Modified ecstasy 'attacks blood cancers'

[toasty]

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

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.

...

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.

...

 

[nabraxas]

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

[woof woof woof]

now modify it to make it less toxic on the brain cells and just as nice as normal mdma + cancer fighting!

ohhhhh yeah! Party your way to good health! ;-)

[toasty]

did you actually read the article?

...

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

...

 

the amount of unmodified ecstasy would have been fatal, they have modified it to be 100x as effective in fighting cancer.

[Thelema]

Enhancing the anti-lymphoma potential of 3,4-methylenedioxymethamphetamine ('ecstasy') through iterative chemical redesign: mechanisms and pathways to cell death.

Wasik AM, Gandy MN, McIldowie M, Holder MJ, Chamba A, Challa A, Lewis KD, Young SP, Scheel-Toellner D, Dyer MJ, Barnes NM, Piggott MJ, Gordon J.

SourceSchool of Immunity & Infection, The Medical School, Birmingham, University of Birmingham, Edgbaston, Birmingham, B15 2TT, UK.

Abstract

While 3,4-methylenedioxymethamphetamine (MDMA/'ecstasy') is cytostatic towards lymphoma cells in vitro, the concentrations required militate against its translation directly to a therapeutic in vivo. The possibility of 'redesigning the designer drug', separating desired anti-lymphoma activity from unwanted psychoactivity and neurotoxicity, was therefore mooted. From an initial analysis of MDMA analogues synthesized with a modified α-substituent, it was found that incorporating a phenyl group increased potency against sensitive, Bcl-2-deplete, Burkitt's lymphoma (BL) cells 10-fold relative to MDMA. From this lead, related analogs were synthesized with the 'best' compounds (containing 1- and 2-naphthyl and para-biphenyl substituents) some 100-fold more potent than MDMA versus the BL target. When assessed against derived lines from a diversity of B-cell tumors MDMA analogues were seen to impact the broad spectrum of malignancy. Expressing a BCL2 transgene in BL cells afforded only scant protection against the analogues and across the malignancies no significant correlation between constitutive Bcl-2 levels and sensitivity to compounds was observed. Bcl-2-deplete cells displayed hallmarks of apoptotic death in response to the analogues while BCL2 overexpressing equivalents died in a caspase-3-independent manner. Despite lymphoma cells expressing monoamine transporters, their pharmacological blockade failed to reverse the anti-lymphoma actions of the analogues studied. Neither did reactive oxygen species account for ensuing cell death. Enhanced cytotoxic performance did however track with predicted lipophilicity amongst the designed compounds. In conclusion, MDMA analogues have been discovered with enhanced cytotoxic efficacy against lymphoma subtypes amongst which high-level Bcl-2-often a barrier to drug performance for this indication-fails to protect.