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Information on
Graviola
Graviola is a small, upright evergreen tree growing 5 to 6
meters in height with large dark green and glossy leaves. It is
indigenous to most of the warmest tropical areas in South and
North America including the Amazon. It produces a large
heart-shaped edible fruit that is 6-9", yellow green in color,
with white flesh. The fruit is sold in local markets in the
tropics where it is called Guanabana or Brazilian Cherimoya and
is excellent for making drinks and sherbets and, though slightly
sour-acid, can be eaten out-of-hand.
In an 1976 plant
screening program by the National Cancer Institute, the leaves
and stem of Graviola showed active cytotoxicity against cancer
cells and researchers have been following up on this research
ever since. Much of the research on Graviola focuses on a novel
set of phytochemicals called annonaceous acetogenins. The
potent antitumor, pesticidal and/or insect antifeedant
properties of these annonaceous acetogenins have been reported
and patented. Graviola produces these natural compounds in leaf,
bark and twig tissues, and they have be documented to possess
both highly anti-tumor and pesticidal properties. Mode of action
studies in three separate laboratories have recently determined
that acetogenins are superb inhibitors of Complex I in
mitochondrial electron transport systems from several organisms
including tumors. Research on various Annona species of plants
has yielded many extremely potent acetogenins. Many of them have
cytotoxicity with ED50 values as low as 10-9 ug/ml. Active
compounds from Graviola and other Annona plants have been
submitted to the NIH anti-AIDS screen by Purdue University and
their work is continuing with a number of other active plant
species in the Annona plant family. Thus far, Purdue and/or it's
staff have filed at least 9 U.S. and/or international patents on
their work around the antitumorous and insecticidal properties
and uses of these acetogenins. Three separate research groups
have isolated novel compounds in the seeds and leaves of
Graviola which have demonstrated significant anti-tumorous,
anticancerous and selective toxicity against various types of
cancer cells, publishing 8 clinical studies on their findings.
One study demonstrated that an acetogenin in Graviola was
selectively cytotoxic to colon adenocarcinoma cells in which it
was 10,000 times the potency of adriamycin (a chemotherapy
drug). Cancer research is ongoing on Graviola, and four new
studies have been published in 1998 which further narrow down
the specific phytochemicals which are demonstrating the
strongest anticancerous and antiviral properties.
Annonaceous
acetogenins are only found in the Annonaceae family. In general,
various annonaceous acetogenins have been documented with
antitumor, antiparasitic, pesticidal, antiprotozoal, antifeedant,
anthelmintic, and antimicrobial activities. There has been much
interest in the chemicals which have demonstrated potent
antitumor properties and several research groups are trying to
synthesize these chemicals for new chemotherapeutic drugs. In a
review of these natural chemicals in The Journal of Natural
Products in 1999 they noted: "The Annonaceous acetogenins are
promising new antitumor and pesticidal agents that are found
only in the plant family Annonaceae. Chemically, they are
derivatives of long-chain fatty acids. Biologically, they
exhibit their potent bioactivities through depletion of ATP
levels via inhibiting complex I of mitochondria and inhibiting
the NADH oxidase of plasma membranes of tumor cells. Thus, they
thwart ATP-driven resistance mechanisms."
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J.L. McLaughlin, "Use of Selectively Cytotoxic Annonaceous
Acetogenins," filed February 4, 1997, P-97006.00 U.S.
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J.L. McLaughlin, "Annonaceous Acetogenins Selectively
Cytotoxic Against Pancreatic Tumors," filed February 17, 1997,
P-97019.00 U.S.
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Annonaceous Acetogenins against Pesticide-Resistance, "
disclosed to Purdue Research Foundation, October 15, 1997,
P-97059.00. US
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