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Related Concept Videos

Cancer Prevention02:59

Cancer Prevention

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Several factors can increase the risk of cancer in an individual. About 50% of cancer cases can be prevented by adopting a healthy lifestyle, regular exercise, eating healthy, and following a modest cancer prevention diet. Epidemiological studies have consistently shown that populations with vegetable and fruit-rich diets have reduced the incidence of cancer. On the other hand, populations who have a diet rich in animal fat, red meat, junk food, or high calories are predisposed to cancer.
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Combination Therapies and Personalized Medicine02:50

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Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
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Inhibition of Cdk Activity02:34

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

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5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
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Targeted Cancer Therapies02:57

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
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Chirality in Nature02:30

Chirality in Nature

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Chirality is the most intriguing yet essential facet of nature, governing life’s biochemical processes and precision. It can be observed from a snail shell pattern in a macroscopic world to an amino acid, the minutest building block of life. Most of the snails around the world have right-coiled shells because of the intrinsic chirality in their genes. All the amino acids present in the human body exist in an enantiomerically pure state, except for glycine - the sole achiral amino acid.
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Establishment of Hepatocarcinoma in BALB/c-nu Mice and Investigation of the Therapeutic Effect of the Sanleng Jiashen Formula
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Establishment of Hepatocarcinoma in BALB/c-nu Mice and Investigation of the Therapeutic Effect of the Sanleng Jiashen Formula

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Chiral Flavonoids as Antitumor Agents.

Cláudia Pinto1,2, Honorina Cidade1,2, Madalena Pinto1,2

  • 1Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.

Pharmaceuticals (Basel, Switzerland)
|December 28, 2021
PubMed
Summary

Chiral flavonoids, both natural and synthetic, exhibit significant antitumor properties. This review highlights their diverse structures and biological activities, emphasizing the importance of chirality in enhancing anticancer effects.

Keywords:
antitumorchiralenantiomersenantioselective synthesisflavonoids

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Area of Science:

  • Natural Products Chemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Flavonoids are diverse plant compounds with various biological activities, including antioxidant and antitumor effects.
  • Chiral flavonoids, such as flavanones and flavan-3-ols, possess stereogenic centers, and their enantiomers can display differential antitumor activity.
  • Natural flavonoids are often biosynthesized as pure enantiomers but isolated as racemates, necessitating chiral separation for detailed studies.

Purpose of the Study:

  • To provide a comprehensive literature review of natural and synthetic chiral flavonoids with antitumor activity.
  • To highlight the structural diversity and biological significance of chiral flavonoids in cancer research.
  • To underscore the role of chirality in modulating the antitumor efficacy of flavonoid compounds.

Main Methods:

  • Literature search and review of scientific publications on chiral flavonoids and their antitumor activities.
  • Analysis of structural features and biological data of natural and synthetic chiral flavonoids.
  • Compilation of information on enantioselective synthesis and chiral pool approaches for flavonoid development.

Main Results:

  • Chiral flavonoids, both naturally occurring and synthetically derived, demonstrate potent antitumor activities.
  • Enantiomers of chiral flavonoids can exhibit distinct potencies in their anticancer effects.
  • Synthetic strategies, including enantioselective synthesis and chiral pool approaches, have yielded novel chiral flavonoids with enhanced antitumor properties, such as flavopiridol.

Conclusions:

  • Chirality is a critical factor influencing the antitumor activity of flavonoids.
  • The development of synthetic chiral flavonoids offers promising avenues for novel cancer therapeutics.
  • Further research into chiral flavonoids is warranted to fully exploit their potential in cancer treatment.