Institutional Repository of Chengdu Institute of Biology, CAS

李大平

陶勇

何晓红

张礼霞

占国强

一种生物电化学偶联脱氮装置和方法

赵海

靳艳玲

方扬

一种快速降低薯类粘度的方法

Zhang, Zhi-Feng

Chen, Li

Ding, Li-Sheng

Liu, Liang

Zhou, Hua

Luo, Pei

Qing, Lin-Sen

analysis. Recovery of both Compound X and the internal standard
was monitored, along with matrix effects, using the UHPLC-DAD-
MS. Recovery of Compound X was achieved with minimal matrix
effects allowing quantitative measurements of the molecule
extracted from rat plasma. Issues including solubility, stock stabil-
ity and suitable internal standard were overcome. The developed
bioanalysis method was an in–house first and will underpin fur-
ther development to support preclinical pharmacokinetics and tox-
icokinetics in efficacy and safety studies, and subsequent clinical
studies.
doi:10.1016/j.bcp.2017.06.078
O14
Determination of DQ-798 in rat plasma by UHPLC-MS/MS and its
application to a pharmacokinetic study
Zhi-Feng Zhang a,c, Li Chen a, Li-Sheng Ding b, Liang Liu a,c, Hua
Zhou a,c, Pei Luo a,c, Lin-Sen Qing b
a State Key Laboratory for Quality Research in Chinese Medicines, Macau
University of Science and Technology, Macau, China, b Key Laboratory
of Natural Medicine and Translational Medicine, Chengdu Institute of
Biology, Chinese Academy of Sciences, Chengdu, China, c Faculty of
Chinese Medicine, Macau University of Science and Technology, Macau,
China
DQ-798 is a more druggable derivative of astragaloside IV pre-
pared by TEMPO-mediated oxidation, which possess significant
pharmacological activities. In this study, an ultra-high performance
liquid chromatographic method combined with a tandem mass
spectrometry for the determination of DQ-798 in rat plasma was
developed. After simple protein precipitation with acetonitrile
including digoxin (internal standard, IS), the analyte were analyzed
by multiple reaction monitoring in positive ESI mode at m/z transi-
tions of [M + Na]+821? 627 for DQ-798 and 803? 387 for the IS.
The mobile phase is the distilled water and acetonitrile (66:34).
The flow rate for the mobile phase was set at 0.35 mL/min. The lower
limit of quantification of DQ-798 was obtained as 2 ng/mL. The cal-
ibration curve was linear at a range of 2–2000 ng/mL (R2 > 0:999).
The validation parameters investigated, which were specificity, pre-
cision, accuracy, matrix effect, recovery, and stability, were well
within acceptable limits. This analytical method was successfully
applied to monitor the plasma concentrations of DQ-798 following
oral administration in rats.
doi:10.1016/j.bcp.2017.06.079
O15
Bioaccessibility of organosulphur compounds from Allium sati-
vum
Gracia Marti a, Gareth Evans a, Liam Jones a, Blanca Viadel b, Begoña
Ruiz b, Elisa Gallego b, Michael Graz a
a Neem Biotech Ltd., Abertillery, UK, b Ainia, Valencia, Spain
Garlic (Allium sativum), apart from its use as food, has been used
as a medicinal plant for over 4000 years. Several investigations sug-
gest that the biological and medical functions of garlic are due to the
high content of organosulphur compounds. The bioaccessibility of
the organosulphur compounds is an important factor for the evalu-
ation of the functional activity of the garlic. In the present study, a
Dynamic Gastrointestinal Digester (DGD) was used to determine
the bioaccessibility after digestion of two extracts containing the
organosulphur compounds; ajoene and allicin. The DGD is a multi-
compartmental, dynamic and computer-controlled system, which
reproduces the gastrointestinal digestion process including the
chewing, the gastric digestion and the digestion of the small intes-
tine phases. The study showed that after an in vitro gastrointestinal
digestion process, ajoene is seven times more bioaccessible when
encapsulated than in unencapsulated doses, recovering approxi-
mately 51% of the compound administered. Allicin recovered after
digestion, administered as a combination of alliin and alliinase,
showed no significant difference in bioaccessibility when comparing
unencapsulated and encapsulated doses. The allicin recovered after
the gastrointestinal digestion in both cases exceeded 40%. The
results show significant bioaccessibility of the two organosulphur
compounds after in vitro gastrointestinal digestion, which
enables the prediction of their behaviour in the gastrointestinal
tract. The stability of the unencapsulated allicin-potential formula-
tion is also promising for whole gut availability. Future work is
recommended to understand the absorption of the compounds for
a better understanding of their possible beneficial effects in human
health.
doi:10.1016/j.bcp.2017.06.080
Session 6: Novel sources of bioactives IV
O16
Phyto-oestrogenic property of mimosine: A phenylalanine alka-
loid
A.K.M. Moyeenul Huq a, Kamal Rullah a, M.F.F.M. Aluwi a, Lam Kok
Wai a, Johnson Stanslas b, Jamia Azdina Jamal a
a Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia, b Universiti
Putra Malaysia, Serdang, Malaysia
Hormone replacement therapy (HRT) has been generally used in
postmenopausal symptoms in women caused by a lack of endoge-
nous oestrogen. However, due to the increased concern around the
potential associated risks of breast and endometrial cancer there is
an increased demand for natural oestrogenic agents with lesser side
effects. Mimosine is a phenylalanine class of alkaloid. It has been
reported that, another phenylalanine alkaloid capsaicine and its ana-
logues possess oestrogenic activity. Therefore, this study was
designed to investigate the oestrogen like activity of mimosine by
using in vitro assays with the ER positive MCF-7 cell line and in silico
models. Cell viability by cellular count and MTT cell proliferation
assays were performed using the oestrogen-dependent MCF-7 breast
cancer cells. The regulation of oestrogen marker TFF1 and PGR gene
expression were also studied. The binding ability of mimosine to ERa
was predicted by in silico docking method. The results indicated that
mimosine caused significant cell proliferation (P < 0.05) and
increased cellular viability at 0.1 lM concentration. It also increased
the expression of both TFF1 (P < 0.01) and PGR mRNA levels
(P < 0.05), while co-treatment with anti-oestrogenic tamoxifen sig-
nificantly decreased MCF-7 cell proliferation (P < 0.001) indicating
an ER mediated effect of mimosine. The docking result showed mod-
erate interaction with the ERa binding site as compared to estradiol.
The results indicate the oestrogenicity of mimosine for the first time
and suggest that, it can be further studied and developed as an alter-
native to HRT for postmenopausal women.
doi:10.1016/j.bcp.2017.06.081
114 Abstracts / Biochemical Pharmacology 139 (2017) 105–141


Determination of DQ-798 in rat plasma by UHPLC-MS/MS and its application to a pharmacokinetic study

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一种生物电化学偶联脱氮装置和方法

一种快速降低薯类粘度的方法

Determination of DQ-798 in rat plasma by UHPLC-MS/MS and its application to a pharmacokinetic study

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