Research Support, Non-U.S. Gov'ts
- From the traditional Chinese medicine plant Schisandra chinensis new scaffolds effective on HIV-1 reverse transcriptase resistant to non-nucleoside inhibitors
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Lijia Xu , Nicole Grandi , Claudia Del Vecchio , Daniela Mandas , Angela Corona , Dario Piano , Francesca Esposito , Cristina Parolin , Enzo Tramontano
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J. Microbiol. 2015;53(4):288-293. Published online March 4, 2015
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DOI: https://doi.org/10.1007/s12275-015-4652-0
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Abstract
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HIV-1 reverse transcriptase (RT) is still an extremely attractive
pharmaceutical target for the identification of new inhibitors
possibly active on drug resistant strains. Medicinal
plants are a rich source of chemical diversity and can be used
to identify novel scaffolds to be further developed by chemical
modifications. We investigated the ability of the main lignans
from Schisandra chinensis (Turcz.) Baill. fruits, commonly
used in Traditional Chinese Medicine, to affect HIV-1 RT
functions. We purified 6 lignans from Schisandra chinensis
fruits and assayed their effects on HIV-1 RT and viral replication.
Among the S. chinensis fruit lignans, Schisandrin B
and Deoxyschizandrin selectively inhibited the HIV-1 RTassociated
DNA polymerase activity. Structure activity relationship
revealed the importance of cyclooctadiene ring substituents
for efficacy. In addition, Schisandrin B was also able
to impair HIV-1 RT drug resistant mutants and the early
phases of viral replication. We identified Schisandrin B and
Deoxyschizandrin as new scaffold for the further development
of novel HIV-1 RT inhibitors.
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Citations
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- Antimicrobial Effects of Herbal Extracts on Streptococcus mutans and Normal Oral Streptococci
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Sung-Hoon Lee
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J. Microbiol. 2013;51(4):484-489. Published online August 30, 2013
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DOI: https://doi.org/10.1007/s12275-013-3312-5
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Abstract
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Streptococcus mutans is associated with dental caries. A cariogenic biofilm, in particular, has been studied extensively for its role in the formation of dental caries. Herbal extracts such as Cudrania tricuspidata, Sophora flavescens, Ginkgo biloba, and Betula Schmidtii have been used as a folk remedy for treating diseases. The purpose of this study was to evaluate and compare the antibacterial activity of herbal extracts against normal oral streptococci, planktonic and biofilm of S. mutans. Streptococcus gordonii, Streptococcus oralis, Streptococcus salivarius, Streptococcus sanguinis, and S. mutans were cultivated with brain heart infusion broth and susceptibility assay for the herbal extracts was performed according to the protocol of Clinical and Laboratory Standard Institute. Also, S. mutans biofilm was formed on a polystyrene 12-well plate and 8-well chamber glass slip using BHI broth containing 2% sucrose and 1% mannose after conditioning the plate and the glass slip with unstimulated saliva. The biofilm was treated with the herbal extracts in various concentrations and inoculated on Mitis-Salivarius bacitracin agar plate for enumeration of viable S. mutans by counting colony forming units. Planktonic S. mutans showed susceptibility to all of the extracts and S. mutans biofilm exhibited the highest level of sensitivity for the extracts of S. flavescens. The normal oral streptococci exhibited a weak susceptibility in comparison to S. mutans. S. oralis, however, was resistant to all of the extracts. In conclusion, the extract of S. flavescens may be a potential candidate for prevention and management of dental caries.
- Dysregulation of KSHV Replication by Extracts from Carthamus tinctorius L.
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Han Lee , Hyosun Cho , Myoungki Son , Gi-Ho Sung , Taeho Lee , Sang-Won Lee , Yong Woo Jung , Yu Su Shin , Hyojeung Kang
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J. Microbiol. 2013;51(4):490-498. Published online August 30, 2013
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DOI: https://doi.org/10.1007/s12275-013-3282-7
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Abstract
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Carthamus tinctorius L. (CT) is traditionally used to reduce ailments from diseases of the musculoskeletal system and connective tissue and diseases of blood circulation and the cardiovascular system. Flower extracts from CT are known to have antibacterial activity, anti-inflammatory activity, and to inhibit tumor promotion in mouse skin carcinogenesis. In order to discover new antiviral agents from CT extracts, we tested whether CT extracts contain antiviral activity against gammaherpesvirus infection. This study demonstrated that treatment with CT extracts disrupted KSHV latency in the viral-infected host cells, iSLK-BAC16. n-Hexane and EtOH fractions of CT extracts critically affected at least two stages of the KHSV life-cycle by abnormally inducing KSHV lytic reactivation and by severely preventing KSHV virion release from the viral host cells. In addition to the effects on
KSHV itself, CT extract treatments induced cellular modifications by dysregulating cell-cycle and producing strong cytotoxicity. This study demonstrated for the first time that CT extracts have antiviral activities that could be applied to development of new anti-gammaherpesviral agents.
- Anti-HIV-1 Efficacy of Extracts from Medicinal Plants
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Su-A Lee , Seong-Karp Hong , Chang-Il Suh , Mi-Hwa Oh , Jeong-Ho Park , Byoung-Wook Choi , Seung-Won Park , Soon-Young Paik
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J. Microbiol. 2010;48(2):249-252. Published online May 1, 2010
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DOI: https://doi.org/10.1007/s12275-009-0176-9
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Abstract
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The anti-HIV-1 activities of butanol, hexane, chloroform and water extracts from four widely used folk medicinal plants (Sophora flavescens, Tulipa edulis, Herba ephedra, and Pachyma hoelen Rumph) were evaluated in this study. The hexane extract of Pachyma hoelen Rumph, PH-4, showed effective inhibition against HIV-1. The 50% effective concentration (EC50) of PH-4 was 37.3 μg/ml in the p24 antigen assay and 36.8% in the HIV-1 recombinant RT activity test (at 200 μg/ml). In addition, the PH-4 showed the protective effect on the infected MT-4 cells, with a 58.2% rate of protection. The 50% cytotoxic concentration (CC50) of PH-4 was 100.6 μg/ml. These results suggest that PH-4 from Pachyma hoelen Rumph might be the candidate for the chemotherapy agent against HIV-1 infection with further study.