A B S T R A C TA phytochemical investigation of the ethanol extract of Toona sinensis (A. Juss.) Roem resulted in the isolation of ten new limonoids, toonasinenines A-J (1-10), together with two known compounds, toonafolin (11) and toonacilianin D (12). Their structures were determined by spectroscopic analyses. The isolated components were evaluated in vitro for radical scavenging potential using ABTS ·+ and DPPH test, anti-inflammatory activities for Cox-1 and Cox-2, and cytotoxicies against nine tumour cell lines (A549, BGC-823, CHG-5, HCT15, HeLa, HepG2, MDA-MB-231, SHG-44 and SGC-7901 cells). As a result, 4, 5 and 7-10 showed potent radical scavenging activities, while limonoids 1-4 and 11 exhibited significant antiinflammatory and cytotoxic potential.
It is well known that liver cancer is a highly aggressive malignancy with poor prognosis. Andrographolide (AD), a major bioactive component of Andrographis paniculata (Burm. F.), is a potential anti-cancer pharmacophore and the synthesis of AD derivatives with better cytotoxicity to cancer cells has attracted considerable attentions. In the present study, we evaluated the in vivo inhibitory effects of ADN-9, a 15-benzylidene substituted derivative of AD, on the growth and metastasis of murine hepatoma H22 using an orthotopic xenograft model and a subcutaneous xenograft model, and we further studied the anti-angiogenic action and the related mechanisms of ADN-9 in vivo and in vitro. Importantly, ADN-9 remarkably suppressed the growth and metastasis of both orthotopic and subcutaneous xenograft tumors, and the serum AFP level in orthotopic hepatoma-bearing mice treated with 100mg/kg ADN-9 (ig.) was decreased to the normal level. We also found that ADN-9 showed stronger abilities than AD in shrinking tumors, suppressing the invasion and metastasis of H22 cells, decreasing the MVD and promoting tumor cell apoptosis in subcutaneous xenograft of mice. Additionally, ADN-9 exhibited stronger inhibitory activity than AD against the migration and VEGF-induced capillary-like tube formation in HUVECs, which was further proved to be associated with attenuating VEGF/VEGFR2/AKT signaling pathway. The present research provides the first evidence that a 15-substituted AD derivative is more promising than the parent compound in therapeutic treatment of liver cancer.
Untargeted detection of protein adulteration in Chinese yogurt was performed using near-infrared (NIR) spectroscopy and chemometrics class modelling techniques. sixty yogurt samples were prepared with pure and fresh milk from local market, and 197 adulterated yogurt samples were prepared by blending the pure yogurt objects with different levels of edible gelatin, industrial gelatin, and soy protein powder, which have been frequently used for yogurt adulteration. A recently proposed one-class partial least squares (OCPLS) model was used to model the NIR spectra of pure yogurt objects and analyze those of future objects. To improve the raw spectra, orthogonal projection (OP) of raw spectra onto the spectrum of pure water and standard normal variate (SNV) transformation were used to remove unwanted spectral variations. The best model was obtained with OP preprocessing with sensitivity of 0.900 and specificity of 0.949. Moreover, adulterations of yogurt with 1% (w/w) edible gelatin, 2% (w/w) industrial gelatin, and 2% (w/w) soy protein powder can be safely detected by the proposed method. This study demonstrates the potential of combining NIR spectroscopy and OCPLS as an untargeted detection tool for protein adulteration in yogurt.
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