Antitumor and Immunomodulatory Effect of Gastrodia elata on Colon Cancer In Vitro and In Vivo.

Gastrodia elata Blume (GE) is a well-known kind of herb that has been used in traditional medicine for thousands of years. The extrusion of raw materials from it could improve flavor and enhance bioavailability in food and drug development. The purpose of this study is to investigate antitumor and immune boosting effects of extruded GE in human colon carcinoma cells, splenocytes, and mice-bearing CT26 colon carcinoma cell. Treatment with 100[Formula: see text][Formula: see text]g/mL of extruded GE decreased cell viability and induced the expression of Caspase-3 and Bax in HT29 cells ([Formula: see text]). When we performed DAPI staining, apoptotic bodies with condensed chromatin and fragmented nuclei, known as indicative of apoptotic morphology, increased 24[Formula: see text]h after treatment with 100[Formula: see text][Formula: see text]g/mL of extruded GE. Treatments with extruded GE significantly promoted splenocyte proliferation and IL-2 or IFN-[Formula: see text] secretion, compared with that of control cells ([Formula: see text]). The administration of extruded GE of 200 mg/kg/day decreased tumor growth and Ki-67 or [Formula: see text]-catenin expression in mice ([Formula: see text]). Additionally, we investigated the contents of compounds in extruded GE extracts using ultra performance liquid chromatography. The contents of p-hydroxylbenzyl alcohol and p-hydroxybenzaldehyde in extruded GE were 2.97[Formula: see text]mg/g and 0.04[Formula: see text]mg/g, respectively. It was supposed that antitumor and immunomodulatory effects of extruded GE might exert by the p-hydroxylbenzyl alcohol and p-hydroxybenzaldehyde of many compositions analyzed from extruded GE. These results suggest that extruded GE have the potential to be developed into a natural pharmaceutical and functional food as a cancer chemopreventive agent.

Antithrombotic activity of Vitis labrusca extract on rat platelet aggregation.

Vitis labrusca is a grapevine that has antioxidant, neuroprotective, hepatoprotective, and anticarcinogenic activity. However, the antithrombotic effect of Vitis labrusca leaves on platelets is yet to be ascertained. We investigated the inhibitory effect of V. labrusca leaf extract (VLE) on platelet aggregation in vitro and ex vivo. The thromboxane B2 (TXB2) and serotonin concentrations were measured by ELISA. The flavonoids content was measured by ultraperformance liquid chromatography (UPLC). The antithrombotic activity of VLE was evaluated using various agonists in vitro. VLE strongly inhibited adenosine diphosphate (ADP)-induced platelet aggregation. In rats, VLE treatment (100 mg/kg) reduced ADP-stimulated platelet aggregation, without affecting tail bleeding and coagulation time. Moreover, VLE significantly suppressed TXB2 and serotonin secretion. UPLC analysis indicated that VLE contains quercetin, isorhamnetin, and rutin. Our results indicate that VLE possesses antiplatelet activity via the suppression of TXB2 and serotonin, without affecting bleeding. Further, we identified the flavonoids present in VLE. Thus, VLE may be a potential agent for the prevention of cardiovascular diseases.

Anti-obesity effect of Triticum aestivum sprout extract in high-fat-diet-induced obese mice.

Obesity is a common disease worldwide that often results in serious conditions including hypertension, diabetes, and hyperlipidemia. Many herbal medicines have been examined with regard to ameliorating obesity. We investigated the anti-obesity effects of 50% EtOH extract of Triticum aestivum sprout (TAEE) in high-fat-diet (HFD)-induced obese mice. TAEE administration (10, 50, or 200 mg/kg) for 6 weeks significantly decreased the body weights, serum total cholesterol (TC), and low-density lipoprotein cholesterol levels in HFD-fed mice. TAEE treatment reduced lipid accumulation in epididymal white adipose tissue (EWAT) and liver. Moreover, TC and lipid levels were decreased by TAEE treatment in liver. Serum leptin and adiponectin concentrations were reduced by TAEE treatment. TAEE-treated mice showed decreases in peroxisome proliferator-activated receptor γ (PPARγ) and fatty acid synthase expression in EWAT. Furthermore, TAEE administration elevated levels of PPARα protein in the liver of HFD-induced obese mice. These results suggest that TAEE supplementation might be beneficial for the treatment and prevention of obesity and related diseases.

Sterols from Hericium erinaceum and their inhibition of TNF-α and NO production in lipopolysaccharide-induced RAW 264.7 cells.

Erinarols G-J and 10 known ergostane-type sterols were isolated from a methanol extract of the dried fruiting bodies of Hericium erinaceum. Their chemical structures were elucidated using extensive spectroscopic analyses including 1D and 2D NMR experiments and HR-ESI-MS analysis, as well as through comparison with previously reported data. Anti-inflammatory effects of the isolated compounds were evaluated in terms of inhibition of tumor necrosis factor α (TNF-α) and nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophage cells. The results showed that erinarols H and J, as well as 2 of the ergostane-type sterols exhibited inhibitory activity against TNF-α secretion, with inhibition values ranging from 33.7% to 43.3% at 10 µM. Erinarols J and three ergostane-type sterols exhibited significant inhibitory effects against NO production, with inhibition values ranging from 38.4% to 71.5% at 10 µM.

Chloroform fraction of Euphorbia maculata has antiplatelet activity via suppressing thromboxane B2 formation.

Euphorbia maculata (EM) is a traditionally used antidiarrheal, antibacterial, antifungal and antioxidant agent. However, the effects of EM on platelet activity remain to be elucidated. Therefore, the present study investigated the antiplatelet effect of various EM extract fractions on platelet aggregation in rats. The antiplatelet activity of the EM fractions on collagen or adenosine diphosphate (ADP)­induced platelet aggregation was evaluated in vitro and ex vivo. Thromboxane B2 (TXB2) formation, rat­tail bleeding time and coagulation time were also measured. Among the fractions, the chloroform fraction of EM (CFEM) significantly inhibited ADP­induced platelet aggregation in vitro. Furthermore, oral administration of 50 mg/kg CFEM to rats significantly reduced ADP­induced platelet aggregation without increasing the tail bleeding time or coagulation time. In addition, EM significantly inhibited the level of TXB2 formation in a dose­dependent manner. These results suggest that CFEM exhibits antiplatelet activity, without causing bleeding, via the suppression of TXB2 formation. CFEM may be a type of food which has the potential for preventing cardiovascular disease.

Inhibitory effect of kyungohkgo in the development of 2,4-dinitrochlorobenzene-induced atopic dermatitis in NC/Nga mice.

Kyungohkgo (KOG) is one of the most important formulas in traditional oriental medicine. We investigated the remedial effect of KOG on the development of atopic dermatitis (AD) in female NC/Nga mice. AD-like lesion was induced by the application of 2,4-Dinitrochlorobenzene on to the back skin repeatedly; KOG was administered orally (12.5 and 25.0 mg/kg) and topically (0.5 and 1.0 mg/mouse) to NC/Nga mice once a day for all through the period of this experiment and every mouse body weight was periodically taken. The effects of KOG on 2,4-Dinitrochlorobenzene-treated NC/Nga mice were determined by measuring AD-like skin lesions, the infiltration of mast cells and serum immunoglobulin E concentration. After the KOG applications are over, the KOG groups had less skin lesions than the atopy one, their immunoglobulin E levels were significantly downregulated and the infiltration of mast cells in the dorsal skin were reduced. Our results suggest that KOG may be effective in alleviating the development of AD. The inhibition of AD in NC/Nga mice may be influenced by the prevention of mast cell activation.

Nafamostat mesilate attenuates colonic inflammation and mast cell infiltration in the experimental colitis.

Serine proteases are important in the pathogenesis of intestinal inflammation. Recent studies have shown that nafamostat mesilate (NM) can inhibit the colonic mucosal inflammation induced by TNBS in rats. The aim of this study was to investigate the anti-inflammatory effects of NM on a DSS-induced colitis. Colitis was induced in female BALB/c mice by 5% dextran sulfate sodium (DSS) for 6 days. NM (2 or 20mg/kg body weight) was orally administered once a day for 6 days during treatment of the mice with DSS. The inflammatory response of the colon was assessed 1 week after DSS treatment. NM at a high dose, but not at a low dose significantly decreased disease activity index (DAI) and myeloperoxidase (MPO) induced by DSS. Furthermore, NM (20mg/kg) inhibited the production of tumor necrosis factor (TNF)-α, cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) in the colonic tissues treated with DSS. The increase in chymase activity by DSS treatment was also attenuated by the administration of NM (20mg/kg). NM (20mg/kg) significantly decreased the colonic mucosal injury and the infiltrated mast cell number induced by DSS. These results indicate that NM might inhibit the colonic inflammation through inhibition of both chymase activity and mast cell infiltration in colon tissues of DSS-induced colitis.