| In vitro: |
| Fitoterapia. 2014 Dec;99:276-83. | | Inhibition of hepatitis C virus replication by chalepin and pseudane IX isolated from Ruta angustifolia leaves.[Pubmed: 25454460] |
Hepatitis C virus (HCV) infection is highly prevalent among global populations, with an estimated number of infected patients being 170 million. Approximately 70-80% of patients acutely infected with HCV will progress to chronic liver disease, such as liver cirrhosis and hepatocellular carcinoma, which is a substantial cause of morbidity and mortality worldwide. New therapies for HCV infection have been developed, however, the therapeutic efficacies still need to be improved. Medicinal plants are promising sources for antivirals against HCV. A variety of plants have been tested and proven to be beneficial as antiviral drug candidates against HCV.
METHODS AND RESULTS:
In this study, we examined extracts, their subfractions and isolated compounds of Ruta angustifolia leaves for antiviral activities against HCV in cell culture. We isolated six compounds, chalepin, scopoletin, γ-fagarine, arborinine, kokusaginine and pseudane IX. Among them, chalepin and pseudane IX showed strong anti-HCV activities with 50% inhibitory concentration (IC₅₀) of 1.7 ± 0.5 and 1.4 ± 0.2 μg/ml, respectively, without apparent cytotoxicity. Their anti-HCV activities were stronger than that of ribavirin (2.8 ± 0.4 μg/ml), which has been widely used for the treatment of HCV infection.
CONCLUSIONS:
Mode-of-action analyses revealed that chalepin and pseudane IX inhibited HCV at the post-entry step and decreased the levels of HCV RNA replication and viral protein synthesis. We also observed that arborinine, kokusaginine and γ-fagarine possessed moderate levels of anti-HCV activities with IC₅₀ values being 6.4 ± 0.7, 6.4 ± 1.6 and 20.4 ± 0.4 μg/ml, respectively, whereas scopoletin did not exert significant anti-HCV activities at 30 μg/ml. | | Mutagenesis. 1989 Nov;4(6):467-70. | | The SCE-inducing potency of the furoquinoline alkaloid, gamma-fagarine, and a gamma-fagarine-containing tincture from Rutae Herba, in cultured human lymphocytes.[Pubmed: 2695761] |
METHODS AND RESULTS:
gamma-Fagarine, a furoquinoline alkaloid naturally occurring in Rutae Herba induces sister chromatid exchanges (SCEs) in human lymphocyte cultures in a dose-dependent manner.
The alkaloid is a direct-acting but weak SCE inducer. Similar direct but weak activity was detected in a sample of a commercial Rutae Tinctura which contained 68 micrograms/ml of gamma-Fagarine. The strong toxicity of the tincture makes it difficult to test a broader concentration range.
CONCLUSIONS:
There is some evidence that the SCE-inducing activity of the tincture is mainly due to the presence of gamma-Fagarine. | | Mutat Res. 1985 Dec;144(4):221-5. | | Mutagenic activities of dictamnine and gamma-fagarine from dictamni radicis cortex (Rutaceae).Mutagenic activities of dictamnine and gamma-fagarine from dictamni radicis cortex (Rutaceae).[Pubmed: 4069140] |
METHODS AND RESULTS:
A methanol extract of Dictamni Radicis Cortex exhibited a mutagenic effect on Salmonella typhimurium TA100 and TA98 with S9 mix. Two mutagenic compounds in Dictamni Radicis Cortex were isolated on a Sephadex LH 20 column and silica gel column chromatography and by preparative TLC. These were identified as dictamnine and gamma-Fagarine by UV, EI-Mass, 1H-NMR. Dictamnine and gamma-Fagarine were mutagenic in strain TA100 and TA98 with S9 mix. The dose-response curves were linear in the range 10-40 micrograms.
CONCLUSIONS:
Dictamnine and gamma-Fagarine had specific activities (His+/microgram) of about 50-70 revertant colonies in strain TA100, while in strain TA98 there were about 30-50 revertant colonies. |
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