Article ; Online: Anthocyanins, delphinidin-3-O-glucoside and cyanidin-3-O-glucoside, inhibit immune checkpoints in human colorectal cancer cells in vitro and in silico.
2019 Volume 9, Issue 1, Page(s) 11560
Abstract: The objective was to assess anti-progression and stimulatory immune response effects among anthocyanins (ANC) and their metabolites on human colorectal cancer cells in vitro and in silico. Pure phenolics including delphinidin-3-O-glucoside (D3G) and its ... ...
| Abstract | The objective was to assess anti-progression and stimulatory immune response effects among anthocyanins (ANC) and their metabolites on human colorectal cancer cells in vitro and in silico. Pure phenolics including delphinidin-3-O-glucoside (D3G) and its metabolites, delphinidin (DC) and gallic acid (GA), were tested alone or in combination, on HCT-116 and HT-29 human colorectal cancer cells (100-600 µg/mL). HCT-116 and HT-29 50% inhibition concentrations (µg/mL) were 396 ± 23 and 329 ± 17 for D3G; 242 ± 16 and >600 for DC; and 154 ± 5 and 81 ± 5 for GA, respectively. Using molecular docking, cyanidin-3-O-glucoside (C3G) showed the highest potential to inhibit immune checkpoints: programmed cell death protein-1 (PD-1) (-6.8 kcal/mol) and programmed death-ligand-1 (PD-L1) (-9.6 kcal/mol). C3G, D3G, DC, GA, and D3G-rich extracts decreased PD-L1 protein expression in HCT-116 cells. C3G decreased PD-L1 fluorescence intensity by 39%. ANC decreased PD-1 expression in peripheral blood mononuclear cells in monoculture by 41% and 55%, and co-culture with HCT-116 and HT-29 cells by 39% and 26% (C3G) and 50% and 51% (D3G), respectively. D3G and C3G, abundant in plant foods, showed potential for binding with and inhibiting immune checkpoints, PD-1 and PD-L1, which can activate immune response in the tumor microenvironment and induce cancer cell death. |
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| MeSH term(s) | Adjuvants, Immunologic/chemistry ; Adjuvants, Immunologic/pharmacology ; Anthocyanins/chemistry ; Anthocyanins/pharmacology ; Antineoplastic Agents, Immunological/chemistry ; Antineoplastic Agents, Immunological/pharmacology ; Cell Survival/drug effects ; Colorectal Neoplasms/drug therapy ; Colorectal Neoplasms/immunology ; Glucosides/chemistry ; Glucosides/pharmacology ; HCT116 Cells ; HT29 Cells ; Humans ; Tumor Microenvironment/drug effects |
| Chemical Substances | Adjuvants, Immunologic ; Anthocyanins ; Antineoplastic Agents, Immunological ; Glucosides ; cyanidin-3-O-beta-glucopyranoside ; delphinidin (EM6MD4AEHE) |
| Language | English |
| Publishing date | 2019-08-09 |
| Publishing country | England |
| Document type | Journal Article ; Research Support, U.S. Gov't, Non-P.H.S. |
| ZDB-ID | 2615211-3 |
| ISSN | 2045-2322 ; 2045-2322 |
| ISSN (online) | 2045-2322 |
| ISSN | 2045-2322 |
| DOI | 10.1038/s41598-019-47903-0 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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