ABSTRACT: Numerous studies have documented that in cancer therapy flavonoids extracted from traditional Chinese medicine have anti-tumor activity or can enhance efficiency of chemotherapy in combination with chemotherapeutics. Thus, an awareness of flavonoids is needed by physicians and medical researchers. This review provides evidence about anti-hepatocellular carcinoma activity of flavonoids. First, as a common employed in vitro model, profile of HepG2 is shown. Second, the intracellular signaling pathways induced by flavonoids which inhibit the HepG2 cell line are summarized. Third, study situation of anti-HBV/HCV activity of flavonoids is shown. Our review is aimed at providing an understanding of anti-HBV/HCV activity and anti-HCC mechanisms of flavonoids, and an outlook on flavonoids application on cancer therapy.
Liquid chromatography coupled with electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS) has been frequently utilized for the sensitive and selective determination of the trace level compounds in biological samples. In LC/ESI-MS/MS, chemical derivatization is sometimes used to enhance the detection sensitivity of the analytes. This review presents an overview of the derivatization reagents in LC/ESI-MS/MS that have been applied to the low molecular weight compounds in recent five years (2008-2012).
The aim of the present study was to evaluate the anxiolytic effects of the ethanol extract of Cirsium japonicum (CJ) in mice. The extract was orally administered at dosages of 50, 100, 200, or 400 mg/kg of body weight. The CJ-induced behavioral changes were assessed using the open-field and elevated-plus maze test. The ethanol extract of CJ did not affect overall locomotor activity of mice in the open-field test, however, it showed increase exploration in the unprotected center zone, which is thought to reflect anxiolyticlike effects. Furthermore, the CJ extract (100 and 200 mg/kg) significantly increased the percentage of time spent in the open arms of the elevated plus-maze, indicating the anxiolytic effects of the substance. This anxiolytic effects of the extract were comparable to that of the benzodiazepine, diazepam. To further characterize the anxiolytic activities of CJ, its action on human neuroblastoma cells were assessed. The CJ extract dose-dependently increased chloride ion (Cl‒) influx, which was blocked by co-administration of the GABAA receptor competitive antagonist, bicuculline, suggesting a GABAA receptor – Cl‒ channel mechanism of action. Taken altogether, the present study demonstrates that the ethanol extract of CJ has anxiolytic effects, probably mediated through GABAergic neurotransmission.
Two new chalcones, artocarpusins A and B (1 and 2), one new flavone, artocarpusin C (3), one new 2-arylbenzofuran derivative, artocarstilene A (4), and 15 flavonoids were isolated from the twigs of Artocarpus heterophyllus. Their structures were established on the basis of extensive spectroscopic analysis. Compounds 9 and 16 showed moderate inhibitory activity on the proliferation of the PC-3 and H460 cell lines.
There is an increasing evidence that the oncogenic kinase PAK1 is responsible not only for malignant transformation, but also for several other diseases such as inflammatory diseases (asthma and arthritis), infectious diseases including malaria, AIDS, and flu, as well as a series of neuronal diseases/disorders (neurofibromatosis, tuberous sclerosis, Alzheimer's diseases, Huntington's disease, epilepsy, depression, learning deficit, etc.) which often cause premature death. Interestingly, a few natural PAK1-blockers such as curcumin, caffeic acid (CA) and rosmarinic acid (RA) extend the lifespan of the nematode Caenorhabditis elegans or fruit flies. Here, to explore the possibility that C. elegans could provide us with a quick and inexpensive in vivo screening system for a series of more potent but safe (non-toxic) PAK1-blocking therapeutics, we examined the effects of PAK1-deficiency or down-regulation on a few selected functions of this worm, including reproduction, expression of HSP16.2 gene, and lifespan. In short, we found that PAK1 promotes reproduction, whereas it inactivates HSP16.2 gene and shortens lifespan, as do PI-3 kinase (AGE-1), TOR, and insulin-like signalling /ILS (Daf-2) in this worm. These findings not only support the "trade-off" theory on reproduction versus lifespan, but also suggest the possibility that the reduced reproduction (or HSP16.2 gene activation) of this worm could be used as the first indicator of extended lifespan for a quick in vivo screening for PAK1-blockers.
We aimed to assess the efficacy and safety of concurrent capecitabine and cisplatin over concurrent cisplatin and 5-flurouracil (5-FU) in locally advanced squamous cell carcinoma of the head and neck. One hundred and fifty-three patients (all of whom had stage III or IV unresectable disease with no distant metastases and who had received two cycles of taxol and cisplatin chemotherapy) were randomly assigned to receive either concurrent cisplatin (75 mg/m2 in day 1 and 2) and 5-FU (750 mg/m2 in day 1, 2, and 3) from the first day of radiotherapy at an interval of 3 weeks (Arm I) or cisplatin (75 mg/m2 in day 1 and 2) and capecitabine (750 mg/m2 in two divided doses from day 1-14) from the first day of radiotherapy at a 3-week interval (Arm II). Results showed that patients in Arm II had a significantly better rate of complete response, fewer nodes, and better overall response compared to those in Arm I. The two groups had a similar 3-year disease-free survival, progression-free survival, and overall survival, i.e. they did not differ significantly. Variables indicating the quality of life of the two groups were compared. Patients in Arm II had a significantly higher quality of life compared to those in Arm I. The two groups had similar treatment-related acute and late toxicity, i.e. they did not differ significantly. These results have thoroughly substantiated the contention that concurrent chemoradiation with capecitabine and cisplatin may be regarded as an effective and well-tolerated regimen in the treatment of the patients with locally advanced head and neck cancer.
A case of idiopathic dilated cardiomy-opathy with an arrhythmic storm refractory to the usual antiarrhythmic therapy will be reported. The idiopathic structural heart disease of the patient is a vulnerable anatomic substrate in itself, for electrical instability and reentry mechanism, because of heterogeneous areas of scarred myocardium and low left ventricle ejection fraction. In this case, the ranolazine administration was safe and effective for the prevention of further electrical storms.