Dimeric 1,4-benzoquinone Derivatives with Cytotoxic Activities from the Marine-Derived Fungus Penicillium sp. L129.

Two new dimeric 1,4-benzoquinone derivatives, peniquinone A (1) and peniquinone B (2), a new dibenzofuran penizofuran A (3), and a new pyrazinoquinazoline derivative quinadoline D (4), together with 13 known compounds (5-17), were isolated from a marine-derived fungus Penicillium sp. L129. Their structures, including absolute configurations, were elucidated by extensive spectroscopic data and electronic circular dichroism calculations. Compound 1 exhibited cytotoxicity against the MCF-7, U87 and PC3 cell lines with IC50 values of 12.39 µM, 9.01 µM and 14.59 µM, respectively, while compound 2 displayed relatively weak cytotoxicity activities against MCF-7, U87 and PC3 cell lines with IC50 values of 25.32 µM, 13.45 µM and 19.93 µM, respectively. Furthermore, compound 2 showed weak quorum sensing inhibitory activity against Chromobacterium violaceum CV026 with an MIC value of 20 µg/well.

[Protective effects of total epimedium flavonoids against QA-induced toxicity in SH-SY5Y cells].

OBJECTIVE: To investigate the protective effects and its mechanisms of total epimedium flavonoids (TEF) against Quindinince acid (QA)-induced toxicity in SH-SY5Y cells. METHODS: The MT assay was used to detect the toxicity of QA and the cell viability of pretreatment of TEF and co-incubation with QA in SH-SY5Y cells; Cell apoptosis was observed by Hochest33258 staining; SOD and GSH-Px activities as well as MDA content were measured by colorimetric method; The mitochondrial membrane potential (delta psi m) and intracellular free calcium concentration ([Ca2+]i) were monitored by FCM. RESULTS: TEF increased the cell viability of SH-SY5Y cells, reduced apoptosis cells significantly, improved SOD and GSH-Px activities, decreased MDA content, increased the mitochondrial membrane potential and reduced intracellular free calcium concentration( [Ca2+]i ). CONCLUSION: TEF has significant protective effects against QA-induced toxicity in SH-SY5Y cells,the action mechanism may be associated with resisting oxidative stress, decreasing the [Ca2]i and up-regulating delta psi m.

[Multicentric randomized double blinded clinical study of Yiqi Tongmai Oral Liquid against angina pectoris in patients with coronary heart disease].

OBJECTIVE: To study the efficacy and safety of Yiqi Tongmai Oral Liquid (YQTM), a traditional compound Chinese herbal medicine, in treating angina pectoris in patients with coronary heart disease. METHODS: A multicentric, randomized, double blinded and paralleled controlled trial was conducted on 110 patients in trial group treated with YQTM, and 109 patients in control group treated with Shuxin Oral Liquid (SX). Cure and effective rates in both groups were evaluated. Frequency and duration of angina attack were counted and measured. Coronary angiography (CAG), electrocardiogram (ECG) and flat exercise test were taken in both groups. Blood lipid indexes, such as cholesterol (CH), triglyceride (TG), low-density lipoprotein (LDL), high density lipoprotein (HDL), were determined at pre- and post-treatment. The hemodynamic indexes, such as whole blood viscosity (J2), high-shear reduced viscosity (Eh), low-shear reduced viscosity (Ei), red cell aggregation index (Lb), red cell rigidity index (Rh), fibrinogen (Fb), blood sedimentation rate (BSR) and hematocrit (HCT), were determined at pre-and post-treatment. The indicated scores of symptoms and signs of traditional Chinese medicine (TCM) pattern, such as chest pain, chest constriction, breath shortness, palpitation, fatigue, dim complexion, spontaneous perspiration and tongue proper, tongue coating were evaluated in week 0, 1, 2, 3, 4 during the treatment course. The safety indexes, such as body temperature, pulse, respiration and blood pressure were observed. Routine tests of blood, urine and stool, hepatic function test and renal function test were taken at pre- and post-treatment. RESULTS: There was no significant difference between the total effective rate of the trial group and that of the control group, which were 91.82% and 85.32%, respectively (P>0.05). Trial groups percentile of cure rate is significantly higher than that of the control group (P<0.01). The frequency and duration of angina attack, the positive ratio of CAG and flat exercise test of both groups were lowered, while the effect of the trial group on frequency and duration of angina attack was better. No significant difference was found in ECG features between the two groups (P>0.05). The levels of CH, TG and LDL of both groups were lowered significantly (P<0.05). The effect of lowering CH, TG and LDL of the trial group was stronger than that of the control group (P<0.05). The hemodynamic indexes, such as J2, Eh, Ei, Lb, Rh, Fb, BSR and HCT were improved significantly in both groups (P<0.05). The improvements of J2, Eh, Ei, Lb, Rh, Fb and SR in the trial group were greater than those of control group (P<0.05). The TCM symptoms and signs, such as chest pain, chest constriction, breath shortness, palpitation, fatigue, dim complexion, spontaneous perspiration were improved significantly in both groups (P<0.05). The improvements of chest constriction, palpitation, fatigue and spontaneous perspiration in the trial group were greater than those of the control group (P<0.05). The total indicated score of TCM symptoms and signs was lowered more significantly than that of the control group (P<0.01). No significant changes were found at pre- and post-treatment in safety indexes, such as routine tests for blood, urine and stool, hepatic function test and renal function test. There was no significant difference in safety features of both groups (P>0.05). CONCLUSION: Yiqi Tongmai Oral Liquid bears good therapeutic effect on angina pectoris without adverse reaction, and is superior to Shuxin Oral Liquid. Yiqi Tongmai Oral Liquid is a new effective and safe medicine for the treatment of angina pectoris in patients with coronary heart disease.