Recent Articles on Andrographis sp.

Chemical Fingerprinting of Andrographis paniculata (Burm. f.) Nees by HPLC and Hierarchical Clustering Analysis

J Chromatogr Sci. 2009 Nov-Dec;47(10):931-5.

Chemical Fingerprinting of Andrographis paniculata (Burm. f.) Nees by
HPLC and Hierarchical Clustering Analysis.

Dong HJ, Zhang ZJ, Yu J, Liu Y, Xu FG.

Key laboratory of Drug Quality Control and Pharmacovigilance (China
Pharmaceutical University), Ministry of Education, Nanjing
210009,China; Center for Instrumental Analysis, China Pharmaceutical
University, Nanjing 210009, China.

The aim is to develop a simple and specific method for the extraction
and chemical fingerprinting of Andrographis paniculata (Burm. f.) Nees
and to apply the method to this drug from different regions.
High-performance liquid chromatographic (HPLC) with gradient elution
is used for developing the fingerprints, and liquid chromatography
electrospray ionization mass spectrometry (LC-ESI-MS) technique is
employed to identify the component of the fingerprints. Nine peaks are
selected as common peaks, and six compounds are elucidated by MS data.
Twenty-three samples of A. paniculata from different regions of China
are collected and detected by HPLC fingerprinting. Comparisons of the
chromatograms show that there are obvious differences in the content
of each component contained between the habitat samples in China. The
results of hierarchical cluster analysis show that these samples can
be clustered reasonably into three groups, and the growth of A.
paniculata and their internal quality are related to their habitat.
The HPLC fingerprint developed allows simple identification of A.
paniculata from many natural drugs.

PMID: 19930808 [PubMed - in process]

The effect of Eurycoma longifolia on sperm quality of male rats

Nat Prod Commun. 2009 Oct;4(10):1331-6.

The effect of Eurycoma longifolia on sperm quality of male rats.

Chan KL, Low BS, Teh CH, Das PK.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800
Penang, Malaysia. klchan@usm.my

The present study investigated the effects of a standardized methanol
extract of E. longifolia Jack containing the major quassinoid
constituents of 13alpha(21)-epoxyeurycomanone (1), eurycomanone (2),
13alpha,21-dihydroeurycomanone (3) and eurycomanol (4) on the
epididymal spermatozoa profile of normal and Andrographis paniculata
induced infertile rats. The standardized MeOH extract at doses of 50,
100 and 200 mg/kg, the EtOAc fraction (70 mg/kg), and standardized
MeOH extract at 200 mg/kg co-administered with the EtOAc fraction of
A. paniculata at 70 mg/kg were each given orally to male
Sprague-Dawley albino rats for 48 consecutive days. The spermatozoa
count, morphology, motility, plasma testosterone level and Leydig cell
count of the animals were statistically analyzed by ANOVA with a
post-hoc Tukey HSD test. The results showed that the sperm count of
rats given the standardized MeOH extract alone at doses of 50, 100 and
200 mg/kg were increased by 78.9, 94.3 and 99.2%, respectively when
compared with that of control (p < 0.01). The low count, poor motility
and abnormal morphology of the spermatozoa induced by the A.
paniculata fraction were significantly reversed by the standardized
MeOH extract of E. longifolia (p < 0.001). The plasma testosterone
level of the rats treated with the standardized MeOH extract at 200
mg/kg was significantly increased (p < 0.01) when compared with that
of the control and infertile animals. The spermatocytes in the
seminiferous tubules and the Leydig cells appeared normal.
Testosterone level was significantly higher in the testes (p < 0.01)
than in the plasma after 30 days of oral treatment with the
standardized MeOH extract. Interestingly, eurycomanone (2) alone was
detected in the rat testis homogenates by HPLC-UV and confirmed by
LC/MS, and may have contributed towards the improvement of sperm
quality. Thus, the plant may potentially be suitable for the
management of male infertility.

PMID: 19911566 [PubMed - in process]

Benzylidene derivatives of andrographolide inhibit growth of breast and colon cancer cells in vitro by inducing G1 arrest and apoptosis

Benzylidene derivatives of andrographolide inhibit growth of breast and colon cancer cells in vitro by inducing G1 arrest and apoptosis

S R Jada, C Matthews, M S Saad, A S Hamzah, N H Lajis, M F G Stevens, and J Stanslas

Br J Pharmacol. 2008 November; 155(5): 641–654. Published online 2008 September 22. doi: 10.1038/bjp.2008.368.

Background and purpose:
Andrographolide, the major phytoconstituent of Andrographis paniculata, was previously shown by us to have activity against breast cancer. This led to synthesis of new andrographolide analogues to find compounds with better activity than the parent compound. Selected benzylidene derivatives were investigated for their mechanisms of action by studying their effects on the cell cycle progression and cell death.

Experimental approach:
Microculture tetrazolium, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and sulphorhodamine B (SRB) assays were utilized in assessing the in vitro growth inhibition and cytotoxicity of compounds. Flow cytometry was used to analyse the cell cycle distribution of control and treated cells. CDK1 and CDK4 levels were determined by western blotting. Apoptotic cell death was assessed by fluorescence microscopy and flow cytometry.

Key results:
Compounds, in nanomolar to micromolar concentrations, exhibited growth inhibition and cytotoxicity in MCF-7 (breast) and HCT-116 (colon) cancer cells. In the NCI screen, 3,19-(2-bromobenzylidene) andrographolide (SRJ09) and 3,19-(3-chloro-4-fluorobenzylidene) andrographolide (SRJ23) showed greater cytotoxic potency and selectivity than andrographolide. SRJ09 and SRJ23 induced G1 arrest and apoptosis in MCF-7 and HCT-116 cells, respectively. SRJ09 downregulated CDK4 but not CDK1 level in MCF-7 cells. Apoptosis induced by SRJ09 and SRJ23 in HCT-116 cells was confirmed by annexin V-FITC/PI flow cytometry analysis.

Conclusion and implications:
The new benzylidene derivatives of andrographolide are potential anticancer agents. SRJ09 emerged as the lead compound in this study, exhibiting anticancer activity by downregulating CDK4 to promote a G1 phase cell cycle arrest, coupled with induction of apoptosis.

Keywords: andrographolide derivatives, antitumour, cell cycle, G1 arrest, NCI cell lines, CDK-4, apoptosis, v-Src

PMCID: PMC2584933