Chemical Composition and Cytotoxic Activity of the Fractionated Trunk Bark Essential Oil from Tetraclinis articulata (Vahl) Mast. Growing in Tunisia

The aim of the present research was to determine the chemical composition and the cytotoxic effects of Tetraclinis articulata trunk bark essential oil (HEE) obtained by steam distillation and five fractions obtained by normal phase silica chromatographic separation. Chemical analysis allowed the identification of 54 known compounds. Relatively high amounts of oxygenated sesquiterpenes (44.4–70.2%) were detected, mainly consisting of caryophyllene oxide (13.1–26.6%), carotol (9.2–21.2%),14-hydroxy-9-epi-(E)-caryophyllene (3.2–15.5%) and humulene epoxide II (2.6–7.2%). The cytotoxic activity against human mammary carcinoma cell lines (MDA-MB-231) and colorectal carcinoma cell lines (SW620) of the essential oil and its fractions were assessed. All the samples displayed moderate to weak activity compared to 5-fluorouracil. The colorectal carcinoma cell line was relatively more sensitive to the essential oil and its fractions compared to the breast cancer cell line, showing IC50 values from 25.7 to 96.5 μg/mL. In addition, the essential oil and its fraction E.2 revealed a cytotoxic activity against colorectal carcinoma cell line, with IC50 values lower than 30 μg/mL. This is the first report on the chemical composition and cytotoxic activity of the trunk bark essential oil of T. articulata.

The Identification of a Novel Unsymmetrical Azine as an Apoptosis Inducer in Colorectal Cancer

Background: Defects in the physiological mechanisms of apoptosis are one of the pivotal factors implicated in carcinogenesis. Thus, the development of novel compounds that target various apoptotic pathways has provided promising anticancer therapeutic opportunities. Objective: This study explores the cytotoxic effects of a novel unsymmetrical azine against specific cancer cell lines and investigates the mechanism of cytotoxicity. Methods: Molecular modeling was used to test the binding affinity of four new unsymmetrical azines to a model of an apoptosis inhibitor protein (XIAP). The compound with the highest binding affinity, C4, was further tested on different cell lines. Real-time polymerase chain reaction (PCR) and transmission electron microscope (TEM) were used to study apoptosis induction biochemically and morphologically. Results: In comparison to cisplatin as a control, the compound C4 exhibited notable cytotoxicity against all tested cancer cell lines, especially the human colorectal carcinoma cell line (HCT-116). Furthermore, C4-treated cells demonstrated marked overexpression of the pro-apoptotic proteins Bax and caspase-3 as well as the tumor suppressor p53. On the other hand, the expression of the anti-apoptotic protein Bcl-2 was inhibited. On TEM examination, C4-treated HCT-116 cells showed classical structural signs of apoptosis. Conclusion: This study identifies a novel azine (C4) which induces remarkable cytotoxicity against colorectal carcinoma cell line, mediated through apoptosis induction. These novel insights suggest C4 as a promising therapeutic agent in colorectal cancer.

Synthesis of New Pt(II) Complex Bearing Organoselenium Ligands and Evaluation of Cytotoxic Activity of Some Structurally Related Pd(II) Complexes

Herein we report the synthesis of new trans-bis(2-phenylselenylmethyl)oxolane)dichloroplatinum(II) complex Pt1. Newly synthetized complex, together with two, structurally related trans-Pd(II) complexes (trans-bis(2-(phenylselenylmethyl)oxolane)dichloropalladium(II) Pd1 and trans-bis(2-(phenylselenylmethyl)oxane)dichloropalladium(II)) Pd2, were screened for cytotoxic activity through in vitro study on the HCT-116 colorectal carcinoma cell line and on the MRC-5 healthy lung pleura cell line. Activity of complexes was assessed by comparing it to the cisplatin. The cells viability and proliferation were determined using MTT assay.