Characterization of the antioxidative polysaccharides from Ziziphus jujube cv. Goutouzao and its tumor-inhibitory effects on human colorectal carcinoma LoVo cells via immunocyte activation.

Colorectal cancer, the most common malignancy in Asian and west world, is listed as the fourth lethal neoplastic disease with increasing incidence worldwide. Recently, Ziziphus jujube were reported with hepatoprotective, antihypertensive, and hypoglycemic functions. The polysaccharides from Ziziphus jujube was considered as the main component for these bioactivities. In this study, polysaccharides from Ziziphus jujube cv. Goutouzao (GZSP) was comprehensively investigated, and characterized as a heteropolysaccharide with antioxidant activity. Besides, it can stimulate the viability of immune cells RAW 264.7, which in turn inhibited the proliferation of colorectal carcinoma cells (LoVo) by inducing apoptosis, arresting cell cycle in G0/G1, and increasing intracellular ROS, as demonstrated by Flow Cytometric analyses. The results suggest that, different from chemotherapeutic modalities, GZSP can exert antitumor effects by activating immune reaction, providing more evidence for the development of GZSP-based functional foods and anticancer drugs serving as human colon cancer prevention. PRACTICAL APPLICATIONS: Natural products from medicinal and edible plant are great sources of phytochemicals beneficial to human health, such as tea polyphenols, carotenoids, and phytosterols, etc. In this study, GZSP, the polysaccharides from a well-received fruit, Ziziphus jujube cv. Goutouzao, has been comprehensively investigated. The results show that GZSP fights against free radicals commonly found in human circulation, a property that enables it to be used as an antioxidant food additive with jujube flavor. More importantly, GZSP impedes neoplastic progression by activating immune response, as evidenced by the inhibition of colorectal carcinoma (LoVo) cells. Comparing with chemotherapies usually imposing cytotoxicity on normal tissues, natural product GZSP is able to exert the antiproliferative effects on carcinoma cells with minimal side-effects. Therefore, GZSP-based functional foods and anticancer drugs with the purpose of preventing human colon cancer formation are promising to be developed.

Ethnomedicinal Uses, Phytochemistry, Pharmacology, and Toxicology of Species from the Genus Ajuga L.: A Systematic Review.

The present review is aimed at providing a comprehensive summary of the botanical characteristics, ethnomedicinal uses, phytochemical, pharmacological, and toxicological studies of the genus Ajuga L. The extensive literature survey revealed Ajuga L. species to be a group of important medicinal plants used for the ethnomedical treatment of rheumatism, fever, gout, sclerosis, analgesia, inflammation, hypertension, hyperglycemia, joint pain, palsy, amenorrhea, etc., although only a few reports address the clinical use and toxicity of these plants. Currently, more than 280 chemical constituents have been isolated and characterized from these plants. Among these constituents, neo-clerodane diterpenes and diterpenoids, phytoecdysteroids, flavonoids, and iridoids are the major bioactive compounds, possessing wide-reaching biological activities both in vivo and in vitro, including anti-inflammatory, antinociceptive, antitumor, anti-oxidant, antidiabetic, antimicrobial, antifeedant, antidiarrhoeal, hypolipidemic, diuretic, hypoglycaemic, immunomodulatory, vasorelaxant, larvicidal, antimutagenic, and neuroprotective activity. This review is aimed at summarizing the current knowledge of the ethnomedicinal uses, phytochemistry, biological activities, and toxicities of the genus Ajuga L. to reveal its therapeutic potentials, offering opportunities for future researches. Therefore, more focus should be paid to gathering information about their toxicology data, quality-control measures, and the clinical application of the bioactive ingredients from Ajuga L. species.

Phenylethanoid glycosides of Phlomis younghusbandii Mukerjee ameliorate acute hypobaric hypoxia-induced brain impairment in rats.

High altitude cerebral edema (HACE), whose development process is associated with oxidative stress and inflammatory response, is a life-threatening condition caused by rapid ascent speed to high altitudes. Phenylethanoid glycosides (PhGCs) are primary active constituents isolated from Phlomis younghusbandii Mukerjee that reportedly exhibit potent anti-oxidant and anti-inflammatory activities. The present study aims to investigate the protective effect of phenylethanoid glycosides (PhGCs) from P. younghusbandii in acute hypobaric hypoxia (AHH) - stimulated HACE rats and its underlying mechanisms. The expression of pro-inflammatory cytokine levels (IL-1ß, TNF-α, and IL-6) was detected by RT-PCR and ELISA at mRNA and protein levels in brain tissues. Western blotting was carried out to measure the major protein levels (IL-1ß, TNF-α, and NF-κB) in brain tissues. The oxidative stress biomarkers (MDA, SOD, and GSH) were evaluated using kits. Results demonstrate that PhGCs significantly improved pathological changes in brain tissues, reduced the brain's water content, and attenuated the production and mRNA expression of pro-inflammatory cytokines. Furthermore, the increased oxidative stress and the decrease in anti-oxidant stress system under the AHH condition were also abrogated reversely through PhGCs treatment by elevating the levels of SOD and GSH and suppressing the accumulation of MDA. Simultaneously, there was also a significant reduction in NF-κB, IL-1ß, and TNF-α protein expression levels in brain tissues, suggesting that blocking the NF-κB signaling pathway activation prevented the production of pro-inflammatory cytokines. Taken together, these findings indicate that PhGCs may afford a protectively intervene in HACE through the suppression of oxidative stress and inflammatory response via the inhibition of the NF-κB signaling pathway, indicating that PhGCs are promising agents for the treatment of acute HACE.

Chemical composition and hepatoprotective effects of polyphenol-rich extract from Houttuynia cordata tea.

This study was designed to investigate the antioxidant activity, hepatoprotective effect, and phenolic composition of the ethyl acetate fraction (EAF) extracted from Houttuynia cordata tea. EAF was shown to exhibit strong ferric-reducing antioxidant power (FRAP) and scavenging activity against DPPH radical in vitro, and the antioxidant effects were further verified by suppressing CCl4-induced oxidative stress in mouse liver at three tested doses of EAF (250, 500, and 1000 mg/kg bw). Pretreatment with EAF (1000 mg/kg bw) prior to CCl4 administration significantly (p < 0.001) decreased the CCl4-elevated levels of serum AST, ALT, alkaline phosphatase, total bilirubin, and hepatic MDA in mice and prevented the increases in GSH, SOD, and CAT caused by CCl4. HPLC analysis revealed that three predominantly polyphenolic compounds present in EAF were quercitrin (111.7 µg/mg), quercetin (43.8 µg/mg), and hyperoside (29.1 µg/mg). These results combined with liver histopathology indicate that EAF possesses a significant protective effect against acute hepatotoxicity induced by CCl4, which may be due to the strong antioxidant activity of phenolic components.

Antitumor activities of quercetin and quercetin-5',8-disulfonate in human colon and breast cancer cell lines.

This study is designed to compare the anticancer effects of quercetin and its water-soluble sulfated derivative, quercetin-5',8-disulfonate (QS), in human colon cancer LoVo cells and breast cancer MCF-7 cells. It was found that both quercetin and QS can inhibit the growth of cancer cells in a dose-dependent manner, with the IC(50) values of 40.2 and 28.0 µM for LoVo cells and 30.8 and 19.9 µM for MCF-7 cells, respectively, suggesting QS was more effective against the cancer cells than quercetin. Moreover, flow cytometric assay revealed that quercetin and QS could mediate the cell-cycle arrest principally in the S phase after 24h of treatment with the two tumor cells. It was also found that 69.6% of LoVo cells and 90.6% of MCF-7 cells entered the early phase of apoptosis when treated with 100 µM QS for 48 h. Furthermore, we firstly found the generation of ROS is a critical mediator in QS-induced cell growth inhibition. Taken together, the novel sulfated derivative of quercetin possesses strong antitumor activity via a ROS-dependent apoptosis pathway, and has the excellent potential to be developed into an antitumor precursor compound.