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This study investigated possible analgesic and anti-inflammatory mechanisms of the methanol extract ofFicus pumila(FPMeOH). Analgesic effects were evaluated in two models including acetic acid-induced writhing response and formalin-induced paw licking. The results showedFPMeOHdecreased writhing response in the acetic acid assay and licking time in the formalin test. The anti-inflammatory effect was evaluated by λ-carrageenan-induced mouse paw edema and histopathological analyses.FPMeOHsignificantly decreased the volume of paw edema induced by λ-carrageenan. Histopathologically,FPMeOHabated the level of tissue destruction and swelling of the edema paws. This study indicated anti-inflammatory mechanism ofFPMeOHmay be due to declined levels of NO and MDA in the edema paw through increasing the activities of SOD, GPx, and GRd in the liver. Additionally,FPMeOHalso decreased the level of inflammatory mediators such as IL-1β, TNF-α, and COX-2. HPLC fingerprint was established and the contents of three active ingredients, rutin, luteolin, and apigenin, were quantitatively determined. This study provided evidence for the classical treatment ofFicus pumilain inflammatory diseases.

The aim of this study was to examine the antioxidant activities and phenolic components of the crude extracts of 10 Desmodium species from Taiwan. In this study, DPPH free radical scavenging activity, ABTS radical monocation scavenging activity, ferric-reducing antioxidant power (FRAP) and reducing power of the 10 Desmodiumspecies were evaluated for their antioxidant activities. The results showed that, of all the samples, Desmodium sequax was the most active in ABTS, DPPH, FRAP and reducing power assays. The total polyphenol, total flavonoid and total flavonol contents of the crude extract were calculated. The correlation coefficient (R2) values of TEAC with phenolic compounds indicated strong positive correlations, except for total flavonoid content. Furthermore, HPLC chromatographic fingerprints were established, and chlorogenic acid and vitexin in D. sequax were quantified. Chlorogenic acid was confirmed to express strong antioxidant activities in ABTS, DPPH, FRAP and reducing power assays. The present study indicated the antioxidant activities of the 10Desmodium species were related to their phenolic components. D. sequax is a potent antioxidant medicinal plant, and chlorogenic acid may be an important factor in the antioxidant activity of this plant. Key words: Desmodium, antioxidant activity, chlorogenic acid, vitexin

Oxidative stress and inflammation are related to several chronic diseases including cancer and atherosclerosis. Kalanchoe gracilis (L.) DC is a special folk medicinal plant in Taiwan. The aim of this study was to evaluate the antioxidant, anti-inflammatory and antiproliferative activities of the methanolic extract and fractions of the stem of K. gracilis. TEAC, total phenolic compound content, total flavonoid content, DPPH radical scavenging activity, reducing power, inhibition of NO production in LPS-induced RAW264.7 cells, and inhibition of cancer cell proliferation were analyzed. Among all fractions, the chloroform fraction showed the highest TEAC and DPPH radical scavenging activities. The chloroform fraction also had the highest content of polyphenols and flavonoids. Chloroform fractions also decreased LPS-induced NO production and expressions of iNOS and COX-2 in RAW264.7 cells. The antiproliferative activities of the methanolic extract and fractions were studied in vitro using HepG2 cells, and the results were consistent with their antioxidant capacities. Chloroform fractions had the highest antiproliferative activity with an IC50 of 136.85 ± 2.32 μg/ml. Eupafolin also had good pharmacological activity in the antioxidant, anti-inflammation and antiproliferative. Eupafolin might be an important bioactive compound in the stem of K. gracilis. The above experimental data indicated that the stem of K. gracilis is a potent antioxidant medicinal plant, and such efficacy may be mainly attributed to its polyphenolic compounds.

The aims of this study intended to investigate the anti-inflammatory activity of the 70% ethanol extract from Scoparia dulcis (SDE) and betulinic acid on λ-carrageenan-induced paw edema in mice. The anti-inflammatory mechanism of SDE and betulinic acid was examined by detecting the levels of cyclooxygenase-2 (COX-2), nitric oxide (NO), tumor necrosis factor (TNF-α), interleukin-1β (IL-1β) and malondialdehyde (MDA) in the edema paw tissue and the activities of superoxide dismutase (SOD), glutathione peroxidase (GPx) and glutathione reductase (GRd) in the liver. The betulinic acid content in SDE was detected by high performance liquid chromatography (HPLC). In the anti-inflammatory model, the results showed that SDE (0.5 and 1.0 g/kg) and betulinic acid (20 and 40 mg/kg) reduced the paw edema at 3, 4 and 5 h after λ-carrageenan administration. Moreover, SDE and betulinic acid affected the levels of COX-2, NO, TNF-α and IL1-β in the λ-carrageenan-induced edema paws. The activities of SOD, GPx and GRd in the liver tissue were increased and the MDA levels in the edema paws were decreased. It is suggested that SDE and betulinic acid possessed anti-inflammatory activities and the anti-inflammatory mechanisms appear to be related to the reduction of the levels of COX-2, NO, TNF-α and IL1-β in inflamed tissues, as well as the inhibition of MDA level via increasing the activities of SOD, GPx and GRd. The analytical result showed that the content of betulinic acid in SDE was 6.25 mg/g extract.

This study aims to investigate the hepatoprotective activity and active constituents of the ethanol extract of Scoparia dulcis (SDE). The hepatoprotective effect of SDE (0.1, 0.5 and 1 g/kg) was evaluated on the carbon tetrachloride ( CCl4)-induced acute liver injury. The active constituents were detected by high performance liquid chromatography (HPLC). Mice pretreated orally with SDE (0.5 and 1.0 g/kg) and silymarin (200 mg/kg) for five consecutive days before the administering of a single dose of 0.2% CCl4(10 ml/kg of bw, ip) showed a significant inhibition of the increase of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Histological analyses also showed that SDE (0.5 and 1.0 g/kg) and silymarin reduced the extent of liver lesions induced by CCl4, including vacuole formation, neutrophil infiltration and necrosis. Moreover, SDE decreased the malondialdehyde (MDA) level and elevated the content of reduced glutathione (GSH) in the liver as compared to those in the CCl4group. Furthermore, SDE (0.5 and 1.0 g/kg) enhanced the activities of anti-oxidative enzymes including superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase (GRd) and glutathione-S-transferase (GST). The quantities of active constituents in SDE were about 3.1 mg luteolin/g extract and 1.1 mg apigenin/g extract. The hepatoprotective mechanisms of SDE were likely associated to the decrease in MDA level and increase in GSH level by increasing the activities of antioxidant enzymes such as SOD, GPx, GRd and GST. These results demonstrated that SDE could alleviate CCl4-induced acute liver injury in mice.

In this study, we evaluated the analgesic effect of methanol extract from Desmodium triflorum DC (MDT) by using animal models of acetic acid-induced writhing response and formalin test. The anti-inflammatory effect of MDT was investigated by lambda-carrageenan-induced paw edema in mice. In order to study the anti-inflammatory mechanism of MDT, we detected the activities of glutathione peroxidase (GPx) and glutathione reductase (GRd) in the liver, the levels of interleukin-1beta (IL-1beta), tumor necrosis factor (TNF-alpha), malondialdehyde (MDA) and nitric oxide (NO) in the edema paw tissue. In the analgesic test, MDT (0.5 and 1.0 g/kg) decreased the acetic acid-induced writhing response and the licking time on the late phase in the formalin test. In the anti-inflammatory test, MDT (0.5 and 1.0 g/kg) decreased the paw edema at the 3rd, 4th, 5th and 6th hour after lambda-carrageenan administration. On the other hand, MDT increased the activities of SOD and GRd in liver tissues and decreased the MDA level in the edema paw at the 3rd hour after lambda-carrageenan-induced inflammation. MDT also affected the levels of interleukin-1beta, tumor necrosis factor-alpha, NO and MDA which were induced by lambda-carrageenan. The results suggested that MDT possessed analgesic and anti-inflammatory effects. The anti-inflammatory mechanism of MDT might be related to the decreases in the level of MDA in the edema paw via increasing the activities of SOD and GRd in the liver, and the NO level via regulating the IL-1beta production and the level of TNF-alpha in the inflamed tissues.

We investigated possible mechanisms of analgesic and anti-inflammatory activities of the methanol extract from the leaf of Elaeagnus oldhamii Maxim. (EOMeOH). EOMeOHwas evaluated for its analgesic activity in acetic acid-induced writhing response and formalin test, and anti-inflammatory effect was examined by λ-carrageenan-induced paw edema assay. We detected the activities of GPx, GRd and SOD in the liver, and the levels of inflammatory mediators including IL-1β, IL-6, TNF-α, COX-2, MDA and NO in the edema paw to investigate the mechanism of action against inflammation. Total polyphenol, flavonoid and flavanol contents of EOMeOHwere detected to explore its antioxidant activities. Results showed that, in the analgesic test, EOMeOHdecreased acetic acid-induced writhing response and the licking time in the late phase of formalin test. In the anti-inflammatory test, EOMeOHdecreased paw edema at the 2nd, 3rd, 4th and 5th h after λ-carrageenan had been injected. EOMeOHincreased the activities of SOD and GPx in liver tissue and decreased MDA, NO, IL-1β, IL-6, TNF-α and COX-2 levels in paw edema tissue at the 3rd h after λ-carrageenan-induced inflammatory reaction. EOMeOHexhibited abundant polyphenol, flavonoid and flavanol contents. In HPLC fingerprint test of EOMeOH, two index ingredients, ursolic acid and pomolic acid, were isolated from EOMeOHand were exhibited in HPLC chromatographic analysis. The results demonstrated analgesic and anti-inflammatory effects of EOMeOH. It was indicated that the anti-inflammatory mechanism of EOMeOHmay be due to declined levels of NO and MDA in the edema paw through increasing the activities of SOD, GPx and GRd in the liver. Additionally, EOMeOHdecreased IL-1β, IL-6, TNF-α and COX-2 levels in the edema paw. The results suggested its value in future development of herbal medicine for the treatment of inflammatory diseases.

The objective of this study was to examine the potential of enhancing the antileukemic activity of arsenic trioxide (ATO) by combining it with a folk remedy, crude methanolic extract ofMucuna macrocarpa(CMEMM). Human leukemia cells HL-60, Jurkat, and Molt-3 were treated with various doses of ATO, CMEMM, and combinations thereof for 24 and 48 h. Results indicated that the combination of 2.5 μM ATO and 50 μg/mL CMEMM synergistically inhibited cell proliferation in HL-60 and Jurkat cell lines. Apoptosis triggered by ATO/CMEMM treatment was confirmed by accumulation of cells in the sub-G1phase in cell cycle analyses, characteristic apoptotic nuclear fragmentation, and increased percentage of annexin V-positive apoptotic cells. Such combination treatments also led to elevation of reactive oxygen species (ROS). The antioxidantsN-acetyl cysteine (NAC), butylated hydroxytoluene, andα-tocopherol prevented cells from ATO/CMEMM-induced apoptosis. The ATO/CMEMM-induced activation of caspase-3 and caspase-9 can be blocked by NAC. In summary, these results suggest that ATO/CMEMM combination treatment exerts synergistic apoptosis-inducing effects in human leukemic cells through a ROS-dependent mechanism and may provide a promising antileukemic approach in the future.

In this study, we evaluated the analgesic effect of the methanol extract of Kalanchoe gracilis (MKGS) stem in animal models by inducing writhing response with acetic acid and conducting formalin test. The anti-inflammatory effect of MKGS was also estimated on mice with lambda-carrageenan induced paw edema model. In order to investigate the anti-inflammatory mechanism of MKGS, we analyzed the activities of glutathione peroxidase (GPx) and glutathione reductase (GRx) in the liver, and the levels of interleukin-1beta (IL-1beta), tumor necrosis factor (TNF-alpha), malondialdehyde (MDA) and nitric oxide (NO) in the edema paw tissue. In the analgesic tests, MKGS (0.5 and 1.0 g/kg) decreased both the acetic acid-induced writhing response and the licking time in the late phase of the formalin test. In the anti-inflammatory test, MKGS (0.1, 0.5 and 1.0 g/kg) decreased paw edema at the third, fourth, fifth and sixth hours after lambda-carrageenan had been administrated. Furthermore, MKGS increased the activities of SOD and GRx in liver tissues and decreased MDA level in the edema paws three hours after lambda-carrageenan was injected. MKGS also affected the levels of IL-1beta, TNF-alpha and NO induced by lambda-carrageenan. All these results suggested that MKGS possessed analgesic and anti-inflammatory effects. The anti-inflammatory mechanism of MKGS might be related to the lowering of MDA level in the edema paw via increasing the activities of superoxide dismutase (SOD) and GRx in the liver, as well as the decreases in the levels of TNF-alpha and NO, and the production of IL-1beta in inflamed tissues.

This study evaluated the antioxidant and antiproliferative activities of the crude extract and fractions of Desmodium triflorum (L.) DC. The total phenolic content, 1,1-diphenyl-2- picrylhydrazyl hydrate (DPPH) free radical scavenging activity, trolox equivalent antioxidant capacity (TEAC), reducing power, total flavonoid content of D. triflorum were evaluated for the exploration of its antioxidant activities. Furthermore, its antiproliferative activities were investigated through the MTT method. It was compared with the antioxidant capacities of known antioxidants, including catechin, α-tocopherol, trolox and ascorbic acid. Among all fractions, ethyl acetate fraction was the most active in scavenging DPPH and TEAC radicals, of which 0.4 mg was equivalent to 186.6 ± 2.5 μg and 82.5 ± 2.1 μg of α-tocopherol and trolox respectively. The total phenolic and flavonoid contents of the crude extract were equivalent to 36.60 ± 0.1 mg catechin and 45.6 ± 0.6 mg rutin per gram respectively. In the reducing power assay, 1.25 mg of crude extract was similar to 61.2 ± 0.3 μg of ascorbic acid. For the assessment of the safety and toxicity of D. triflorum, LD50 of the crude extract was greater than 10 g/kg when administered to mice through gastric intubation. The above experimental data indicated that D. triflorum was a potent antioxidant medicinal plant, and such efficacy may be mainly attributed to its polyphenolic compounds.