Anti-cancer agents in medicinal chemistry from natural compounds

Cancer could be a general term for a large group of diseases that are affecting the whole body. However, with such a large variety, common characteristic for all of them is fast, rapid, uncontrollable, and genetically different from the rest of the body cell and tissue growth that can expand throughout the body.

By the WHO information, in the year 2020 cancer was accountable for 10 million deaths with the most common being:

  • lung (1.80 mils) 
  • colon and rectum (935 000) 
  • liver (830 000)
  • stomach (769 000)
  • breast (685 000).

Due to this fact, anti-cancer therapy has been a point of high attention for decades. The development of new drug candidates is a very difficult process and some drug developers are looking into nature for extraordinary drug scaffolds and compounds. 

Still by this time, one of the most used anti-cancer treatments is from nature-derived compounds like taxol, doxorubicin, and others. To learn more about natural compound activity against cancer, keep on reading.

Mechanisms of how natural compounds inhibit the development of cancer

Anti-cancer drugs could be divided into several categories:

  • Antimetabolites
  • Antibiotics
  • Alkylating reagents
  • Monoclonal antibodies
  • Steroid hormones and their antagonists
  • Others

Natural compounds that exhibit anti-cancer properties are most commonly put into the first two categories especially in antimetabolites. 

Most commonly natural compounds are tested for their ability to induce several cellular pathways hence being antimetabolite. There have been identified multiple modes of action, how natural compounds are inhibiting growth, spread, and the development of cancer like:

  • Induction of apoptosis
  • Inhibition of angiogenesis
  • Inhibition of metastasis
  • Induction of oxidative stress
  • Cancer cell chemo-sensitization
  • and many more

Induction of apotosis

One of the main mechanisms that have been identified for natural compounds is the induction of apoptosis.

This has been identified as one of the main cellular mechanisms, how many natural compounds like ursolic acid, betulinic acid, resveratrol, phloretin, and many more.

Apoptosis is a nature-designed series of biochemical reactions that eventually lead to cell death and is highly vital in tissue homeostasis.

There are two main signaling pathways and one more minor pathway that induce apoptosis: the death receptor, mitochondria-mediated, and growth factor pathways. These pathways are linked together and can influence each other.

The death receptor pathway (extrinsic) is initiated by the activation of the Fas receptor with an appropriate ligand or tumor necrosis factor interaction with the corresponding receptor. 

Mitochondria-mediated pathways (intrinsic) are activated by the release of cytochrome-c from the intramembrane into the cytosol for the assembly of the apoptosome that promotes caspase-9 activation – the start of the intracellular death.

Inhibition of cell proliferation

There are several mechanisms of how natural compounds are inhibiting the maturation and the development of cells.

Some scientific groups have identified that the natural compound betulin is involved in tumor protein p53 activation – a guardian protein that prevents mutations of the genome. Betulin was able to promote the concentration of p53 and therefore inhibit the maturation of damaged cells.

Natural compound apigenin has been identified to inhibit the growth of pancreatic cancer cells by the suppression of cyclin A and B and phosphorylated forms of csc2 and cdc25 – this induced G2/M phase cell cycle arrest – the damage of intracellular DCN is too difficult to repair.

Other mechanisms

There are other mechanisms as well, that is quite effective to stop the spread of cancer cells.

Scientists have identified that mangiferin is able to inhibit angiogenesis – the formation of new blood vessels. This in fact leads to inhibition of metastasis formation hence inhibiting the spread of cancer throughout the body.

Other compounds like lanosterol are able to chemo-sensitize cancer cells – making them more suspectable hance the treatment more effective from the regular anti-cancer medication.

In conclusion

Indeed, nature is full of various compounds that could be effective against cancer. We could speculate that due to such a large variety, there most probably is a natural compound for almost every type of anti-cancer treatment by being effective via various mechanisms. If you wish to continue this research with high-quality chemicals, visit our products store.