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Anti-HIV, antitumor and immunomodulatory activities of paclitaxel from fermentation broth using molecular imprinting technique.

ABSTRACT: In this study, a single component paclitaxel was obtained from fermentation broth by molecular imprinting technique, and its antiviral, antitumor and immunomodulatory activities were studied. The results showed that paclitaxel had a good inhibitory activity on human breast cancer MCF-7 cells and showed a concentration- dependent relationship with an IC50 of about 15 μg/mL in the sulforhodamine B assay. At the same time, paclitaxel exerted a weak inhibitory activity on cervical cancer Hela cells. In addition, paclitaxel not only inhibited the invasion of HIV-1 pseudovirus into cells, but also exhibited inhibitory activity to a certain extent after viral invasion of the cells. At a paclitaxel concentration of 20 μg/mL, the inhibition of HIV-1 pseudovirus reached about 66%. The inhibition of HIV-1 protease activity was concentration-dependent. At a concentration of 20 μg/mL, the inhibitory effect of paclitaxel on HIV-1 protease was similar to that of the positive control pepstatin A, being 15.8%. The HIV-1 integrase inhibiting activity of paclitaxel was relatively weak. Paclitaxel significantly up-regulated the expression of interleukin-6.

SUBMITTER: Ryang J

PROVIDER: S-EPMC6890922 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Anti-HIV, antitumor and immunomodulatory activities of paclitaxel from fermentation broth using molecular imprinting technique.

Ryang Junhyok J Yan Yan Y Song Yangyang Y Liu Fang F Ng Tzi Bun TB

AMB Express 20191203 1

In this study, a single component paclitaxel was obtained from fermentation broth by molecular imprinting technique, and its antiviral, antitumor and immunomodulatory activities were studied. The results showed that paclitaxel had a good inhibitory activity on human breast cancer MCF-7 cells and showed a concentration- dependent relationship with an IC50 of about 15 μg/mL in the sulforhodamine B assay. At the same time, paclitaxel exerted a weak inhibitory activity on cervical cancer Hela cells. ...[more]

PMID: 31797089

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Project description:Melanoma is the most aggressive and lethal type of skin cancer, responsible for approximately 60,000 deaths annually. The main strategy for treating melanoma is surgery to completely remove the lesion and its margins. However, for more advanced cases with a high recurrence rate, the preferred approach is to combine chemotherapy with immunotherapy treatments. Tumor-associated macrophages (TAMs) are the most abundant leukocytes in solid tumors. Current immunotherapy approaches target TAMs by inhibiting pro-tumoral TAMs and activating anti-tumoral TAMs, repolarizing them to the M1 phenotype. The antitumor and immunomodulatory activities of molecules derived from 1,2,4-oxadiazole, as demonstrated in the literature, highlight the potential of this class as a source of promising candidates for therapeutic applications. Thus, the present study aims to evaluate the antitumor and immunomodulatory effects of the synthetic derivative 1,2,4-oxadiazole, N-cyclohexyl-3-(3-methylphenyl)-1,2,4-oxadiazole-5-amine (1,2,4-oxadiazole derivative 2), in melanoma cells and murine Bone Marrow-Derived Macrophages (BMDMs). Cytotoxicity in B16-F10 and BMDMs cells was assessed using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) MTT method. 1,2,4-oxadiazole derivative 2 exhibited antiproliferative effects on both cell lines, being 2.6 times more selective for B16-F10. Necrosis was identified as the active induced death pathway. BMDMs isolated and exposed to 1,2,4-oxadiazole derivative 2 polarize to the M1 phenotype and induce TNF-α at a concentration of 64.34 μM. Exposure to melanoma murine supernatants also promotes M1 polarization. Supernatants containing traces of 1,2,4-oxadiazole derivative 2 (Supernatants B, C, and D) increased the percentage of M1 cells compared to Supernatant A, as well as elevated levels of nitrite, TNF-α, and IL-12. 1,2,4-oxadiazole derivative 2 combined with Supernatant A and 1,2,4-oxadiazole derivative 2 combined with LPS also resulted in higher M1 polarization, suggesting a synergistic effect on M1 polarization and TNF-α production. Our findings underscore the significance of the 1,2,4-oxadiazole compound class and highlight the potential of 1,2,4-oxadiazole derivative 2 as an antitumoral and immunotherapeutic agent.

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Anti-HIV, antitumor and immunomodulatory activities of paclitaxel from fermentation broth using molecular imprinting technique.

Publications

Anti-HIV, antitumor and immunomodulatory activities of paclitaxel from fermentation broth using molecular imprinting technique.

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