Research Article Open Access
Volume 2 • Issue 2 • 1000117
Chemotherapy
ISSN: 2167-7700 CMT, an open access journal
Open Access Research Article
Chemotherapy: Open Access
Uddin et al., Chemotherapy 2013, 2:2
http://dx.doi.org/10.4172/2167-7700.1000117
*Corresponding author: Ghias Uddin, Institute of Chemical Sciences, University
of Peshawar, Peshawar-25120, Pakistan, E-mail: drghiasuddin@hotmail.com,
Ghiasuddin@upesh.edu.pk
Received July 31, 2013; Accepted August 17, 2013; Published August 26, 2013
Citation: Uddin G, Rauf A, Siddiqui BS, Khan A, Marasini BP, et al. (2013)
Broad Spectrum Anticancer Activity of Pistagremic Acid. Chemotherapy 2: 117.
doi:10.4172/2167-7700.1000117
Copyright: © 2013 Uddin G, et al. This is an open-access article distributed under
the terms of the Creative Commons Attribution License, which permits unrestricted
use, distribution, and reproduction in any medium, provided the original author and
source are credited.
Keywords: Pistacia integerrima; Pistagremic acid; Antiproliferative
agent; Anticancer agent
Introduction
Pistacia integerrima belongs to family Anacardiacea and found in
eastern Himalayan range [1]. he leaves, bark and galls of the plant
are generally used for the treatment of cough, asthma, fever, vomiting,
diarrhea, infection, hyperuricemia, hepatitis and other liver disorders
[2-7].
Cancer is one of the notorious and lethal diseases responsible for
7.6 million deaths (approx. 13% of all deaths) with 12.7 million new
cases in 2008, that are projected to continue rising, with an estimated
13.1 million deaths with are 22.2 million cases in 2030 [8,9]. Although
various types of cancer reported, cancers of the prostate, lung, and liver
the most commonly reported worldwide. here is similar index as the
worldwide to developing countries like Pakistan [9].
Researchers have been spending several decades to identify
efective agents against cancer which is one of the leading causes of
death worldwide. hus, about 60% of anticancer drugs are structural
modiication and their analogues from the natural sources such as
vinblastine, taxol and camptothecin [10]. However, the management
of cancer is still not up to mark and always needs to ind out new
chemotherapeutic agents. In continuation of our previous investigation
on the bioactivities of pistagremic acid (Figure 1) [11], which was
evaluated for its cytotoxic efects against NCI 60-cell panel on eight
organs (leukemia, non-small cell lung cancer, colon, CNS, melanoma,
ovarian, prostate, renal and breast) at National Cancer Institute (NCI)
USA, showed signiicant inhibition of human cancer cell lines.
Materials and Methods
Pistacia integerrima galls were collected from Razagram,
Khyber Pakhtunkhwa, Pakistan in February, 2010 and identiied as
P. integerrima by Prof. Dr. Abdur Rashid, Department of Botany,
University of Peshawar. A voucher specimen (RF-895) preserved in
the herbarium of the Department of Botany, University of Peshawar,
Pakistan.
he plant material was shade-dried at room temperature, grinded
into powder and subsequently successively extracted repeatedly
(thrice) with methanol (MeOH). he combined methanolic extracts
were freed of the solvent under vacuum to obtained thick syrup.
hen 400 g of the concentrated methanolic extract was successively
partitioned between n-hexane/water, chloroform/water, ethyl acetate/
water and butanol/water. he chloroform fraction was concentrated
under vacuum pressure and 10 g of it was subjected to silica gel column
chromatography, eluting with n-hexane, n-hexane-ethyl acetate
(EtOAc) in an increasing order of polarity. As a result, 13 fractions
(RF-1 to RF-13) were obtained based on TLC proiles. Fraction RF-4
(90 mg, eluted n-hexane-EtOAc, 82:18) aforded colorless crystals of
various sizes which were separated from the solution by decantation.
he crystals were re-crystallized with appropriate solvents (n-hexane-
acetone, 4:1). he chemical structure of the pure crystalline compound
was identiied as 2-Methyl-6-(4, 4, 10, 13, 14-pentamethyl-3-xo-2, 3,
4, 5, 6, 7, 10, 11, 12, 13, 14, 15, 16, 17-tetradecahydro-1H-cyclopenta
[a] phenanthren-17-yl) hept-2-enoic acid (pistagremic acid) by X-ray
crystallography analysis as reported earlier [12].
Anticancer Assay
he anticancer assay against cancer cell lines were conducted at NCI
by using Sulphorhodamine B assay [13,14]. hese cancer cell lines were
grown in RPMI-1640 medium, supplemented with fetal bovine serum
(10%) and L-glutamine (2 mM). he culture lasks were kept in CO
2
Broad Spectrum Anticancer Activity of Pistagremic Acid
Ghias Uddin
1
*, Abdur Rauf
1
, Bina Shaheen Siddiqui
2
, Ajmal Khan
2
, Bishnu P Marasini
2
, Abdul Latif
1
and Thomas J Simpson
3
1
Institute of Chemical Sciences, University of Peshawar, Peshawar-25120, Pakistan
2
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
3
School of Chemistry, University of Bristol, Bristol BS8 1TS, UK
Abstract
Background: Pistagremic acid; 3-methyl-7-(4,4,10,13,14-pentamethyl-3-2,3,4,5,6,7,10,11,12,13,14,15,16,17-
tetradecahydro-1H-cyclopenta[a]phenanthr-en-17-yl)-oct-3-enoic acid was isolated from the chloroform fraction of
Pistacia integerrima. Cytotoxic evaluation against NCI-60 DTP human tumor cell line was performed.
Methods: The anticancer assays for this compound were performed in accordance with the protocol of the Drug
Evaluation Branch, of the National Cancer Institute (NCI) Developmental Therapeutic Program (www.dtp.nci.nih.gov)
for their anticancer activity in vitro.
Results: It showed broad spectrum antiproliferative activity with an average GI
50
, and TGI, values 0.103 µM and
0.259 µM, respectively. It also showed signiicant LC
50
value at the average 0.634 µM against all cell lines excluding
K-562, RPMI-8226, NCI-H226, and NCI-H460 cell-lines.
Conclusions: Pistagremic acid showed cytotoxicity for all tested cancer cell line, thus it may serve as a potential
structure lead for the development of new anticancer drugs.