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ANTDIABETIC ACTIVITY
Overview of Diabetes
Diabetes is a syndrome associated with excess blood sugar due to
either low levels of insulin production by the pancreas or insulin resistance.
Diabetes can lead to a variety of illnesses including heart disease, stroke,
kidney failure, blindness, limb amputations and birth defects. It is estimated
that around 250 million people in the world are living with diabetes today and
this number will increase to around 380 million by 2025 (WHO
prediction). The US alone has 20.8 million people suffering from diabetes (LeadDiscovery,
2009) while the UK hosts about 2.5 million sufferers (Diabetes
UK). Diabetes has also become a major cause of premature illness and death
in many countries, mainly through the increased risk of cardiovascular diseases.
According to WHO estimates, over 1.1 million people around the world die
annually directly from diabetes. The number of people whose death was recorded
as heart disease or kidney failure where diabetes was a contributory factor is,
however, considerably higher. Accordingly, diabetes related causes account for
over 3.8 million deaths; equivalent to one death every ten seconds and claiming
the lives of as many people as HIV/AIDS (Espicom
2009).
According to Diabetes UK reports,
the incidence of Type-1 diabetes (lack of insulin) in children is rising at a
rate of three to four percent a year. The increase in Type-2 diabetes (insulin
resistance) which has been closely linked to an aging population is also rapidly
rising together with the numbers of obese or overweight people. Type-2 diabetes,
traditionally a condition associated with older age groups, is now also
appearing in children and adolescents.
The economic impact
and market share of antidiabetic drugs
It is estimated that the global diabetes therapy market is at
around US$26.3 billion in 2009 and is expected to grow to around US$34.5 billion
by 2013 (Espicom 2009). Market analysis by
various interested groups indicates that oral antidiabetic drugs account for
around 39% of the total market value. Metformin is the recommended first-line
therapy for Type-2 diabetes and accounts for around 11-12% of the total market
value. Other oral agents include sulphonylureas, thiazolidinediones (TZDs or
glitazones), glinides and α-glucosidase inhibitors. Many of these are reported
to be widely available generically and the sales of leading proprietary oral
agents are now over US$7 billion. There are also quite few current trials and
developments in insulin formulations, injectable glucagon-like peptide-1 (GLP-1)
agonists, oral dipeptidyl peptidase-4 (DPP-4) inhibitors, etc, but the
hope still is on the discovery of novel antidiabetic drugs.
With widely accepted prediction of an already large
market for diabetes medications to show continuous growth, the potential of drug
discovery researches in this area is enormous.
Our Research Strategy
Being aware of the impact of scientific research in this field,
we introduced several bioassay systems by the beginning of 2009. Our strategy is
to study medicinal plants with claimed traditional uses for the management
of diabetes. When activity is detected, we undertake a comprehensive
bioassay-guided isolation study to identify the active principles. The following
are among the most relevant bioassay screens of interest:
·
Inhibition
of the catalytic activity of α-glucosidase leads to the retardation of glucose
absorption from the gut leading to decreased level of postprandial blood
glucose. We are targeting this enzyme by natural products to identify
chemotherapeutic agents for diabetes as well as obesity.
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The common feature of hyperglycaemia is
glycation reaction resulting in the formation of various products which are
commonly associated with diabetes, aging and neurodegenerative diseases: We use
an in vitro model of protein glycation measurements.
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Compounds that enhance insulin-dependent
increase in glucose uptake in adiposities and myoblasts are regarded as
antidiabetic agents: glucose transport in cultured cells is a relevant
method of sugar uptake study.
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Read our recent article
which describes interesting synergistic effect
of
potential antidiabetic compounds: HABTEMARIAM S.
(2011). a-Glucosidase
inhibitory activity of kaempferol-3-O-rutinoside.
Natural Product Communications
6(2),
201-203.
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By using our bioassay guided phytochemistry studies, we have identified several hit extracts - we would like to hear from
anyone with similar interests...Contact
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