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Modified ecstasy a potential treatment for cancer

By timkanu, Aug 19, 2011 | Updated: Aug 19, 2011 | | |
Rating:
4/5,
  1. timkanu
    Modified ecstasy 'attacks blood cancers'

    _54669514_000207178-1.jpg

    Ecstasy was already known to kill some cancerous cells, but the doses needed were fatal
    Modified ecstasy could one day have a role to play in fighting some blood cancers, according to scientists.


    Ecstasy is known to kill some cancer cells, but scientists have increased its effectiveness 100-fold, they said in Investigational New Drugs journal.
    Their early study showed all leukaemia, lymphoma and myeloma cells could be killed in a test tube, but any treatment would be a decade away.

    A charity said the findings were a "significant step forward".
    In 2006, a research team at the University of Birmingham showed that ecstasy and anti-depressants such as Prozac had the potential to stop cancers growing.
    The problem was that it needed doses so high they would have been fatal if given to people.

    The researchers, in collaboration with the University of Western Australia, have chemically re-engineered ecstasy by taking some atoms away and putting new ones in their place.

    One variant increased cancer-fighting effectiveness 100-fold. It means that if 100g of un-modified ecstasy was needed to get the desired effect, only 1g of the modified ecstasy would be needed to have the same effect. Scientists say this also reduced the toxic effect on the brain.

    Lead researcher Professor John Gordon, from the University of Birmingham, told the BBC: "Against the cancers, particularly the leukaemia, the lymphoma and the myeloma, where we've tested these new compounds we can wipe out 100% of the cancer cells in some cases.

    Tweaking the structure of ecstasy has made it more effective in attacking some cancers.
    "We would really need to pinpoint which are the most sensitive cases, but it has the potential to wipe out all the cancer cells in those examples.
    "This is in the test tube, it could be different in the patient, but for now it's quite exciting."

    'Soapy' cells It is believed that the drug is attracted to the fat in the membranes of the cancerous cells.
    Researchers think it makes the cells "a bit more soapy", which can break down the membrane and kill the cell.
    They said cancerous cells were more susceptible than normal, healthy ones.

    However, doctors are not going to start prescribing modified ecstasy to cancer patients in the near future.
    The research has been demonstrated only in samples in a test tube. Animals studies and clinical trials would be needed before prescribing a drug could be considered.

    First, however, chemists in the UK and Australia are going to try to tweak the modified ecstasy even further as they think it can be made even more potent.

    'Genuinely exciting' If everything is successful, a drug is still at least a decade away.
    Dr David Grant, scientific director of the charity Leukaemia and Lymphoma Research, said: "The prospect of being able to target blood cancer with a drug derived from ecstasy is a genuinely exciting proposition.

    "Many types of lymphoma remain hard to treat and non-toxic drugs which are both effective and have few side effects are desperately needed.
    "Further work is required but this research is a significant step forward in developing a potential new cancer drug."

    http://www.bbc.co.uk/news/health-14572284

Comments

  1. zodd. man.
    [​IMG] A modified version of the drug MDMA - also known as ecstasy - could be used in the future to treat some blood cancers, scientists claim.
    Scientists at the University of Birmingham say the modified ecstasy is 100 times more effective at attacking and killing cancerous cells than MDMA alone, and could potentially be used to treat blood cancers such as leukaemia, lymphoma and myeloma.
    Six years ago, the same team of scientists discovered that more than half of the white blood cell cancers they looked at responded to psychotropic drugs in laboratory experiments.
    These included amphetamine derivatives such as ecstasy and weight-loss pills, and antidepressants such as fluoxetine (Prozac).
    But the concentration of MDMA needed to treat a cancerous tumour would have been fatal to the patient.
    Now the Birmingham scientists, along with researchers from the University of Western Australia, have "redesigned the designer drug," and developed a more potent compound.
    The researchers also think they may have discovered how the drug works.
    It appears to be attracted to the fatty molecules in the cell membrane - lipids - so the cell becomes "more soapy," making it easier for the drug to get into the cell. Normal healthy cells are more resistant to this action.
    Further work could lead to MDMA-derivatives being used in patient trials, they said.
    Professor John Gordon, from the University of Birmingham’s School of Immunology and Infection, said: "This is an exciting next step towards using a modified form of MDMA to help people suffering from blood cancer.
    "While we would not wish to give people false hope, the results of this research hold the potential for improvement in treatments in years to come."
    Dr David Grant, Scientific Director of the charity Leukaemia & Lymphoma Research, which helped fund the study, said: "The prospect of being able to target blood cancer with a drug derived from ecstasy is a genuinely exciting proposition.
    "Many types of lymphoma remain hard to treat and non-toxic drugs which are both effective and have few side effects are desperately needed. Further work is required but this research is a significant step forward in developing a potential new cancer drug."
    The study is published in the journal Investigational New Drugs.
  2. cyferman
    i wonder what the effect of this soapyness of cells would mean to a healthy person? would it make them more vulnerable to cancers forming aswell? I cant seem to find any information on the specific analogue of E either
  3. Synaps
    I wonder if this drug would, in addition to its anti-cancerous effects, also retain the empathogenic qualities of the drug it derived from. I reckon 'rolling through cancer therapy would make the process considerably easier.
  4. Phenoxide
    While the candidate drug molecules they've created share the general skeleton of phenethylamines and the characteristic methylenedioxyphenyl ring found in MDMA, MDA and methylone, the amine moiety itself is replaced with other groups. Losing the amine would be expected to cause a pretty substantial drop in psychoactive potential. As the BBC article suggests they've had to try and engineer the molecule to retain the anti-tumorogenic properties but lose the psychoactivity to prevent injury by overstimulation at therapeutic doses. Effectively they've taken out the fun and turned it into an effective toxin.

    It's a very interesting observation that the tumor cells are more vulnerable to non-polar substances with structures like this. Hopefully this will lead to development of further candidate drugs, some of which may be of psychoactive interest. This is good news to hear though. It can only be good for the reputation of the phenethylamine family for them to be finding their way into new branches of biomedical research.
  5. Euphoric
    Modified ecstasy 'attacks blood cancers'

    Ecstasy Ecstasy was already known to kill some cancerous cells, but the doses needed were fatal

    Modified ecstasy could one day have a role to play in fighting some blood cancers, according to scientists.

    Ecstasy is known to kill some cancer cells, but scientists have increased its effectiveness 100-fold, they said in Investigational New Drugs journal.

    Their early study showed all leukaemia, lymphoma and myeloma cells could be killed in a test tube, but any treatment would be a decade away.

    A charity said the findings were a "significant step forward".

    In 2006, a research team at the University of Birmingham showed that ecstasy and anti-depressants such as Prozac had the potential to stop cancers growing.

    The problem was that it needed doses so high they would have been fatal if given to people.

    The researchers, in collaboration with the University of Western Australia, have chemically re-engineered ecstasy by taking some atoms away and putting new ones in their place.

    One variant increased cancer-fighting effectiveness 100-fold. It means that if 100g of un-modified ecstasy was needed to get the desired effect, only 1g of the modified ecstasy would be needed to have the same effect.

    Scientists say this also reduced the toxic effect on the brain.

    Lead researcher Professor John Gordon, from the University of Birmingham, told the BBC: "Against the cancers, particularly the leukaemia, the lymphoma and the myeloma, where we've tested these new compounds we can wipe out 100% of the cancer cells in some cases.
    A molecule of ecstasy Tweaking the structure of ecstasy has made it more effective in attacking some cancers.

    "We would really need to pinpoint which are the most sensitive cases, but it has the potential to wipe out all the cancer cells in those examples.

    "This is in the test tube, it could be different in the patient, but for now it's quite exciting."
    'Soapy' cells

    It is believed that the drug is attracted to the fat in the membranes of the cancerous cells.

    Researchers think it makes the cells "a bit more soapy", which can break down the membrane and kill the cell.

    They said cancerous cells were more susceptible than normal, healthy ones.

    However, doctors are not going to start prescribing modified ecstasy to cancer patients in the near future.

    The research has been demonstrated only in samples in a test tube. Animals studies and clinical trials would be needed before prescribing a drug could be considered.

    First, however, chemists in the UK and Australia are going to try to tweak the modified ecstasy even further as they think it can be made even more potent.
    'Genuinely exciting'

    If everything is successful, a drug is still at least a decade away.

    Dr David Grant, scientific director of the charity Leukaemia and Lymphoma Research, said: "The prospect of being able to target blood cancer with a drug derived from ecstasy is a genuinely exciting proposition.

    "Many types of lymphoma remain hard to treat and non-toxic drugs which are both effective and have few side effects are desperately needed.

    "Further work is required but this research is a significant step forward in developing a potential new cancer drug."

    By James Gallagher Health reporter, BBC News

    18 August 2011

    http://www.bbc.co.uk/news/health-14572284
  6. cyferman
    its funny that in the bbc news broadcast it says something like "many modern pharmaseuticals have roots from current illegal drugs" (also spoken in the positively toned drone) almost giving someone a [generally misinformed] reason to challenge the view that "Drugs'rr bad Nmmkay".
  7. jon-q
  8. venkecske
    A predecessor paper, originally published over a year ago, has been uploaded. Interestingly, the media did not picked it up then. Representative structures are shown below:
  9. godztear
    Re: Modified ecstasy 'attacks blood cancers'

    Its a shame that they make no mention of the actual drug that is being modified considering the many possibilities that ecstasy could be.
  10. timkanu
    Re: Modified ecstasy 'attacks blood cancers'


    I know its a bit silly. But Joe public are treated like fools and "ecstasy" makes for a more sensational headline in the eyes of the writers unfortunately.

    They do definatly mean MDMA though.


    "The team from Birmingham has been working with researchers from the University of Western Australia who produced the new compounds for them.
    Lead author Professor John Gordon said: "Together, we were looking at structures of compounds that were more effective.
    "They started to look more lipophilic, that is, they were attracted to the lipids that make up cell walls. This would make them more 'soapy' so they would end up getting into the cancer cells more easily and possibly even start dissolving them.
    He added: "This is an exciting next step towards using a modified form of MDMA to help people suffering from blood cancer."

    http://news.sky.com/home/uk-news/article/16052448
  11. enquirewithin
    A TEAM of UWA researchers have found they may be able to alter the club drugecstasy’ to kill certain types of blood cancers at the same time boosting the potency and reducing the psychoactivity.

    PhD student Michael Gandy, who worked on the project and Associate Professor Matthew Piggot. Image: Bob Blucat School of Biomedical, Biomolecular and Chemical Sciences Associate Professor Matthew Piggott says when the UWA team was researching the use of methylenedioxymethamphetamine (MDMA) in Parkinson’s disease drug discovery, they came across a paper suggesting it may also be useful in treating blood cancer.

    So the UWA scientists collaborated with University of Birmingham Professor John Gordon and his team to increase the toxicity of the drug toward blood cancer cell lines, while decreasing its psychoactive effects.
    While MDMA was never marketed as a therapeutic drug, it was discovered as a ‘party drug’ in the late 70s and early 80s mainly due to its ability to induce euphoria. Now, A/Prof Piggott says MDMA’s structure can be “tinkered with” with to create MDMA analogues (compounds structurally similar to MDMA) that could have improved therapeutic properties

    “Professor Gordon found MDMA to be weakly toxic to certain types of blood cancer cell lines, so he presented the idea of ‘redesigning the designer drug’,” he says. “We contacted him and he was very keen to test our analogues—initially created for Parkinson’s disease treatment research—on his cell lines. “That’s how it started.”

    In order to make the analogues suitable for treatment, the team must focus on removing the psychoactive effect while boosting the toxicity to cancer cells. To do this, the researchers change some ‘substituents’, particularly the alpha-substituent, in the analogues, much like removing or adding building blocks. The altered structure modifies the biological properties. “We had some limited anecdotal evidence...because of the work of maverick chemist Alexander Shulgin, who would make different compounds and test them out on himself and his friends,” A/Prof Piggott says. In terms of increasing its potency against blood cancer cells lines, A/Prof Piggott says it involves “logical trial and error”.

    “Initially six compounds were screened but most were not very active. However, there was one that was ten times more potent, and this became the basis for the next batch of analogues,” he says. “We are currently at the process of making analogues of the best ‘lead’ compound we have discovered so far—which is 100-fold more potent.”

    A/Prof Piggott says the compounds are being evaluated using in vitro cell lines, but the next step would be testing them in an animal model of blood cancer.

    ________________

    A comment posted might be of interest:

    If you actually read the paper, there is no control against normal cells!! Also the IC50 of the best compound is around 10 micromoles per litre. To achieve any 'real' benefit the concentration would have to better than this. But this is all after 'logical trial and error'....not too logical and real drug design does not take such a weak approach. There are far better compounds available that have a far great poyency than these compounds and do not have the dangerous side effects that molecules like these do.

    ---------------------

    Ecstasy derivative targets blood cancers
    http://www.sciencewa.net.au/3653-ecstasy-derivative-targets-blood-cancers.html

    The reference to Sasha Schulgin is intersting....
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