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New class of hybrids based on chalcone and melatonin: a promising therapeutic option for the treatment of colorectal cancer

Published on Monday, 19 September 2022

Abstract

Considering that conventional chemotherapy provides only a limited increase of overall survival for patients with colorectal cancer (CRC), and resistance is a major cause of therapeutic failure, the emergence of new therapies is needed.

Development of different compounds is based on molecular hybridization, which constitutes an effective strategy to inhibit cancer cells and overcome cancer drug resistance.

For this purpose, a novel series of chalcone- and melatonin- based hybrids (6a–h) was designed, synthesized, and evaluated for the cytotoxic and antiproliferative effect against SW480 human colon cancer cell line, as well as nonmalignant CHO-K1 cells.

All compounds exerted a strong cytotoxic effect against the malignant cell line, with better results than 5-FU, exhibiting half-maximal inhibitory concentration (IC50) values in the range of 0.24 to 4.14 µM. It is interesting to note that upon 48 h of treatment, hybrid 6f induced a remarkable cytotoxic activity toward SW480 cells (IC50 = 0.26 ± 0.03 μM) with lower effect against nonmalignant cells, as evidenced in the selectivity index (SI = 17.38).

Additionally, combined calculations on drug-like and pharmacokinetics properties suggested that compound 6f has favorable oral absorption and thus it could be a promising candidate for further studies related to cancer therapy.

NOTE: This publication cites (Ref. N.39): Di Bella G., Mascia F., Gualano L., Di Bella L. - Melatonin anticancer effect: review. Int J Mol Sci. 2013;14:2410–2430.

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About this publication.

- The Di Bella Method (A Fixed Part - Melatonin tablets. From 30-40mg/day up to 200mg/day orally in patients with advanced stage of cancer disease and/or patients without respond to traditional treatments);

- Melatonin use in cancer patients have started in 1974, when melatonin prepared according to Prof. Di Bella’s formulation [...]. For 11 days was administered to the patient, admitted to the general medical ward at the Maggiore-Pizzardi Hospital in Bologna, very slowly (over approx. 8 hours) and intravenously administered 1000 mg of melatonin for 11 days. During the course of each day, the patient was intravenously administered 4 saline drips of 500 ml, each containing ten 25 mg bottles of freeze-dried melatonin, lasting 2 hours, totaling 1000 mg per day. No other drug of any kind was administered in order to ascertain the effect of the MLT without interference [...]. From Melatonin with adenosine solubilized in water and stabilized with glycine for oncological treatment - technical preparation, effectivity and clinical findings;

- About Melatonin - In vitro, review and in vivo publications;

- Publication: Melatonin anticancer effects: Review (from Di Bella's Foundation);

- Publication: Key aspects of melatonin physiology: 30 years of research (from Di Bella's Foundation);

- The Di Bella Method (A Fixed Part - Cyclophosphamide 50mg tablets and/or Hydroxyurea 500mg tablets, one or two per day);

- The Di Bella Method (A Variable Part - Selenium methonine, 40 μg capsules, twice a day);

- The Di Bella Method (A Fixed Part - Somatostatin, Octreotide, Sandostatin LAR, analogues and/or derivatives);

- Somatostatin in oncology, the overlooked evidences - In vitro, review and in vivo publications;

- Publication, 2018 Jul: Over-Expression of GH/GHR in Breast Cancer and Oncosuppressor Role of Somatostatin as a Physiological Inhibitor (from Di Bella's Foundation);

- Publication, 2018 Sep: The over-expression of GH/GHR in tumour tissues with respect to healthy ones confirms its oncogenic role and the consequent oncosuppressor role of its physiological inhibitor, somatostatin: a review of the literature (from Di Bella's Foundation);

- Publication, 2019 Aug: The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity (from Di Bella's Foundation);

- Publication, 2019 Sep: Effects of Somatostatin and Vitamin C on the Fatty Acid Profile of Breast Cancer Cell Membranes (from Di Bella's Foundation);

- Publication, 2019 Sep: Effects of somatostatin, curcumin, and quercetin on the fatty acid profile of breast cancer cell membranes (from Di Bella's Foundation);