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Recent Studies and Biological Aspects of Substantial Indole Derivatives with Anti-cancer Activity

Published on Friday, 23 September 2022

Abstract

Background: All cancers are leading causes of morbidity and mortality worldwide. The urgent need for new lead compounds for the treatment of cancer is higher than ever before. Scientists search and try to discover effective but less harmful new anti-tumor agents. Surgery, chemotherapy and radiation are the bestknown methods for treating cancer, however, they continued to be limited. Rising efforts of the scientists toward success of the drug discovery is increasing. Indole ring is considered as a key molecule existing in various biologically active compounds. Indole derivatives are recognized to prevent proliferation and invasion of many cancer cells.

Conclusion: This review presents the existing status and the very recent studies of indoles which have promising activities such as derivatives of indole-3-carbinol, 3,3'-diindolylmethane (DIM), isatin etc. Their chemical and biological behavior as well as a general overview of the anticancer activity is discussed.

NOTE 1: This publication cites DBM (The Di Bella Method) in Di Bella' et al. publications:

Ref #61: Di Bella G. - The Di Bella Method (DBM) improved survival, objective response and performance status in a retrospective observational clinical study on 122 cases of breast cancer. Neuro. Endocrinol. Lett., 2011, 32, 751-762;
Ref #62: Di Bella G., Biagio C. - The Di Bella Method (DBM) improved survival, objective response and performance status in a retrospective observational clinical study on 23 tumors of the head and neck. Neuro. Endocrinol. Lett., 2012, 33, 249-256;

NOTE 2: This publication cites (Ref. N.53): 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 Variable Part - Omega 3 Essential/Unsaturated Fatty Acids. From 1.5 grams up to 3.0 grams per day orally);

- The Di Bella Method (A Fixed Part - All-Trans Retinoic Acid, Analogues and/or Derivatives - Approximately 60mg per day orally: 40mg per day Beta-Carotene/β-Carotene, 10mg per day ATRA and 10mg per day Axerophthol palmitate);

- All-Trans-Retinoic Acid (ATRA - analogues and/or derivatives) - In vitro, review and in vivo publications;

- Solution of retinoids in vitamin E in the Di Bella Method biological multitherapy;

- 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);