Siraitia grosvenorii fruit (SGF) has been used as a natural sweetener and traditional medicine in China for more than two centuries. This study evaluated the effect of SGF extract supplementation (0.5%, 1%, and 2%) on the chemical, microbial and sensory properties of probiotic yogurt. The antioxidant, angiotensin-converting-enzyme inhibitory (ACE-I) and antibacterial bioactivities were determined. SGF extract supplementation improved some of the chemical and physicochemical characteristics. Probiotic yogurt with the fruit extract had significantly more Lactobacillus casei and Lactobacillus bulgaricus, whereas there was no significant effect on the number of Streptococcus thermophiles. The bioactivities were significantly increased by SGF extract supplementation. Probiotic yogurt with 2% SGF extract showed the highest antioxidant, ACE-I, and antibacterial activities, whereas the one with 1% SGF extract conferred the highest sensory attributes score. Overall, SGF extract offers a promising option as a dietary supplement to produce novel dairy products that have high nutritional and bioactivity values.

Organic fractions and extracts of willow () leaves, produced by sequential solvent extraction as well as infusion and decoction, exhibited anticancer potencies in four cancerous cell lines, including breast (MCF-7), colorectal (HCT-116), cervical (HeLa) and liver (HepG2). Results of the MTT assay revealed that chloroform (CHCl) and ethyl acetate (EtOAc)-soluble fractions exhibited specific anticancer activities as marginal toxicities were observed against two non-cancerous control cell lines (BJ-1 and MCF-12). Ultra-high-resolution mass spectrometry Q-Exactive™ HF Hybrid Quadrupole-Orbitrap™ coupled with liquid chromatography (UHPLC) indicated that both extracts are enriched in features belonging to major phenolic and purine derivatives. Fluorescence-activated cell sorter analysis (FACS), employing annexin V-FITC/PI double staining indicated that the observed cytotoxic potency was mediated via apoptosis. FACS analysis, monitoring the increase in fluorescence signal, associated with oxidation of DCFH to DCF, indicated that the mechanism of apoptosis is independent of reactive oxygen species (ROS). Results of immunoblotting and RT-qPCR assays showed that treatment with organic fractions under investigation resulted in significant up-regulation of pro-apoptotic protein and mRNA markers for Caspase-3, p53 and Bax, whereas it resulted in a significant reduction in amounts of both protein and mRNA of the anti-apoptotic marker Bcl-2. FACS analysis also indicated that pre-treatment and co-treatment of human amniotic epithelial (WISH) cells exposed to the ROS HO with EtOAc fraction provide a cytoprotective and antioxidant capacity against generated oxidative stress. In conclusion, our findings highlight the importance of natural phenolic and flavonoid compounds with unparalleled and unique antioxidant and anticancer properties.

Vinpocetine (VNP), a semisynthetic drug, is utilized for the treatment of cerebrovascular and memory disorders. This work aimed at formulation of biodegradable VNP long-circulating nanoparticles utilizing Polyethylene glycol methyl ether-block-poly lactide-co-glycolide (PEG-PLGA) copolymer to surmount the drug drawbacks including low oral bioavailability and short elimination half-life. VNP nanoparticles were formulated using nanoprecipitation technique. A 2 factorial design was applied to assess the impact of formulation and process variables on the nanoparticles' characteristics. Statistical analysis revealed that nanoparticles size (Y) significantly increased with increasing PEG-PLGA amount (X), poly-vinyl alcohol concentration (X), and PLGA content (X), while decreased with increasing sonication time (X). Furthermore, the entrapment efficiency (Y) was positively affected by both PEG-PLGA amount and PLGA content, while negatively affected by poly-vinyl alcohol concentration. The optimized formulation prepared using 200 mg of PEG-PLGA polymer (PEG: PLGA 2000: 4,500), 0.5% polyvinyl alcohol with sonication time of 60 s achieved spherical shape with particle size of 43 nm and drug entrapment of 82%. A significant bioavailability enhancement of VNP with marked prolongation of the in vivo systemic exposure of the drug and increased brain levels has also been achieved following intraperitoneal administration in Wistar rats. Thus, the optimized formulation could be regarded as a promising stealth nanocarrier that could surmount the drug pitfalls and enhance its brain delivery.