Previous studies have indicated that the Ilex genus exhibits antioxidant, neuroprotective, hepatoprotective, and anti-inflammatory activities. However, the pharmacologic action and mechanisms of Ilex cornuta against cardiac diseases have not yet been explored. The present study was designed to investigate the antioxidant and cardioprotective effects of Ilex cornuta root with in vitro and in vivo models. The anti-oxidative effects of the extract of Ilex cornuta root (ICR) were measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging and MTT assays as well as immunoassay. Furthermore, a rat model of myocardial ischemia was established to investigate the cardioprotective effect of ICR in vivo. Eight compounds were isolated and identified from ICR and exhibited DPPH free-radical scavenging activities. They also could increase cell viability and inhibit morphological changes induced by H2O2 or Na2S2O4 in H9c2 cardiomyocytes, followed by increasing the SOD activities and decreasing the MDA and ROS levels. In addition, it could suppress the apoptosis of cardiomyocytes. In the rat model of myocardial ischemia, ICR decreased myocardial infarct size and suppressed the activities of LDH and CK. Furthermore, ICR attenuated histopathological alterations of heart tissues and the MDA levels, while increasing SOD activities in serum. In conclusion, these results suggest that ICR has cardioprotective activity and could be developed as a new food supplement for the prevention of ischemic heart disease.

A comprehensive phytochemical study of the chemical constituents of green vegetable soybeans resulted in the isolation of two new alkaloids, soyalkaloid A, 1, and isoginsenine, 2, together with four known ones, ginsenine, 3, (1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid, 4, (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid, 5, and indole-3-carboxylic acid, 6. The structures of compounds 1–6 were elucidated on the basis of spectroscopic and chemical analyses. All of the alkaloids were isolated from soybeans for the first time, and compound 1 was a new indole-type alkaloid with a novel carbocyclic skeleton. Their inhibitory activities on the proliferation of concanalin A-activated lymphocytes were assessed by CCK8 assay.

•Seven new triterpenoids (1–7) were isolated from the aerial parts of Ilex cornuta.•All compounds were characterized by spectroscopic methods.•Compound 4 had significant cell-protective effect.Seven new triterpenoids (1–7), together with two known ones (8–9), were isolated from the aerial parts ofIlex cornuta. The leaves of I. cornuta are the major source of “Kudingcha”, a popular herbal tea consumed in China and other countries. The structures of compounds 1–7 were determined as 20-epi-urs-12,18-dien-28-oic acid 3β-O-α-l-arabinopyranoside (1), 20-epi-urs-12,18-dien-28-oic acid 2′-O-acetyl-3β-O-α-l-arabinopyranoside (2), 20-epi-urs-12,18-dien-28-oic acid 3β-O-β-d-glucuronopyranoside-6-O-methyl ester (3), 3β,23-dihydroxy-20-epi-urs-12,18-dien-28-oic acid (4), 23-hydroxy-20-epi-urs-12,18-dien-28-oic acid 3β-O-α-l-arabinopyranoside (5), 23-hydroxy-20-epi-urs-12,18-dien-28-oic acid 3β-O-β-d-glucuronic acid (6), 23-hydroxy-20-epi-urs-12,18-dien-28-oic acid 3β-O-β-d-glucuronopyranoside-6-O-methyl ester (7), on the basis of spectroscopic analyses (IR, ESI–MS, HR-ESI–MS, 1D and 2D NMR) and chemical reactions. Protective effects against H2O2-induced H9c2 cardiomyocyte injury were tested in vitro for compounds 1–9, and the data showed that compound 4 had significant cell-protective effect. Compounds 1-9 did not show significant DPPH radical scavenging activity.

•Cantharidin caused NRK cell apoptosis..•Cantharidin induced renal injury in rat..•Ginsenosides reduced apoptosis rate induced by Cantharidin.•Ginsenosides have protective effects on acute renal injury induced by cantharidin.Ginsenosides are major active constituent of Panax ginseng which is a popularly used functional food or drug in several Asian countries. The effects of ginsenosides on the renal dysfunction and injury caused by cantharidin were investigated in vitro and in vivo. Ginsenosides inhibited the cytotoxicity in rat normal kidney NRK cell induced by cantharidin. Cantharidin caused NRK cell apoptosis accompanied with decreasing bcl-2 expression. Pretreatment of ginsenosides reduced apoptosis rate and increased bcl-2 expression. In experimental rats, administration of cantharidin (0.14 mg/kg) for 15 days induced renal damage, which was evident from significantly increased levels of serum creatinine, urine protein and urea nitrogen. Pretreatment of ginsenosides reduced the increases of serum creatinine, urine protein, urea nitrogen and histological change in rats. These findings provide the evidence that ginsenosides might be useful in enhancing the tolerance of the kidney against renal injury associated with cantharidin.

Pulsatilla chinensis (Bunge) Regel is a Chinese medicinal herb for “blood-cooling” and detoxification. Now it is used for the treatment of malignant tumor, but the antitumor mechanisms and toxic side effects of P. chinensis are unclear. The present study was undertaken to investigate if P. chinensis saponins (PRS) possesses anticancer effects and toxic side effects in human liver tumor 7402 cells in vitro and vivo. 7402 cells were treated with different concentrations of PRS for 24 h. Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cell apoptosis was assessed by flow cytometry. The in vivo effect of PRS on 7402 tumor cells transplanted in athymic nude mice was investigated. 15 saponins were isolated and identified from PRS. PRS inhibited the proliferation of human liver tumor 7402 cells in vitro by apoptosis. 19 days after administration of PRS (100, 200 mg/kg), the weight of tumor mass was markly decreased in nude mice. The anti-tumor effect of PRS in vivo was associated with a significant increase in the 7402 apoptosis rate. Although PRS inhibited the weight of mice, it showed almost no effect on leukocyte number, liver and spleen weight index. Light microscopic histopathological examination showed that PRS had no specific lesion in organ. These results suggested that P. chinensis saponins exert potential anticancer activity in treating tumors in nude mice and no toxic side effects.Download high-res image (360KB)Download full-size image