Table 3.
The activities of some compounds from Lonicera japonica.
| Compounds | Effects | In vivo | In vitro | Reference |
|---|---|---|---|---|
| Caffeic acid | Antioxidative activity | Showed marked antioxidant and scavenging activities with IC50 values of 5.72 μM for DPPH radicals, and 3.18 μM for ONOO− | Choi et al. (2007) | |
| Chlorogenic acid | Anti-tumor activity | With IC50 values of 55 μmol/L and corresponding cell (HepG2 cell) viabilities was 62% ± 4%. And the cytotoxicities of chlorogenic acid were partially eliminated by the antioxidant effect of N-acetyl-l-cysteine (NAC) | Yip et al. (2006) | |
| Antibacterial activity | Compared to the Gram-positive bacteria, the chlorogenic acid to Gram-negative bacteria's bacteriostasis activeness was stronger; the minimum inhibitory concentration of chlorogenic acid to shigella and salmonella was 0.125 mg/ml, almost the same to 0.1 mg/ml kanamycin | Xu (2008) | ||
| MIC was 0.025 g/ml, 0.025 g/ml, 0.1 g/ml and 0.8 g/ml against Escherichia coli, Sarcina luteus, Bacillus subtillis and Staphylococcus aureus | Wu (2005) | |||
| Antioxidative activity | The DPPH scavenging activity was 74% at the dose of 0.1 g/ml | Wu (2005) | ||
| Antiviral activity | At the doses of 0.05 mg/ml, 0.1 mg/ml, 0.4 mg/ml, 0.8 mg/ml and 0.8 mg/ml, it respectively inhibited respiratory syncytia virus, coxsackie B3 virus, adeno-associated 7 viruses, adeno-associated 3 viruses and Coxsackie B5 virus | Hu et al. (2001) | ||
| The 0% toxic dose, minimum effective concentration and therapeutic index against to human cytomegalovirus were 100 μg/ml, 1 μg/ml and 100, respectively | Chen et al. (2009) | |||
| Anti-inflammatory activity | It (5, 10, 15 mmol/L) decreased the expression of NF-kB P65 induced by LPS at 4 h (P < 0.05), and the concentration of NO at 6 h. At the same time, it would increase the decrease of activity of GSH-Px induced by LPS at 6 h (P < 0.05) | Huo et al. (2003) | ||
| Hypoglycemic activity | 1 mM inhibited about 40% of glucose-6-phosphatase activity (P < 0.05) in the microsomal fraction of hepatocytes. It promoted a significant reduction (P < 0.05) in the plasma glucose peak at 10 and 15 min during the oral glucose tolerance test, probably by attenuating intestinal glucose absorption. This suggested a possible role for it as a glycaemic index lowering agent and highlighting it as a compound of interest for reducing the risk of developing type 2 diabetes | Bassoli et al. (2008) | ||
| Dicaffeoylquinic acids | Antiviral activity | Results showed that 3,5-dicaffeoylquinic acid and two analogues were potent and selective inhibitors of HIV-1 IN in vitro. All of the dicaffeoylquinic acids were found to inhibit HIV-1 replication at concentrations ranging from 1 to 6 μM in T cell lines, whereas their toxic concentrations in the same cell lines were >120 μM. In addition, it inhibited HIV-1 IN in vitro at submicromolar concentrations. So the dicaffeoylquinic acids as a class are potent and selective inhibitors of HIV-1 IN and form important lead compounds for HIV drug discovery | Robinson et al. (1996) | |
| Hederagenin | Anti-inflammatory activity | 100 mg/kg showed anti-inflammatory activity in the same model with 42% and 23% inhibition rates (P < 0.001) | Lee et al. (1995a) | |
| Hyperoside | Antibacterial activity | It showed a excellent antibacterial effect on SA strains with a low MIC of 0.5–1 mg/ml, and the MIC of 2 mg/ml for strains of Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumonia were observed | Tang (2008) | |
| The antibacterial activity with synergistic effect | The FIC index indicated that the addition effects were found in 55%, 30%, 25% and 15% of MRSA strains (n = 20) when hyperoside combined with oxacillin, benzylpenicillin, gatifloxacin and levofloxacin, respectively. Results suggested that hyperoside could enhance the anti-MRSA efficiency of these β-lactams or quinolones. It combined with chlorogenic acid showed an obvious cumulate bactericidal action on Pseudomonas aeruginosa ATCC27853 with a FIC index of 0.75 | Tang (2008) | ||
| Hepatoprotective | 80 μg/mL exhibited the best protective effects for hepatocytes injured by CCl4, characterized as the levels of ALT, AST and MDA decreasing, elevation of GSH level and survival hepatocytes increasing with little damage in cell structure. The significant hepatoprotective effects for CCl4-attatcked rats were found in three dosages of hyperoside (10, 20 and 30 mg/kg) with the obvious improve biochemical indexes and liver histopathology examination. The results of animals received hyperoside of 30 mg/kg were almost similar to that of normal controls | Tang (2008) | ||
| Anti-tumor activity | 5, 10, 20, 25 μg/mL have inhibitory effect on Hep-2 cells when it was used as photosensitizer in PDT or as radiosensitizer in radiotherapy. And this indicate that hypericin may be a hopeful agent to treat laryngeal carcinoma | Sun (2002) | ||
| Isorhamnetin 3-O-β-d-glucopyranoside | Antioxidative activity | Showed marked antioxidant and scavenging activities with IC50 values of 11.76 μM for DPPH radicals, and 3.34 μM for ONOO− | Choi et al. (2007) | |
| Loganin | Anti-inflammatory activity | 100 mg/kg presented anti-inflammatory activity against mouse ear edema induced by croton-oil and arachidonic acid with 20% and 19% inhibition rates | Lee et al. (1995a) | |
| Loniceroside A | Anti-inflammatory activity | 100 mg/kg showed anti-inflammatory activity against mouse ear edema induced by croton-oil and arachidonic acid with 34% and 23% inhibition rates. Although far less potent than prednisolone (52% and 36%), it was comparable to aspirin at the dose of 100 mg/kg. 100 mg/kg/day also could reduce adjuvant-induced arthritis in rats (P < 0.05). The reference compound showed potent activity at a dose of 20 mg/kg/day (P < 0.01). At the same time, it (100 mg/kg, p.o.) against mouse ear edema provoked by croton oil with 30.2% inhibition rate |
Lee et al. (1995a) Kwak et al. (2003) |
|
| Loniceroside C | Anti-inflammatory activity | At the doses of 50, 100, 200 mg/kg (p.o.), it showed antiinflammatory activity against mouse ear edema provoked by croton oil with 15%, 31% and 28.7% inhibition rates, respectively | Kwak et al. (2003) | |
| Lonicerin | Anti-inflammatory activity | It presented anti-inflammatory activity against mouse ear edema induced by croton-oil with 39% (P < 0.001) | Lee et al. (1995a) | |
| Luteolin | Antioxidative activity | |||
| Anti-inflammatory activity | It effectively inhibited the lipopolysaccharide (LPS)-induced tumor necrosis factor-α, interleukin-6 and inducible nitric oxide production in vitro, protect against LPS-induced lethal toxicity by inhibiting pro-inflammatory molecule expression in vivo and reducing leukocyte infiltration in tissues | Park et al. (2005), Xagorari et al. (2001), Kotanidou et al. (2002) | ||
| Anti-tumor activity | The MTT assay showed that was 20% viability when HepG2 hepatocellular carcinoma cells were incubated at 100 μmol/L. IC50 values of 40 μmol/L and corresponding cell viabilities of 53% ± 5%. The cytotoxicities were partially eliminated by the antioxidant effect of N-acetyl-l-cysteine | Yip et al. (2006) | ||
| Anti-5-lipoxygenase activity | It presented the 5-lipoxygenase inhibitory activities with 97% inhibition at 20 μM. Nordihydroguaiaretic acid was used as a reference compound with 100% inhibition at 20 μM | Lee et al. (2010) | ||
| Luteolin 7-O-β-d-glucopy ranoside | Antioxidative activity | Showed marked antioxidant and scavenging activities with IC50 values of 9.97 μM for DPPH radicals, and 3.18 μM for ONOO− | Choi et al. (2007) | |
| Ochnaflavon | Anti-inflammatory activity | It inhibited cyclooxygenase-2 (COX-2) dependent phases of prostaglandin D2 (PGD2) generation in bone marrow-derived mast cells with IC50 values of 0.6 μM. Western blotting showed that the decrease in quantity of the PGD2 product was accompanied by a decrease in the COX-2 protein level. And this compound could consistently inhibit the production of leukotriene C4, with an IC50 value of 6.56 μM. So ochnaflavone has a dual cyclooxygenase-2/5-1ipoxygenase inhibitory activity. It also strongly inhibited degranulation reaction, with an IC50 value of 3.01 μM | Son et al. (2006) | |
| At 10 μM, ochnaflavone showed the suppressive activity against lymphocyte proliferation induced by Con A or LPS | Lee et al. (1995b) | |||
| Protocate chuic acid | Antioxidative activity | Showed marked antioxidant and scavenging activities with IC50 values of 7.21 μM for DPPH radicals, and 1.47 μM for ONOO− | Choi et al. (2007) | |
| Anti-tumor activity | It was capable of stimulating the c-Jun N-terminal kinase (JNK) and p38 subgroups of the mitogen-activated protein kinase (MAPK) family. It induced cell death was rescued by specific inhibitors for JNK and p38, with IC50 values of 60 μmol/L | Yip et al. (2006) | ||
| Quercetin 3-O-β-d-glu copyranoside | Antioxidative activity | Showed marked antioxidant and scavenging activities with IC50 values of 4.60 μM for DPPH radicals, and 1.76 μM for ONOO− | Choi et al. (2007) | |
| Rutin | Anti-apoptotic activity | Improved I/R-induced myocardial contractile function and reduced infarct size (32.0% ± 6.0%). Rutin administration also inhibited apoptosis in myocardial tissues in I/R rats by increasing Bcl-2/bax ratio and decreasing active caspase-3 expression. These results suggest that rutin reduced oxidative stress-mediated myocardial damage in vitro and in vivo model, which might be useful in treatment of myocardial infarction | Rutin decreased expression of both cleaved from of caspase-3 (P < 0.01, at 20 μM) and increased Bcl-2/Bax ratio in H9c2 cells. The protective effect of rutin was inhibited by PI3K inhibitor or ERK inhibitor. It increased phosphorylation of ERK and Akt in H9c2 cells. These anti-apoptotic effects of rutin were confirmed both by annexin-V and TUNEL assay | Jeong et al. (2009) |
| Shuangkangsu | Antiviral activity | It inhibited markedly influenza B virus and influenza A3 virus (P < 0.5). IC50 < 0.31 mg/embroy, therapeutic index (TI) > 32. And also could inhibit respiratory syncytial virus (RSV) (P < 0.005), IC50 = 0.9 mg/ml, TI = 6.2 | Li (2008a) |