Interesting that I have never heard of this. Has your doctor? Looks like lots of research needed on this. I would expect the ASA, NSA and WSO to start up clinical trials in a year. Hell no, they won't do a damn thing about this news.
http://www.alphagalileo.org/ViewItem.aspx?ItemId=153700&CultureCode=en
Chemists at The Scripps Research Institute (TSRI) have invented the
first practical, scalable method for synthesizing jiadifenolide, a
plant-derived molecule that may have powerful brain-protecting
properties.
Finding a good way to synthesize jiadifenolide has been a goal of
chemists around the world since the compound was discovered in 2009.
Preliminary studies have hinted that it might be useful in protecting
brain cells from neurodegenerative diseases such as Alzheimer’s and
perhaps other neurological conditions including stroke and traumatic
brain injury. But it is very difficult to obtain useful quantities of
jiadifenolide from plants, and the synthesis methods reported in the
past few years also have low yields.
“Prior synthetic routes to jiadifenolide yield a few milligrams,
suitable mainly for cell-culture experiments, but with our new method
someone could make the gram to kilogram quantities needed for tests in
animals and humans,” said Ryan A. Shenvi, associate professor at TSRI.
The feat by Shenvi and his team, described in an Advance Online
Publication in Nature Chemistry on June 15, 2015, may therefore lead to
the development, years from now, of a jiadifenolide-derived drug.
The achievement also demonstrates the increasing power of synthetic
chemistry to produce the potentially valuable molecules found in nature
on large scale at low cost.
“There are more and more examples these days of syntheses that start
with cheap, readily available chemicals and assemble them into complex
and valuable molecules on a meaningful scale—much more efficiently than
if you tried to isolate the molecules from nature or produce them in
genetically engineered organisms,” said Shenvi.
A Tantalizing Target
Jiadifenolide is found in trace quantities in the fruit of the star
anise-related shrub Illicium jiadifengpi, which grows in southern China.
It and other Illicium plants have long featured in Chinese traditional
medicine. Most parts of I. jiadifengpi are poisonous if eaten, but root
extracts applied to the skin have been used to treat arthritis.
In 2009, a team of Japanese and Chinese scientists reported isolating
tiny quantities of jiadifenolide from I. jiadifengpi. They determined
that the compound, unlike many others from the plant, is not toxic, and
indeed strongly promotes the growth of axons and dendrites (output and
input branches) from rat neurons in a culture dish. Subsequent research
has suggested that jiadifenolide works by enhancing the activity of
natural brain growth factors, known as neurotrophins.
“Neurotrophin levels are depressed in diseases like Alzheimer’s, so
researchers have long sought compounds that behave like neurotrophins or
that amplify their activity, especially those that could be taken in a
pill,” said Shenvi.
Neurotrophins themselves are large molecules that effectively can’t
be used as drugs, because they are rapidly broken down by enzymes in the
digestive tract and bloodstream and also don’t cross the blood-brain
barrier easily. Jiadifenolide by contrast is a small molecule, and thus
has more potential to be developed into an oral drug.
‘A Completely Different Approach’
Shenvi’s laboratory took up the jiadifenolide synthesis challenge a
few years after the first, low-yield method was reported in 2011. “While
we worked on this, two other groups reported their own synthetic
routes, which pushed us to find a completely different approach,” said
Hai-Hua Lu, a research associate in the Shenvi laboratory who was lead
author of the new study.
The new, eight-step synthesis involves merging two simple molecules,
called butenolides, via a process called the Michael reaction—in fact, a
double Michael reaction—to make a compound very close to jiadifenolide
itself.
“It’s a chemical reaction that few people (myself included) would have confidently predicted to work,” Shenvi said.
“After we figured out how to do that, though, the rest was much
easier, and we found we could obtain more than a gram from one batch,”
said Lu.
Now that jiadifenolide can be produced in sufficient quantities,
Shenvi is looking for companies that can help with further studies of
the compound, including tests in animal models of neurodegenerative
diseases.
Shenvi also suspects that the new method can be adapted for the
practical synthesis of related trace compounds found in Illicium plants.
He admits, though, that it is not just the therapeutic potential of
this plant metabolite that has attracted him and other synthetic
chemists.
“The peculiar geometry of jiadofenolide lends it a certain beauty,
like a geodesic dome or a mosaic tessellation. It’s the combination of
structural beauty, chemical challenge and therapeutic potential that has
stimulated so much interest,” he said.
The other author of the paper, “An eight-step gram-scale synthesis of
(−)-jiadifenolide,” was National Science Foundation (NSF) pre-doctoral
fellow Michael D. Martinez, a second-year graduate student in the Shenvi
laboratory. “Many related Illicium sesquiterpenes also demonstrate
neurotrophic properties and share a common structural core with
(-)-jiadifenolide. Our route to access (-)-jiadifenolide may provide
inroads to these related natural products and analogues.”
The research was funded in part by the NSF (DGE-1346837), as well as
Amgen, Boehringer Ingelheim, the Baxter Foundation, Bristol-Myers
Squibb, Eli Lilly, Novartis and the Sloan Foundation.
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