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Pharmacognosy 2018
American Journal of Ethnomedicine
ISSN: 2348-9502
Page 34
April 16-17, 2018
Amsterdam, Netherlands
6
th
Edition of International Conference on
Pharmacognosy and
Medicinal Plants
Statement of Problem:
Human hyaluronidase-1 (Hyal-1) is
an enzyme strongly involved in the regulation of extracellular
matrix by balancing the deposition and potential degradation
of hyaluronic acid (HA) in the tissue. The inhibition of Hyal-
1 by specific inhibitors might be a promising target for
improved wound healing, tissue regeneration, and looking at
renal function also for induction of diuresis. Following the
discovery of the inhibitory effects of isoflavonoids from the
roots of
Ononis spinosa
L. on Hyal-1 in our previous work,
further studies have been conducted on selected flavonoid/
isoflavonoid compounds from natural sources with the aim to
study structure - activity relationships. Although glycosides
of these compounds abound and some have been proven to
show anti-hyaluronidase activity, the aglycones were chosen
because generally they are known to exhibit higher anti-
hyaluronidase effect.
Methodology:
By using surface-displayed human Hyal-1 on
Escherichia coli
F470, HA as substrate and stains-all method
for quantification of undegraded, high molecular polymer, the
enzyme activity can be determined easily. Apigenin (flavonoid
hyaluronidase inhibitor), Biochanin A (isoflavonoid present in
roots of
Ononis spinosa L
.) andMaackiain (pterocarpan present
in roots of
Ononis spinosa L
.) were used as representatives of
the above classes. Glycyrrhizinic acid, a known Hyal-1 inhibitor
was used as a standard.
Findings:
At a concentration of 250 µM, Maackiain and
Apigenin were found to be inactive. The IC50 values obtained
for Glycyrrhizinic acid and Biochanin A were 181 µM and 126
µM respectively.
Conclusion & Significance:
Strong inhibitory activity
(comparable to standard) against Hyal1 was found in the
isoflavonoid with the flavonoid and pterocarpan exhibiting
virtually no activity. This information will serve as a guide
toward more elaborate structure-activity studies.
Conclusion & Significance:
The results of this study will
support the use of this plant extract for diabetic healing over
the use of commercially available synthetic drugs.
Recent Publications
1. Monica Mame Soma Nyansa, Patrick Doe Fiawoyife,
Nana Ama Mireku-Gyimah and John Nii Adotey
Addotey (2017) Stability-indicating HPLC method for
the simultaneous determination of paracetamol and
tramadol hydrochloride in fixed-dose combination
tablets. International Journal of Biomedical Science
and Engineering 5(4):41–47.
2. Addotey JNAandAdosrakuRK (2016) Pilot production
of 5-HTP from the seeds of Griffonia simplicifolia.
World Journal of Pharmacy and Pharmaceutical
Sciences 5(6)204–221.
3. Cudjoe E K, Addotey J N A, Okine N N A, Adosraku R
K and Annan K (2016) Isolation and development of
an HPLC method for the quantification of a biomarker
in the roots of Paullinia pinnata. Int J Pharm Sci Res
7(8):3446–52.
4. John Nii Adotey Addotey and Monica Mame Soma
Nyansah (2016) Quality assessment of some topical
polyherbal preparations on the Ghanaian Market.
World Journal of Pharmacy and Pharmaceutical
Sciences 5(4)461–472.
Preliminary structure activity studies on Hyal1 inhibitors
J Addotey, M Lechtenberg, F Petereit, I Lengers, J Jose
and
A Hensel
University of Münster, Germany
J Addotey et al., Am J Ethnomed 2018, Volume 5
DOI: 10.21767/2348-9502-C1-005