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Medchem & Toxicology 2018
Page 64
Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123
A n n u a l C o n g r e s s o n
Medicinal Chemistry,
Pharmacology and toxicology
J u l y 3 0 - 3 1 , 2 0 1 8
Am s t e r d a m , N e t h e r l a n d s
A
s many as 200 million people worldwide are infected with hepatitis C virus (HCV) and more than 350,000 people die yearly
from hepatitis C-related diseases (WHO, June 2011). There is no preventive vaccine available for HCV due to its highly
mutable nature evidenced by the presence of more than 50 subtypes of HCV. In the present study, the water extract of the leaves
of the wild Egyptian artichoke (WEA) (
Cynara cardunculus
L. var. sylvestris (Lam.) Fiori) showed improvement of HCV infection
symptoms through the clinical investigation of WEA extract on some infected Egyptian patients. The results showed outstanding
activity against HCV and its complications such as ascites and jaundice by measuring the PCR, and liver functions such as
alanine transaminase (ALT), and aspartate transaminase (AST). The phytochemistry of the WEA extract and its subsequent
evaluation of inhibition capacity
in vitro
using cell-culture derived HCV resulted in the identification of two potent sesquiterpene
lactones showing
in vitro
activity against all genotypes. Their structural elucidation was done by extensive spectroscopic tools
such as NMR and HR-MS spectroscopy. The absolute configuration was determined by TDDFT ECD calculations and comparison
with the experimental CD spectra. Cynaropicrin and grosheimol showed EC50 at 1.03 μM, and 1.27 μM, by using a luciferase-
carrying reporter virus. Time-of-addition experiments revealed that these compounds inhibited HCV virus at a time-point during
entry. Finally, the results showed that compounds cynaropicrin and grosheimol inhibited HCV particles from genotypes 1a, 1b,
2b, 3a, 4a, 5a, 6a and 7a indicating that these compounds inhibit HCV cell entry independently of viral genotype or subtype. Most
important is that compound cynaropicrin can inhibit HCV through many important mechanisms: cell-entry inhibitor, inhibition of
cell to cell coinfection, antihyperlipedemic and antitumor activities3. There is a plenty of publications confirmed that cynaropicrin
is a very promising drug as antitumor agent.
elsebai72@yahoo.comPromising natural compounds for treatment of
hepatitis C virus and its complications
Mahmoud F Elsebai
1
, Jukka Hakkola
2
and Mohamed Mehiri
3
1
Mansoura University, Egypt
2
University of Oulu, Finland
3
University Nice Sophia Antipolis, France
J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C3-009