Anti-AIDS Agents, 6. Salaspermic Acid, an Anti-HIV Principle from Tripterycium wilfordii, and the Structure-activity Correlation with its Related Compounds

Chen, Ke; Shi, Qian; Kashiwada, Yoshiki; Zhang, De Cheng; Hu, Chun; Jin, Ji Qin; Nozaki, Hirōshi; Kilkuskie, Robert E.; Tramontano, Enzo; Cheng, Yung Chi; McPhail, Donald R.; McPhail, Andrew T.; Lee, Kuo Hsiung̀

doi:10.1021/np50081a010

Cited by 61 publications

(25 citation statements)

References 9 publications

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“…In according to the literature, this PCTT showed anti-HIV activity (Chen et al, 1992). It allows the premise that the activity of this extract should be due to the presence of this compound, that was not tested in this work, or of other substance found in the plant.…”

Section: Resultsmentioning

confidence: 57%

Evaluation of antibacterial activity of "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)

Miranda¹,

Duarte²,

Silva³

et al. 2009

Rev. bras. farmacogn.

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RESUMO: "Avaliação da atividade antibacteriana de "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)". Austroplenckia populnea (Mangabarana) é popularmente utilizada em Minas Gerais, Brasil, para o tratamento de disenterias. A ela também são atribuídas propriedades antitumoral e antiúlcera. Extratos de partes desta planta obtidos com solventes de diferentes polaridades e triterpenos pentacíclicos (TTPCs) isolados destes, por métodos fitoquímicos foram submetidos a testes de atividade antibacteriana. Os resultados mostraram a existência desta atividade e abriram perspectivas para a continuidade dos estudos com outros compostos orgânicos isolados desta planta.Unitermos: Austroplenckia populnea, Celastraceae, atividade antibacteriana, triterpenos pentacíclicos.ABSTRACT: Austroplenckia populnea (Mangabarana) is popularly used by people from Minas Gerais, Brazil for dysenteries diseases treatment. Antitumor and antiulcer activities were also attributed to this plant. Extracts obtained using solvents of different polarities and pentacyclic triterpenes (PCTTs) isolated from these extracts through phytochemical methods were submitted to antibacterial assays. The results showed the existence of this activity and open perspectives for news studies with other organic compounds isolated from this plant.

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Section: Resultsmentioning

confidence: 57%

Evaluation of antibacterial activity of "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)

Miranda¹,

Duarte²,

Silva³

et al. 2009

Rev. bras. farmacogn.

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“…Our previous results indicate that betulinic acid derivatives possess anti-HIV activity (7,15,17,22,28,41). These betulinic acid derivatives can inhibit HIV-1 envelope-mediated membrane fusion at concentrations ranging from 10 to 40 g/ml, which is at least 1,000-fold higher than that required to inhibit viral replication.…”

Section: Resultsmentioning

confidence: 95%

“…Betulinic acid derivatives have been shown to inhibit human immunodeficiency virus type 1 (HIV-1) replication (7,15,17,20,22,28,29,32,34,40,41,43). Dependent upon chemical structure, betulinic acid derivatives have been reported as inhibitors of HIV-1 entry (29,40), HIV-1 protease (43) or reverse transcriptase (RT) (34).…”

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confidence: 99%

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Role of Human Immunodeficiency Virus (HIV) Type 1 Envelope in the Anti-HIV Activity of the Betulinic Acid Derivative IC9564

Holz-Smith

Sun

Jin³

et al. 2001

Antimicrob Agents Chemother

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The betulinic acid derivative IC9564 is a potent anti-human immunodeficiency virus (anti-HIV) compound that can inhibit both HIV primary isolates and laboratory-adapted strains. However, this compound did not affect the replication of simian immunodeficiency virus and respiratory syncytial virus. Results from a syncytium formation assay indicated that IC9564 blocked HIV type 1 (HIV-1) envelope-mediated membrane fusion. Analysis of a chimeric virus derived from exchanging envelope regions between IC9564-sensitive and IC9564-resistant viruses indicated that regions within gp120 and the N-terminal 25 amino acids (fusion domain) of gp41 are key determinants for the drug sensitivity. By developing a drug-resistant mutant from the NL4-3 virus, two mutations were found within the gp120 region and one was found within the gp41 region. The mutations are G237R and R252K in gp120 and R533A in the fusion domain of gp41. The mutations were reintroduced into the NL4-3 envelope and analyzed for their role in IC9564 resistance. Both of the gp120 mutations contributed to the drug sensitivity. On the contrary, the gp41 mutation (R533A) did not appear to affect the IC9564 sensitivity. These results suggest that HIV-1 gp120 plays a key role in the anti-HIV-1 activity of IC9564.

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“…15 The terpenoid saponin actein (17) was identified as the anti-HIV principle by BDFI from the methanol extract of the rhizome of Cimicifuga racemosa, commonly known as black cohosh. Compound 17 exhibited promising antiviral activity with an EC 50 of 0.55 mM and TI of 144.…”

Section: Tetracyclic Triterpenesmentioning

confidence: 99%

New developments in natural products‐based anti‐AIDS research

Morris‐Natschke

Lee

2006

Medicinal Research Reviews

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This review discusses anti-HIV natural products from several compound classes, including terpenoids, coumarins, alkaloids, polyphenols, tannins, and flavonoids. Natural products can provide novel anti-AIDS chemotherapeutic leads that are structurally unique or have new mechanisms of action. The drug discovery and development process proceeds from bioactivity-directed isolation and identification of a promising lead natural product, followed by rational design-based structural modification and structure-activity relationship analyses to optimize the lead compound as a drug candidate. This process is notably exemplified by the discovery of the modified betulinic acid derivative, DSB [PA-457], which is currently in Phase II clinical trial and is the first-in-class HIV maturation inhibitor (MI).

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Anti-AIDS Agents, 6. Salaspermic Acid, an Anti-HIV Principle from Tripterycium wilfordii, and the Structure-activity Correlation with its Related Compounds

Cited by 61 publications

References 9 publications

Evaluation of antibacterial activity of "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)

Evaluation of antibacterial activity of "Mangabarana" Austroplenckia populnea Reissek (Celastraceae)

Role of Human Immunodeficiency Virus (HIV) Type 1 Envelope in the Anti-HIV Activity of the Betulinic Acid Derivative IC9564

New developments in natural products‐based anti‐AIDS research

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