Masculino , Camundongos , Camundongos Endogâmicos ICR , Oxirredução , Sarcoma 180/tratamento farmacológico , Inibidores da Topoisomerase IRESUMO
Formation of glutathione (GSH) conjugates with 2- or 6-(1-hydroxymethyl)- and 2-(1-hydroxyethyl)-DMNQ derivatives (DMNQ, 5,8-dimethoxy-1,4-naphthoquone) was carried out in phosphate buffer (pH 7.4), in the presence of glutathione-S-transferase (GST), in rat liver S-9 fraction and by perfusion, and the rates of conjugates formation were compared and correlated to cytotoxicity. The GSH conjugates of 6-(1-hydroxyalkyl)-DMNQ derivatives were formed faster than 2-(1-hydroxyalkyl)-DMNQ derivatives under all of the media, implying that steric hindrance was the cause of lowering the rate of conjugate formation of 2-substituted derivatives. For both isomers, addition of GST did not improve the reaction rate, compared with that in buffer, while the reaction in the S-9 fraction and the perfusate was accelerated to a great extent. The catalytic effect of the S-9 fraction and the perfusion on 2-isomers was greater than on 6-substituted ones, suggesting that S-9 fraction and the perfusate contain an effective system relaxing the steric hindrance of 2-(1-hydroxyalkyl)-DMNQ derivatives. Furthermore, a good correlation between the formation of the GSH conjugates and the cytotoxic activity of both naphthazarin isomers suggests that the steric hindrance is a cause of lowering the cytotoxicity of 2-isomers.
Assuntos
Antineoplásicos/metabolismo , Glutationa Transferase/metabolismo , Glutationa/metabolismo , Fígado/metabolismo , Microssomos Hepáticos/metabolismo , Naftoquinonas/metabolismo , Animais , Camundongos , Naftoquinonas/farmacologia , Perfusão , Ratos , Relação Estrutura-AtividadeRESUMO
A series of 2-(1-hydroxyiminoalkyl)-1,4-dimethoxy-9,10-anthraquinones (oximes) was synthesized and evaluated for cytotoxicity against L1210 cells and A549 cells. These oximes showed a greater cytotoxic activity compared to those of 2-(1-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones as the hydroxyalkyl bioisosteres. The enhanced cytotoxicity assumed to be due to the improved water solubility of the hydroxyimino group. Moreover, it was found that the cytotoxicity of the oximes decreased with elongation of alkyl groups at the side chain. All of the synthesized compounds showed higher cytotoxicity against L1210 cells than A549 cells.
Assuntos
Antraquinonas/síntese química , Antineoplásicos/síntese química , Animais , Antraquinonas/farmacologia , Antineoplásicos/farmacologia , Humanos , Leucemia L1210/tratamento farmacológico , Leucemia L1210/patologia , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/patologia , Camundongos , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
An attempt to estabilish the relationship between anti-cell adhesive action of phenylacetylshikonin anallogues and their cytotoxicity against A549 cells was done. In the one hour incubation with A549 cells, alpha-methoxyphenylacetyl-(9), alpha-acetoxyphenylacetyl-(13), 3,4-methylen-edioxyphenylacetyl-(15) and 4-(N,N-dimethylamino)-phenylacetylshikonin (17) analogues showed a high anti-cell adhesive activity (IC(100) value, 4-8 mug/ml), while halophenylacetyl-and dimethoxy-or trimethoxyphenylacetyl analogues expressed no activity at 40 mug/ml, indicating that the presence of a bulky group at C'-alpha and a polar group at C-4 of phenylacetyl moiety may be important. A similar structure activity relationship exists for the 48 hr cytotoxocity (ED(50)) of phenylacetylshikonin analogues in A 549 cells, but not in either K562 or L1210 cells. Furthermore, the difference between IC(100) values for anti-cell adhesive activity and ED(50) values for cytotoxicity of potent compound in A549 cells was not so great (1.5 to 3 times). Based on these observations, it is proposed that the anti-cell adhesive action of phenylacetylshikonins might be responsible for their cytotoxicity in A549 cells.
RESUMO
2-(1-Aryl-1-hydroxymethyl)- and 2-aroyl-DHAQ derivatives (DHAQ, 1,4-dihydroxy-9,10-anthraquinone), and 2-(1-aryl-1-hydroxymethyl)-ATO derivatives (ATO, anthracene-1,4,9,10-tetraone) were synthesized and their antitumor activities were determined. 2-(1-Aryl-1-hydroxymethyl)-DHAQ derivatives showed a stronger cytotoxicity compared to the series of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives. It was suggested that the presence of aryl group at the side chain accelerated the bioreductive activation leading to cell death. 2-Aroyl-DHAQ derivatives, despite their higher electrophilicity, revealed smaller cytotoxicity and antitumor activity (expressed by T/C value) than 2-(1-aryl-1-hydroxymethyl)-DHAQ derivatives. Thus, no consistent relationship between the electronic effect on aromatic side chain and the cytotoxicity was observed. ATO series exhibited a higher antitumor activity (T/C, 125 to approximately 218%), though their cytotoxicity was not further improved compared to that of 2-(1-aryl-1-hydroxymethyl)-1,4-dihydroxy-9,10-anthraquinones. They manifested no correlation between the cytotoxicity and the antitumor activity. In case of 2-[1-hydroxy-1-(4-propylphenyl)-methyl]-ATO, the most bioactive one in vivo among the same series, it showed an ED50 value of 10.2 mg/mL and a T/C value of 218%. It is assumed that the anthracene-1,4,9,10-tetraones after uptake into cellular tissues might be transformed to a cytotoxic metabolite(s).
Assuntos
Antracenos/síntese química , Antracenos/farmacologia , Antraquinonas/síntese química , Antraquinonas/farmacologia , Antineoplásicos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2- and 6-(1-azidoalkyl)-DMNQ derivatives.
Assuntos
Antineoplásicos/síntese química , Azidas/síntese química , Inibidores Enzimáticos/síntese química , Naftoquinonas/síntese química , Inibidores da Topoisomerase I , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Azidas/química , Azidas/farmacologia , Cromatografia em Camada Fina , Ensaios de Seleção de Medicamentos Antitumorais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Leucemia L1210/patologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Naftoquinonas/química , Naftoquinonas/farmacologia , Transplante de Neoplasias , Sarcoma Experimental/tratamento farmacológico , Sarcoma Experimental/patologia , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1-hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%
Assuntos
Antineoplásicos/uso terapêutico , Naftoquinonas/uso terapêutico , Sarcoma 180/tratamento farmacológico , Animais , Antineoplásicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Masculino , Camundongos , Camundongos Endogâmicos ICR , Naftoquinonas/química , Células Tumorais CultivadasRESUMO
Various analogues of 5,8-dimethoxy-1,4-naphthoquinone (DMNQ) such as 2- or 6-(1-hydroxyiminoalkyl)-DMNQs were prepared and evaluated for the antitumor action. (1-Hydroxyiminoalkyl)-DMNQ derivatives expressed greater antitumor action than (1-hydroxyalkyl)- or acyl-DMNQ derivatives. Moreover, 6-(1-hydroxyiminoalkyl)-DMNQ derivatives expressed higher antitumor action than 2-sudstituted ones, suggestive of a steric effect. Some of 6-(1-propyloxyalkyl)-DMNQ derivatives with an alkyl group of butyl to octyl moiety showed T/C values of >400%.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Naftoquinonas/síntese química , Naftoquinonas/farmacologia , Sarcoma 180/tratamento farmacológico , Animais , Indicadores e Reagentes , Injeções Intraperitoneais , Masculino , Camundongos , Camundongos Endogâmicos ICR , Transplante de Neoplasias , Relação Estrutura-Atividade , Análise de SobrevidaRESUMO
Thirty-four glutathione conjugates of 5,8-dimethoxy-1,4-naphthoquinones (DMNQ) were synthesized and their structure was determined. The yield of GSH conjugate was dependent on size of alkyl group; the longer the size of alkyl group was, the lower was the yield. It was also found that the length of alkyl side chain influenced the chemical shift of quinonoid protons; the quinonoid protons of 2-glutathionyl DMNQ derivatives with R=H to propyl, 6.51-6.59 ppm vs. other ones with R=butyl to heptyl, 6.64-6.68 ppm. This was explained to be due to a folding effect of longer alkyl group. Glutathione (GSH) reacted with DMNQ derivative first to form a 1,4-adduct (2- or 3-glutathionyl-1,4-dihydroxy-5,8-dimethoxynaphthalenes) and then, the adduct was autooxidized to 2- or 3-glutathionyl-DMNQ derivatives. Moreover, GSH reduced DMNQ derivatives to their hydrogenated products. It was suggested that such an organic reaction might play an important role for a study of metabolism or toxicity of DMNQ derivatives in the living cells.
Assuntos
Glutationa/síntese química , Glutationa/metabolismo , Naftoquinonas/síntese química , Cromatografia em Camada Fina , Desenho de Fármacos , Glutationa/análogos & derivados , Glutationa/química , Peróxido de Hidrogênio/análise , Indicadores e Reagentes , Naftoquinonas/química , OxirreduçãoRESUMO
Fourty eight derivatives of 2-(1-oxyalkyl)-1,4-dioxy-9,10-anthraquinone were synthesized, and their antitumor activity was evaluated. On the whole, 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinones (DHAQ = 1,4-dihydroxy-9,10-anthraquinone) showed stronger cytotoxic activity against L1210 cells than 2-(1-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones(DMAQ = 1,4-dimethoxy-9,10-anthraquinone), implying that free hydroxy groups at C-1 and C-4 of the anthraquinone structure are necessary for the cytotoxic activity. The bioactivity of 2-(1-hydroxyalkyl)-DHAQ derivatives differed according to the size of alkyl group at C-1; while the elongation of alkyl group over 7 carbon atoms failed to enhance the bioactivity, the derivatives possessing alkyl moiety of 1-6 carbon atoms showed an increase in the cytotoxicity and the antitumor activity in Sarcoma-180; 2-hydroxymethyl-DHAQ (ED50, 15 micrograms/ml; T/C, 125%), 2-(1-hydroxyethyl)-DHAQ(1.9 micrograms/ml; 139.2%), 2-(1-hydroxypropyl)-DHAQ (7.2 micrograms/ml; 135.1%), 2-(1-hydroxybutyl)-DHAQ (10.2 micrograms/ml; 125.3%), 2-(1-hydroxypentyl)-DHAQ (23.7 micrograms/ml; 110.1%), and 2-(1-hydroxyhexyl)-DHAQ (58 micrograms/ml; 108%). Next, 2-(1-Hydroxyalkyl)-DHAQ derivatives were acetylated to produce 2-(1-acetoxyalkyl)-DHAQ analogues. Although the acetylation somewhat enhanced the cytotoxicity, but not the antitumor action. In addition, the presence of phenyl group at C-1' enhanced the cytotoxicity and the T/C value, compared to alkyl groups of same size; 2-(1-hydroxy-1-phenyl)-DHAQ (ED50, 5.6 micrograms/ml; T/C, 137%).
Assuntos
Antineoplásicos/síntese química , Quinonas/síntese química , Acetilação , Animais , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Leucemia L1210/tratamento farmacológico , Longevidade/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos ICR , Quinonas/farmacologia , Sarcoma 180/tratamento farmacológico , Células Tumorais CultivadasRESUMO
The effects of boiled water extracts of clonorchicidal raw drugs screened by the EPG counts in vivo on the structure of Clonorchis sinensis were investigated. The extracts of Cassia obutusifolia and Dictamnus dasycarpus did not seem to induce the morphological changes of the worms, and in those of Machilus thunbergii and Prunús mume, widening of bladder to lower level of seminal receptacle was visible without any other changes. Those of Inula helenium and Saussurea lappa, however, disclosed regressive and progressive changes as degeneration, atrophy, necrosis, dilatation, etc. of viscera of the worms. The recover rates of the worms from experimentally infected rabbits administered with the extracts of I. helenium and S. lappa for 30 days, beginning at the 3rd day of inoculation, were as low as 2% and 2.8%, respectively.
Assuntos
Anti-Helmínticos/uso terapêutico , Clonorquíase/tratamento farmacológico , Clonorchis sinensis/efeitos dos fármacos , Plantas Medicinais , Animais , Anti-Helmínticos/isolamento & purificação , Clonorquíase/parasitologia , Clonorchis sinensis/ultraestrutura , Feminino , Masculino , Coelhos , Especificidade da EspécieRESUMO
In order to investigate clonorchicidal activity in vivo, boiled water extracts of 32 species of clonorchicidal raw drugs in vitro were orally administered into rabbits infected with Clonorchis sinensis. The results of the observation of EPG variation were as follows: Suppression effects of egg-laying capacity from the rabbits administered Prunus mume and Inula helenium were greatest. Those from Dictamnus dasycarpus and Saussurea lappa were somewhat effective. Machilus thunbergii and Cassia obutusifolia, however, were less effective.
Assuntos
Anti-Helmínticos/uso terapêutico , Clonorquíase/tratamento farmacológico , Plantas Medicinais , Animais , Anti-Helmínticos/isolamento & purificação , China , Clonorquíase/parasitologia , Avaliação Pré-Clínica de Medicamentos , Fezes/parasitologia , Contagem de Ovos de Parasitas , CoelhosRESUMO
Two new polyines showing good cytotoxic activity against L1210 cells were isolated from Korean ginseng root. These were 3-acetyloxy-9,10-epoxy-heptadec-1-en-4,6-diyne(acet ylpanaxydol, ED50 = 0.52 microgram/ml) and 10-chloro-3,9-dihydroxyheptadec-1-en-4,6-diyne(Panaxydolc hlorohydrin, ED50 = 0.50 microgram/ml).