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Acriflavine - Cancer Treatment Potential

Updated on November 9, 2009

What is Acriflavine

Acriflavine (akri-flàv-een) was synthesized in 1912 by Dr. Paul Ehrlich, a German medical researcher and was used as a treatment for sleeping sickness.

Lately it has been used as a topical antiseptic much like Betadine. It has the form of an orange or brown powder which can be mixed with sterile water to create a topical wash.

It is a dye used to clean the skin. It can stain the skin and may irritate the eyes and mucus membranes.

Please note that penicillin, one of a class of antibiotics called Beta-lactam antibiotics, was not discovered until 1928.

Dr. Paul Ehrlich
Dr. Paul Ehrlich

Dr. Paul Ehrlich

Dr. Ehrlich spent a considerable portion of his life studying dyes and how they could be used to make microscopic examination of formerly invisible microbes possible. In the process he discovered that some of the dyes actually had therapeutic effect on disease. Notably sleeping sickness, diphtheria and syphilis. Dr. Eherlich, also being a top notch chemist, knew that if some of the compounds he discovered were too toxic for human use, he could modify the molecule, come up with variants of these compounds, and create a much less toxic drug.

When therapeutic quantities of acriflavine were successfully used to treat sleeping sickness it was noted that those levels were also toxic. Dr. Ehrlich went on to develop Arsphenamine which is similar in structure to acriflavine, but much less toxic. This compound was later used to treat the three diseases above with less toxic side-effects. Arsphenamine was also known as 606 as it was the six hundred and sixth compound Ehrlich and his team developed in an attempt to find a drug that was simultaneously deadly to bacteria and only mildly toxic to humans.

Dr. Ehrlich's claim to fame is that he was the first immunologist to take on and tackle Diphtheria with a serum. He also coined the terms "chemotherapy" and "magic bullet."


Cancer Treatment

Acriflavine has now been found to inhibit the growth of new blood vessels (angiogenesis) feeding cancerous cells. This discovery was made by Johns Hopkins University School of Medicine.

Rodent Studies
Mice who are designed to develop cancer showed no new or existing tumor growth when they were injected with acriflavine daily. Apparently acriflavine disables the function of a protein called HIF-1. This protein is key player in new blood vessel formation.

"Mechanistically, this is the first drug of its kind," said Jun Liu, "It is acting in a way that is never seen for this family of proteins."

Researchers at Johns Hopkins continue to explore new uses for old drugs in the school's expansive drug library.

Johns Hopkins School of Medicine (JHSM) Research
This discovery of the effect of acriflavine on cancer growth was made quite by accident as researchers at JHSM will go through it's vast library of three thousand (3,000+) plus drugs.

"As cancer cells rapidly divide, they consume considerable amounts of oxygen. To continue growing, a tumour must create new blood vessels to deliver oxygen to the tumour cells," said Dr. Gregg Semenza.

Acriflavine has been found to interfere with the function of a protein called hypoxia-inducible factor (HIF)-1. This protein was discovered by Semenza's team in 1992. It is thought that when HIF-1 "senses" a low oxygen level in surrounding tissue, it can turn on the genes required for blood vessel development. HIF-1 has also been found to be essential to normal tissue growth and wound repair, but it can also be "turned on" by cancers demanding oxygen for growth.

Once the protein for blood vessel development was identified the Johns Hopkins team then went through their 3000+ drug library to see what might affect the protein.

They were astonished to find that such an old drug could bind to the protein and disable it.


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  • LiamBean profile image

    LiamBean 7 years ago from Los Angeles, Calilfornia

    I have another hub about Accutane which is used to treat acne. I mention thalidomide in that one as Accutane and Thalidomide are the only two drugs with as many restrictions on them that are still on the market.

  • profile image

    jrb 7 years ago

    Facinating. Another drug which was from 1957-1961 and was banned it was found to cause birth defects in infants is Thalidomide. It also has the ability to restrict the development of new blood vessles, which is exactly why it was causing birth defects in pregnant women.