Phenolic-rich feijoa extracts from flesh, peel and whole fruit activate apoptosis pathways in the LNCaP cell line.

This study aimed to explore the potential anticancer activity of phenolic-rich feijoa extracts from the flesh, peel, and whole fruit on the human prostate cancer cell line (LNCaP). Results showed that feijoa extracts had cancer-specific anti-proliferative activity on the LNCaP cell line. The anticancer activity of feijoa extracts was shown through activation of the caspase-dependent apoptosis pathway based on the increase of sub-G1 phase in the cell cycle, the decrease of mitochondrial membrane potential, as well as the elevated caspase 3, 8, and 9 activity in the treated LNCaP cells. The anti-cancer activity of feijoa extracts could be attributed to the high total phenolic contents (0.14-0.37 mg GAE/mg dw) and, in particular, the high ellagic acid content (2.662-9.119 µg/mg dw). The successful activation of the caspase-dependent apoptosis pathway indicates that phenolic-rich feijoa extracts have a good potential to be utilized as a functional ingredient in foods and nutraceuticals.

Screening of Cytotoxicity and Anti-Inflammatory Properties of Feijoa Extracts Using Genetically Modified Cell Models Targeting TLR2, TLR4 and NOD2 Pathways, and the Implication for Inflammatory Bowel Disease.

Feijoa has been increasingly studied in the recent decade, while investigations into its bioactivities including anti-inflammatory activity are lacking. In this article, the cytotoxicity and anti-inflammatory properties of feijoa extracts, from flesh, peel and whole fruit, from four cultivars namely APOLLO, UNIQUE, OPAL STAR and WIKI TU are presented. Three inflammatory pathways, Toll-like receptor 2 (TLR2), TLR4 and nucleotide-binding oligomerization domain-containing protein 2 (NOD2), were investigated using genetically modified cell models namely HEK-Blue™ hTLR2, HEK-Blue™ hTLR4, NOD2-WT and NOD2-G908R. Results show that feijoa peel extract induced higher cytotoxicity than flesh and whole fruit extracts, and the APOLLO cultivar was the most anti-inflammatory among the four tested cultivars. The anti-inflammatory activity of feijoa flesh was detected only through the TLR2 pathway, and the activity of feijoa peel and whole fruit was evident mainly through the TLR2 and NOD2 pathways. Most notably, feijoa anti-inflammatory activity was superior to ibuprofen particularly through the TLR2 pathway, with significantly lower secreted embryonic alkaline phosphatase IC50 concentrations (7.88, 12.81, 30.84 and 442.90 µg/mL for APOLLO flesh, peel, whole fruit extract and ibuprofen respectively). These findings indicate that feijoa has great potential to be used in the treatment and prevention of inflammation-related diseases including inflammatory bowel disease.

Core bioactive components promoting blood circulation in the traditional Chinese medicine compound xueshuantong capsule (CXC) based on the relevance analysis between chemical HPLC fingerprint and in vivo biological effects.

Compound xueshuantong capsule (CXC) is an oral traditional Chinese herbal formula (CHF) comprised of Panax notoginseng (PN), Radix astragali (RA), Salvia miltiorrhizae (SM), and Radix scrophulariaceae (RS). The present investigation was designed to explore the core bioactive components promoting blood circulation in CXC using high-performance liquid chromatography (HPLC) and animal studies. CXC samples were prepared with different proportions of the 4 herbs according to a four-factor, nine-level uniform design. CXC samples were assessed with HPLC, which identified 21 components. For the animal experiments, rats were soaked in ice water during the time interval between two adrenaline hydrochloride injections to reduce blood circulation. We assessed whole-blood viscosity (WBV), erythrocyte aggregation and red corpuscle electrophoresis indices (EAI and RCEI, respectively), plasma viscosity (PV), maximum platelet aggregation rate (MPAR), activated partial thromboplastin time (APTT), and prothrombin time (PT). Based on the hypothesis that CXC sample effects varied with differences in components, we performed grey relational analysis (GRA), principal component analysis (PCA), ridge regression (RR), and radial basis function (RBF) to evaluate the contribution of each identified component. Our results indicate that panaxytriol, ginsenoside Rb1, angoroside C, protocatechualdehyde, ginsenoside Rd, and calycosin-7-O-ß-D-glucoside are the core bioactive components, and that they might play different roles in the alleviation of circulation dysfunction. Panaxytriol and ginsenoside Rb1 had close relevance to red blood cell (RBC) aggregation, angoroside C was related to platelet aggregation, protocatechualdehyde was involved in intrinsic clotting activity, ginsenoside Rd affected RBC deformability and plasma proteins, and calycosin-7-O-ß-D-glucoside influenced extrinsic clotting activity. This study indicates that angoroside C, calycosin-7-O-ß-D-glucoside, panaxytriol, and protocatechualdehyde may have novel therapeutic uses.

Protective effects of traditional Chinese medicine formula NaoShuanTong capsule on haemorheology and cerebral energy metabolism disorders in rats with blood stasis.

NaoShuanTong capsule (NSTC), an oral traditional Chinese medicine formula, is composed of Pollen Typhae, Radix Paeoniae Rubra, Rhizoma Gastrodiae, Radix Rhapontici and Radix Curcumae. It has been widely used to treat ischemic stroke in clinic for many years in China. In addition to neuronal apoptosis, haemorheology and cerebral energy metabolism disorders also play an important role in the pathogenesis and development of ischemic stroke. The present study was designed to evaluate the in vivo protective effects of NSTC on haemorheology and cerebral energy metabolism disorders in rats with blood stasis. Sixty specific pathogen-free sprague-dawley rats, male only, were randomly divided into six groups (control group, model group, aspirin (100 mg/kg/d) group, NSTC low-dose (400 mg/kg/d) group, NSTC intermediate-dose (800 mg/kg/d) group, NSTC high-dose (1600 mg/kg/d) group) with 10 animals in each. The rats except those in the control group were placed in ice-cold water (0-4 °C) for 5 min during the time interval (4 h) of two adrenaline hydrochloride injections (0.8 mg/kg) to induce blood stasis. After treatment, whole blood viscosity at three shear rates, plasma viscosity and erythrocyte sedimentation rate significantly decreased in NSTC intermediate- and high-dose groups; erythrocyte aggregation index and red corpuscle electrophoresis index significantly decreased in all the three dose NSTC groups. Moreover, treatment with high-dose NSTC could significantly improve Na+-K+ adenosine triphosphatase (ATPase) and Ca2+ ATPase activity, as well as lower lactic acid level in brain tissues. These results demonstrated the protective effects of NSTC on haemorheology and cerebral energy metabolism disorders, which may provide scientific information for the further understanding of mechanism(s) of NSTC as a clinical treatment for ischemic stroke. Furthermore, the protective effects of activating blood circulation as observed in this study might create valuable insight for the utilisation of NSTC to be a feasible alternative therapeutic agent for patients with blood stasis.