Colchicine Compounds Research Articles

Neutrophils as emerging immunotherapeutic targets: Indirect treatment of tumors by regulating the tumor immune environment based on a sialic acid derivative-modified nanocomplex platform

Tumor cells are dependent on their microenvironment; thus, targeting the non-cancerous components surrounding the tumor may be beneficial. Neutrophils are important inflammatory cells in the tumor microenvironment that significantly affect tumor cell proliferation, metastasis, and immune regulation. Targeted regulation of tumor-associated neutrophil-related pathways is expected to become a new therapeutic approach. Colchicine compounds are powerful anti-inflammatory drugs that strongly inhibit the chemotaxis of neutrophils to the inflammatory site. We attempted to achieve anticancer effects by utilizing its ability to inhibit neutrophil recruitment rather than killing tumor cells. As such drugs are likely to cause non-specific damages due to the lack of selectivity, we synthesized and used sialic acid and cholesterol derivatives (SA-CH) for surface modification of the newly synthesized low-toxic colchicine derivative (BCS) nanocomposite to improve neutrophil targeting. In vivo and in vitro experiments have shown that SA-CH-modified BCS preparations are effectively absorbed by neutrophils, inhibit cell migration, reduce infiltration of tumor-associated neutrophils, enhance T lymphocyte function, and exhibit good anti-S180 early tumor effect. In addition, in a triple-negative breast cancer model, the agent could strongly inhibit tumor metastasis to the lungs.

Thiocolchicoside and Colchicine Induced Apoptosis in Breast Cancer (MCF-7) Cells Via Up-regulated Expression of p53 Tumor Suppressor Protein Gene: An In vitro and In silico Docking Approaches

This study describes the antiproliferative activity of thiocolchicoside and colchicine compounds in a dose-dependent manner against breast cancer cell line (MCF-7). MTT assay results show that IC50 (inhibitory concentration 50 %) values towards MCF-7 breast cancer cell line were 79.02 and 74.23 nmol for thiocolchicoside and colchicines compounds, respectively. Further, in vitro interaction between thiocolchicoside and colchicine compound ligands binding with the p53 tumor suppressor protein gene and its expression was also confirmed by western blot analysis. Results clearly show that the expression of p53 protein was more abundant in treated MCF-7 cancer cell line and up-regulated expression of the p53 gene was positively correlated with thiocolchicoside and cochicine concentrations used. The thiocolchicoside compound was found to be more effective against p53 protein accumulation levels when compared with colchicine and adriamycin. Molecular docking analysis was performed to reveal the interactions of receptor binding sites (molecular targets) with ligands. These compounds show efficient inhibitory action on the target p53 tumor suppressor protein expression which confirms their increased anti-proliferative activity against cancer cell growth. The present results could be used for the improvement of a novel formulation with enhanced inhibition of MCF-7 cancer cell growth. The docking scores were found to be high in thiocolchicoside compound against cellular tumor antigen p53 (-5.9 kcal/mol) with the strong interaction followed by colchicine (-5.3 kcal/mol) and the hydrogen bond counts, confirming the capability of these compounds for binding with receptor active site. Therefore, thiocolchicoside and colchicine compounds with effective p53 inhibitory activity strongly suggest that these compounds could be used as strong anticancer agents to treat MCF-7 breast cancer cell growth arrest effectively.

Size and Density of Artemisia annua Stomata Soaked in Water Extract of Gloriosa superba Seeds

<p class="IsiAbstrakIndo"><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB"> is a herbaceous plant that produces artemisinin as a malaria drug, haemorrhoids therapy, aromatherapy, antiviral, anticancer and antibacterial. </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> is a plant that contains high colchicine compounds, especially on the seeds. </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> extracts of tubers, stems, seeds, and leaves were used as biomutagen for many plants. Colchicine contains of these plants as antimitotic have been studied and proven by the mitotic index plants. Water extracts of </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> seeds was used as a mutagen for </span><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB">. The aim of this study was to determine the size and density of </span><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB"> stomata soaked in water extract of </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> seeds as a mutagen. Extraction of </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> seeds obtained naturally on Krakal Beach, Gunung Kidul by using a maceration method with water solvent (1:1). </span><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB"> sprouts were obtained from B2P2TOOT Tawangmangu. Variables treatment on sprouts using water extract concentration of </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> seeds and soaking time of </span><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB"> sprouts. Measurements of stomatal length, width and density were conducted in epidermis of </span><em><span lang="EN-GB">Artemisia annua</span></em><span lang="EN-GB"> leaf. Observation and measurements of the stomata were conducted by using a light microscope. The results showed that the length and width of stomata were 0.025 mm and 0.017 mm respectively. The stomatal density of the control leaf (174.69 amount/mm2) was lower than the other treated plants. Stomatal size and density has increased with the increasing concentration extracts on treated plants. Water extracts of </span><em><span lang="EN-GB">Gloriosa superba</span></em><span lang="EN-GB"> seeds proved the effects on stomatal size and density of treated plants. </span></p>