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1. Single-dose and multiple-dose pharmacokinetics of zaltoprofen after oral
administration in healthy Chinese volunteers. J Biomed Res, 2011;
25(1):56-62
Lingjun Li, Pengcheng Ma, Yuping Cao, Lei Tao, Yue Tao
Department of Pharmacology, Institute of Dermatology, Chinese Academy of
Medical Sciences and Peking Union Medical College, Nanjing, Jiangsu 210042,
China.
Abstract: Zaltoprofen, a propionic acid derivative of non-steroidal anti-inflammatory
drugs, has strong inhibitory effects on actue and chronic inflammation. A randomized,
dose-escalating study was conducted to evaluate the pharmacokinetics of single and
multiple oral doses of zaltoprofen in 12 healthy Chinese volunteers. Pharmacokinetics
was determined from serial blood samples obtained up to 24 h after administration of
a single dose of zaltoprofen at 80, 160 or 240 mg and after multiple doses of
zaltqorofen at 80 mg 3 times daily. The Cmax and AUC0-24 of zaltoprofen were found
to be proportional to drug dose. Zaltoprofen was rapidly absorbed (tmax =1.46±0.83 h)
and cleared (t1/2 =4.96±2.97 h). Pharmacokinetic parameters after multiple doses were
similar to those after single doses. Zaltoprofen was well tolerated. These results
support a tid regimen of zaltoprofen for the management of acute and chronic
inflammation.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR110107&flag=1
2. The efficacy of NP11-4-derived immunotoxin scFv-artesunate in reducing
hepatic fibrosis induced by Schistosoma japonicum in mice. J Biomed Res,
2011; 25(2):148-154
Hong Lia,b, Chunyan Gua,b, Yongya Rena,b, Yang Daic, Xiaojuan Zhua,b, Jing Xua,
Yuhua Lib, Zhenning Qiua, Jin Zhua,d, Yinchang Zhuc, Xiaohong Guana, Zhenqing
Fenga,b
a
Key Labortary of Antibody Technique of Ministry of Health, Nanjing Medical
University, Nanjing, Jiangsu 210029, China;
b
Pathology Department, Nanjing Medical University , Nanjing, Jiangsu 210029, China;
c
Jiangsu Institute of Parasitic Diseases, Wuxi, Jiangsu 214000, China;
d
Huadong Medical Institute of Biotechniques, Nanjing, Jiangsu 210002, China.
Abstract: Schistosomiasis is one of the most prevalent parasitic diseases in China, and
hepatic fibrosis caused by schistosome infection is the principal cause of death. The
aim of this study was to evaluate the efficacy of NP11-4-derived immunotoxin
scFv-artesunate on Schistosoma japonicum-induced hepatic fibrosis. A single-chain
variable fragment (scFv) was generated from the murine anti-Schistosoma japonicum
(S. japanicum) monoclonal antibody NP11-4. The scFv was expressed as a soluble
protein and purified by Ni-affinity chromatography. After conjugation with artesunate,
the binding ability with soluble egg antigens (SEA) was determined by an
enzyme-linked immunosorbent assay (ELISA). The biological activity of purified
scFv, scFv-artesunate (immunotoxin), and artesunate was detected in vivo. Image-Pro
Plus software was used to analyze the size of egg granuloma and the extent of liver
fibrosis. The recombinant scFv expession vector was constructed and expressed
successfully. Af-ter purification by a His-trap Ni-affinity column, the scFv yield was
approximately 0.8 mg/L of culture medium. ELISA results showed that chemical
conjugation did not affect the binding activity of the immunotoxin. Our ani-mal
experiments indicated that the immunotoxin could significantly reduce the size of egg
granuloma in the liver and inhibit hepatic fibrosis. The immunotoxin could be used as
a promising candidate in the targeted therapy of S. japonicum-induced hepatic
fibrosis.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=jbr110209&flag=1
3. Aspirin suppresses growth of human gastric carcinoma cell by inhibiting
survivin expression. J Biomed Res, 2011; 25(4):246-253
Li Yanga, Huaijun Zhub, Dongxiao Liua, Song Lianga, Hao Xua, Jie Chenc, Xuerong
Wangc, Zekuan Xua
a
Department of General Surgery, the First Affiliated Hospital of Nanjing Medical
University, Nanjing, Jiangsu 210029, China;
bDivision
of Clinical Pharmacy, Department of Pharmacy, Drum Tower Hospital Affiliated to Medical
School of Nanjing University, Nanjing, Jiangsu 210008, China;
c
Department of Pharmacology, Nanjing Medical University, Nanjing, Jiangsu
210029, China.
Abstract: Regular use of aspirin (ASA) could reduce the risk of gastric cancer
although the precise mechanism remains unclear. Down-regulation of survivin may be
one of the cyclooxygenase-independent mechanisms whereby ASA induces apoptosis
of gastric cancer cell. In this study, we investigated the effect of ASA on the growth,
apoptosis and survivin expression of gastric cancer cell line SGC7901. The survival
of cells treated with 3.0 and 10.0 mmol/L ASA for 24 h was decreased by 44.6% and
88.5%, respectively. ASA at 3.0 mmol/L inhibited the viability of SGC7901 cells in a
time-dependent manner. Apoptosis analysis showed similar results with MTT assay.
ASA at 3.0 and 10.0 mmol/L decreased the mRNA transcript levels of survivin and
reduced survivin protein levels in SGC7901 cells also in a time-dependent manner.
Our findings indicated that ASA inhibited the proliferation of SGC7901 by
sup-pressing survivin at both the transcriptional and translational level.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=jbr110403&flag=1
4. Cardioprotective activity of alcoholic extract of Tinospora cordifolia (Willd.)
Miers in calcium chloride-induced cardiac arrhythmia in rats. J Biomed Res,
2011; 25(4):280-286
Ashish Kumar Sharmaa, Kunal Kishorea, Divya Sharmaa, B.P Srinivasanb, Shyam
Sunder Agarwalb, Ashok Sharmaa, Santosh Kumar Singha, Samir Gaura, Vijay Singh
Jatava
a
Department of Pharmacology, Gyan Vihar School of Pharmacy, Suresh Gyan
Vihar University, Jagatpura, Jaipur (Rajasthan)302025, India;
b
Delhi Institute of Pharmaceutical Sciences & Research, Department of
Pharmacology, Pushpvihar, Sector-III. New Delhi 110017, India.
Abstract: The present study investigated the antiarrhythmic activity of alcoholic
extract of Tinospora cordifolia (T. cordifolia) in CaCl2 induced arrhythmia. CaCl2 (25
mg/kg) was administered by intravenous infusion (iv) to produce arrhythmia in rats.
The animals were then treated with T. cordifolia extract (150, 250, and 450 mg/kg)
and verapamil (5 mg/kg,iv). Lead II electrocardiogram was monitored. Plasma
calcium, sodium and potassium levels were measured. In CaCl2 induced arrhythmia,
heart rate was decreased by 41.10%, T. cordifolia at 150, 300, and 450 mg/kg decreased
the heart rate by 26.30%, 29.16%, and 38.29%, respectively, and verapamil reduced
the heart rate by 9.70% compared to the normal group. The PQRST waves were
normalized and atrial and ventricular fibrillation was controlled in rats treated with
verapamil and T. cordifolia. CaCl2 increased calcium and sodium levels and decreased
potassium levels in blood. T. cordifolia dose-dependently decreased calcium and
sodium levels and increased potassium levels. Hence, T. cordifolia can be used in
antiarrhythmic clinical settings and beneficial in atrial and ventricular fibrillation and
flutter and may be indicated in ventricular tachyarrhythmia.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=jbr110408&flag=1
5. Effects of minocycline on the expression of NGF and HSP70 and its
neuroprotection role following intracerebral hemorrhage in rats. J Biomed
Res, 2011; 25(4):292-298
Jingnan Pu, Wei Shi, Zizhang Wang, Ruizhi Wang, Zhenyu Guo, Chongxiao Liu,
Jianjun Sun, Ligui Gao, Ren Zhou
Department of Neurosurgery, the Second Affiliated Hospital of Medical College of
Xi’an Jiaotong University, Xi’an, Shaanxi 710004, China.
Abstract: The present study was aimed to investigate the effects of minocycline (MC)
on the expression of nerve growth factor (NGF) and heat shock protein 70 (HSP70)
following intracerebral hemorrhage (ICH) in rats, and explore the neuroprotective
function of MC. Seventy-eight male SD rats were randomly assigned to three groups:
the ICH control group (n = 36), ICH intervention group (n = 36) and sham operation
group (n = 6). The ICH control group and ICH intervention group were subdivided
into 6 subgroups at 1, 2, 4, 5, 7 and 14 d after ICH with 6 rats in each subgroup. Type
IV collagenase was injected into the basal nuclei to establish the ICH model. All rats
showed symptoms of the nervous system after the model was established, and the
sympotsm in the ICH control group were more serious than the ICH intervention
group. The number of NGF-positive cells and HSP70-positive cells in the ICH
intervention group was higher than that of the ICH control group. MC administration
by intraperitoneal injection can increase the expression of NGF and HSP70. MC may
inhibit the activation of microglia, the inflammatory reaction and factors, matrix
metalloproteinases and apoptosis, thus protecting neurons. The change of the
expression of NGF and HSP70 may be involved in the pathway of neuroprotection by
MC.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=jbr110410&flag=1
6. Comparison of liquid-liquid extraction-thin layer chromatography with
solid-phase extraction-high-performance thin layer chromatography in
detection of urinary morphine. J Biomed Res, 2011; 25(5):362-367
Ali Ahadia, Alireza Partoazarb, Mohammad-Hassan Abedi-Khorasganic, Seyed Vahid
Shetab-Boushehrid
a
Department of Physiology; bDepartment of Pharmacology; dDepartment of
Medical Nanotechnology, School of Medicine, Tehran University of Medical
Sciences, Tehran, I.R. 1449614535 Iran;
c
Legal Medicine Organization of Iran, Tehran, I. R. 1449614535; Iran.
Abstract: Liquid-liquid extraction-thin layer chromatography (LLE-TLC) has been a
common and routine combined method for detection of drugs in biological materials.
Solid-phase extraction (SPE) is gradually replacing the traditional LLE method. High
performance thin layer chromatography (HPTLC) has several advantages over TLC.
The present work studied the higher efficiency of a new SPE-HPTLC method over
that of a routine LLE-TLC method, in extraction and detection of urinary morphine.
Fifty-eight urine samples, primarily identified as morphine-positive samples by a strip
test, were re-screened by LLE-TLC and SPE-HPTLC. The results of LLE-TLC and
SPE-HPTLC were then compared with each other. The results showed that the
SPE-HPTLC detected 74% of total samples as morphine-positive samples whereas the
LLE-TLC detected 48% of the same samples. We further discussed the effect of
codeine abuse on TLC analysis of urinary morphine. Regarding the importance of
morphine detection in urine, the present combined SPE-HPTLC method is suggested
as a replacement method for detection of urinary morphine by many reference
laboratories.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=jbr110508&flag=1
7. Involvement of adenosine and standardization of aqueous extract of garlic
(Allium sativum Linn.) on cardioprotective and cardiodepressant properties
in ischemic preconditioning and myocardial ischemia-reperfusion induced
cardiac injury. J Biomed Res, 2012; 26(1):24-36
Ashish Kumar Sharmaa, Arshee Munajjama, Bhawna Vaishnava, Richa Sharmaa,
Ashok Sharmaa, Kunal Kishorea, Akash Sharmaa, Divya Sharmaa, Rita Kumaria,
Ashish Tiwaria, Santosh Kumar Singha, Samir Gaura, Vijay Singh Jatava, Barthu
Parthi Srinivasanb, Shyam Sunder Agarwalb
a
Department of Pharmacology, Gyan Vihar School of Pharmacy, Suresh Gyan
Vihar University, Mahal, Jagatpura, Jaipur (Rajasthan) 302025, India;
bDepartment
of Pharmacology, Delhi Institute of Pharmaceutical Sciences & Research, Pushpvihar,
Sector-III. New Delhi 110017, India.
Abstract: The present study investigated the effect of garlic (Allium sativum Linn.)
aqueous extracts on ischemic pre-conditioning and ischemia-reperfusion induced
cardiac injury, as well as adenosine involvement in ischemic pre-conditioning and
garlic extract induced cardioprotection. A model of ischemia-reperfusion injury was
established using Langendorff apparatus. Aqueous extract of garlic dose was
standardized (0.5%, 0.4%, 0.3%, 0.2%, 0.1%, 0.07%, 0.05%, 0.03%, 0.01%), and the
0.05% dose was found to be the most effective. Higher doses (more than 0.05%) were
highly toxic, causing arrhythmia and cardiodepression, whereas the lower doses were
ineffective. Garlic exaggerated the cardioprotective effect of ischemic preconditioning.
The cardioprotective effect of ischemic preconditioning and garlic cardioprotection
was significantly attenuated by theophylline (1,000 μmol/L) and 8-SPT (10 mg/kg,
i.p.) and expressed by increased myocardial infarct size, increased LDH level, and
reduced nitrite and adenosine levels. These findings suggest that adenosine is
involved in the pharmacological and molecular mechanism of garlic induced
cardioprotection and mediated by the modulation of nitric oxide.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR120104&flag=1
8. Soy isoflavone extracts stimulate the growth of nude mouse xenografts
bearing estrogen-dependent human breast cancer cells (MCF-7). J Biomed
Res, 2012; 26(1):44-52
Qian Wu, Ye Yang, Jing Yu, Nianzu Jin
Department of Hygienic Analysis and Detection, School of Public Health, Nanjing
Medical University, 140 Hanzhong Road, Nanjing, Jiangsu 210029, China.
Abstract: We explored the effects of different lifetime exposures to soy isoflavone
extracts on the growth of estrogen-dependent human breast cancer cells (MCF-7)
implanted into athymic mice of different ovarian statuses. The athymic mice,
ovariectomized or not, were implanted with MCF-7 cells. Mice were fed with low,
moderate and high doses of soy isoflavone extract, at dietary concentrations of 6.25,
12.5 and 25 g/kg, in different reproductive models, respectively. The expression of
ki-67 was detected by immunohistochemistry. pS2 expression in tumors was analyzed
by real-time PCR. Estrogen level in the serum was measured by chemiluminescence
enzyme immunoassay. Total genistein and daidzein levels in serum and urine were
determined by liquid chromatography-electrospray tandem mass spectrometry
(LC-ES/MS/MS). In Group A, on week 4, nude mice were exposed to different doses
of soy iosflavone extracts. In Group B, the experimental diets were given to the nude
mice following ovariectomy and tumor implantation. In both groups, 6.25 and 12.5
g/kg soy isoflavone extracts stimulated the growth of MCF-7 xenografts, increased
pS2 expression, proliferation and estrogen level in serum. In both Group B
(postmenopausal mouse model) and Group C (premenopausal mouse model), soy
isoflavone extracts at doses of 6.25 and 12.5 g/kg showed stimulatory effects on the
growth of MCF-7 tumors. In conclusion, administration of soy isoflavone extracts at
doses of 6.25 and 12.5 g/kg during adolescence or later in life stimulated tumor
growth in both menopausal and postmenopausal mouse models.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR120106&flag=1
9. Cynodon dactylon and Sida acuta extracts impact on the function of the
cardiovascular system in zebrafish embryos. J Biomed Res, 2012; 26(2):90-97
Rajaretinam Rajesh Kannan, Samuel Gnana Prakash Vincent
International Center for Nanobiotechnology (ICN), Center for Marine Science and
Technology (CMST), Manonmaniam Sundaranar University, Rajakkamangalam,
Kanyakumari Dist, Tamil Nadu 629502, India.
Abstract: The aim of the present study was to screen cardioactive herbs from Western
Ghats of India. The heart beat rate (HBR) and blood flow during systole and diastole
were tested in zebrafish embryos. We found that Cynodon dactylon (C. dactylon) induced
increases in the HBR in zebrafish embryos with a HBR of (3.968±0.344) beats/s,
which was significantly higher than that caused by betamethosone [(3.770±0.344)
beats/s]. The EC50 value of C. dactylon was 3.738 µg/mL. The methanolic extract of
Sida acuta (S. acuta) led to decreases in the HBR in zebrafish embryos [(1.877±0.079)
beats/s], which was greater than that caused by nebivolol (positive control). The EC50
value of Sida acuta was 1.195 µg/mL. The untreated embryos had a HBR of
(2.685±0.160) beats/s at 3 d post fertilization (dpf). The velocities of blood flow
during the cardiac cycle were (2,291.667±72.169) µm/s for the control,
(4,250±125.000) µm/s for C. dactylon and (1,083.333±72.169) µm/s for S. acuta. The
LC50 values were 32.6 µg/mL for C. dactylon and 20.9 µg/mL for S. acuta. In addition,
the extracts exhibited no chemical genetic effects in the drug dosage range tested. In
conclusion, we developed an assay that can measure changes in cardiac function in
response to herbal small molecules and determine the cardiogenic effects by
microvideography.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR120204&flag=1
10. STAT3 mediates resistance of CD44+CD24-/low breast cancer stem cells to
tamoxifen in vitro. J Biomed Res, 2012; 26(5):325-335
Xiaoyan Wanga, Guozhu Wanga, Yi Zhaoa, Xiaoan Liua, Qiang Dinga, Jingping Shia,
Yin Dingb, Shui Wanga
a
Department of Breast Surgery, the First Affiliated Hospital of Nanjing Medical
University, Nanjing, Jiangsu 210029, China;
b
Laboratory of Mesoscopic Chemistry and Department of Polymer Science and
Engineering, College of Chemistry and Chemical Engineering, Nanjing University,
Nanjing, Jiangsu 210093, China.
Abstract: We sought to determine whether STAT3 mediated tamoxifen resistance of
breast cancer stem cells in vitro. The capacities for mammosphere formation and
STAT3 expression of CD44+CD24-/low MCF-7 and MCF-7 were observed. The
CD44+CD24-/low subpopulation ratio and its sensitivity to adriamycin were analyzed
in MCF-7 and TAM resistant (TAM-R) cells. Cell cycle, apoptosis, STAT3 and
phospho-STAT3 changes were observed after treatment with tamoxifen. Small
interference RNA-mediated knockdown of STAT3 in TAM-R cells was also
performed. CD44+CD24-/low MCF-7 showed higher capacities for mammosphere
formation and STAT3 expression than total MCF-7. The CD44+CD24-/low
subpopulation was also upregulated in TAM-R cells with less sensitivity to
adriamycin than MCF-7. Cell cycle changes, anti-apoptotic effects and STAT3
changes were also found. Meanwhile, the knock-down of STAT3 in TAM-R resulted
in an increase in sensitivity to tamoxifen. It is concluded that STAT3 plays an
essential role in breast cancer stem cells, which correlated with tamoxifen resistance.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR120504&flag=1
Pharmacokinetics
11. Secondary metabolite credentials of Evolvulus alsinoides by high
performance thin layer chromatography (HPTLC). J Biomed Res, 2012;
26(4):295-302
Duraisamy Gomathi, Manokaran Kalaiselvi, Ganesan Ravikumar, Dominic Sophia,
Velliyur Kanniappan Gopalakrishnan, Chandrasekar Uma
Department of Biochemistry, Karpagam University, Coimbatore 641021, India.
Abstract: Plants and plant-based products are the bases of many modern
pharmaceuticals that are current in use today for various diseases. The aim of the
study was to investigate the biochemical constituents and high performance thin layer
chromatography (HPTLC) finger printing of the ethanolic extract of Evolvulus
alsinoides. Phytochemical screening was done by standard procedures and HPTLC
method was also established to analyze alkaloids, flavonoids and phenolic compounds
from the ethanolic extract of Evolvulus alsinoides. Preliminary phytochemical
screening showed that ethanol extracted more secondary metabolites than other
solvents. HPTLC fingerprinting analysis showed the presence of various alkaloids,
flavonoids and phenols (quercetin) in the ethanolic extract. It can be concluded that
Evolvulus alsinoides may serve as a source of potent antioxidants that may be used in
the prevention of various diseases such as cancer, diabetes and cardiovascular
diseases due to the presence of phenolic compounds. HPTLC finger print of
Evolvulus alsinoides may be useful in the differentiation of the species from
adulterants and act as a biochemical marker for this medicinally important plant in the
pharmaceutical industry and plant systematic studies.
http://www.jbr-pub.org/ch/reader/view_abstract.aspx?file_no=JBR120410&flag=1