PMID: 

Bioorg Med Chem Lett. 2013 Oct 15 ;23(20):5511-4. Epub 2013 Aug 22. PMID: 24018191

Abstract Title: 

Anti-proliferative activity of hydnocarpin, a natural lignan, is associated with the suppression of Wnt/β-catenin signaling pathway in colon cancer cells.

Abstract: 

Based on the Wnt inhibitors as potential targets in the development of anticancer agents, natural compounds were evaluated forβ-catenin-mediated transcriptional activity. A natural lignan hydnocarpin isolated from Lonicera japonica was considered a potential inhibitor for Wnt/β-catenin signalings. The anti-proliferative activity of hydnocarpin was also found to be associated with the suppression of Wnt/β-catenin-mediated signaling pathway in human colon cancer cells. These data suggest that hydnocarpin might be a novel Wnt inhibitor and has a potential of signaling regulator in β-catenin-mediated signaling pathways.

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PMID: 

Food Funct. 2013 Nov ;4(11):1654-61. PMID: 24081320

Abstract Title: 

Honeysuckle anthocyanin supplementation prevents diet-induced obesity in C57BL/6 mice.

Abstract: 

This study investigated the anti-obesity effects of honeysuckle anthocyanins (HA) in a high fat diet-induced mouse model. The mice were initially fed with a low-fat diet (LFD) or high-fat diet (HFD) for 8 weeks. After that, the HFD-fed mice were divided into five groups, with 12 mice in each group, including a HFD group, a HFD plus Orlistat group, and three HFD plus HA (at a dose of 50, 100, or 200 mg kg(-1)) groups, for another 8-week experiment. HA at 100 or 200 mg kg(-1) can suppress body weight gain, reduce serum and liver lipid profiles, ameliorate impaired hepatic function, and significantly increase serum adiponectin concentration while decreasing serum insulin and leptin levels. These results suggest that the anti-obesity effect of HA might be through the blockage of lipid accumulation.

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PMID: 

BMC Complement Altern Med. 2013 Oct 1 ;13:244. Epub 2013 Oct 1. PMID: 24083475

Abstract Title: 

Application of proteomics to identify the target molecules involved in Lonicera japonica-induced photokilling in human lung cancer CH27 cells.

Abstract: 

BACKGROUND: The Lonicera japonica has been used as natural and healthy drink for its anti-inflammatory effect and pleasant odor in China and Taiwan.METHODS: 2D electrophoresis was used to analyze the proteins involved in photoactivated Lonicera japonica-induced CH27 cell apoptosis. The fluorescent dyes MitoTracker Red CMXRos, calcein AM and JC-1 were used to elucidate mitochondrial function. The protein expression was performed by Western blotting. Fluorescent image of endoplasmic reticulum was accomplished by using ER-Tracker Green. This study used fluorescent dye CM-H2DCFDA to detect intracellular generation of reactive oxygen species.RESULTS: The identified proteins can be classified into three major groups, which include proteins involved in mitochondrial function, cytoskeleton-related proteins and proteins associated with endoplasmic reticulum (ER) stress. Photoactivated Lonicera japonica caused a significant effect on the mitochondrial function and ER stress in CH27 cells. The reactive oxygen species producing was found to be involved in photoactivated Lonicera japonica-induced CH27 cell apoptosis.CONCLUSION: Mitochondria and endoplasmic reticulum are the integral targets in photoactivated Lonicera japonica-induced CH27 cell apoptosis. We also demonstrated that ethyl acetate fraction of Lonicera japonica extracts caused photocytotoxicity in a dose-dependent manner in CH27 cells. This could explain the fact that the ethyl acetate fraction of Lonicera japonica extracts may contain compounds which exhibit the photosensitizing activity in CH27 cells.

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PMID: 

J Ethnopharmacol. 2014 ;151(1):123-30. Epub 2013 Nov 5. PMID: 24211495

Abstract Title: 

Effects of inhalable microparticle of flower of Lonicera japonica in a mouse model of COPD.

Abstract: 

ETHNOPHARMACOLOGICAL RELEVANCE: Flower of Lonicera japonica (FLJ) is a traditional herbal medicine widely used in East Asia as an anti-inflammatory and anti-oxidative agent. The purpose of this study is to develop an inhalable powder formulation of FLJ and to evaluate its biological effects in a mouse model of chronic obstructive pulmonary disease (COPD).METHODS: Inhalable dry powder containing FLJ was produced by spray-drying with leucine as an excipient. Its aerodynamic properties and anti-inflammatory activities were evaluated using the Anderson cascade impactor (ACI) and a mouse model of COPD, respectively.RESULTS: FLJ microparticle (FLJmp) had a hollow spherical shape in electron microscopy and showed aerodynamic properties suitable for inhalation (fine particle fraction of 54.0± 4.68% and mass median aerodynamic diameter of 4.6 ± 0.34μm). FLJmp decreased TNF-α and IL-6 expression in RAW264.7 cells activated by lipopolysaccharide (LPS). In mice challenged with LPS and cigarette smoke solution (CSS) to develop COPD, FLJmp decreased the levels of TNF-α and IL-6 in bronchoalveolar fluidas well as the number of inflammatory cells including neutrophils in peripheral blood. In addition, FLJmp induced recovery of elastin and collagen distribution, reduction of caspase-3 expression in lung tissues of COPD mice.CONCLUSIONS: Inhalational delivery of FLJ using a microparticle system is a promising strategy for the treatment of COPD.

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PMID: 

EXCLI J. 2014 ;13:427-36. Epub 2014 Apr 28. PMID: 26417269

Abstract Title: 

Antifungal potential of essential oil and ethanol extracts of Lonicera japonica Thunb. against dermatophytes.

Abstract: 

The antifungal potential of essential oil and ethanolic leaf extracts of Lonicera japonica Thunb. was evaluated for controlling the growth of dermatophytes. The oil (1,000 ppm) and extracts (1,500 ppm) of L. japonica revealed 55.1-70.3 % and 40.1-65.5 % antidermatophytic effect against Microsporum canis KCTC 6348, 6349, 6591, Trichophyton rubrum KCTC 6345, 6352, 6375, Trichophyton mentagrophytes KCTC 6077 and 6085, respectively, along with their respective minimum inhibitory concentrations ranging from 62.5-500 and 125-1,000µg/ml. Also, the oil had strong detrimental effect on spore germination of all the tested dermatophytes as well as concentration and time-dependent kinetic inhibition of M. canis KCTC 6348. The results demonstrated that L. japonica oil and extracts could be potential sources of natural fungicides to protect human and animals from fungal infections.

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PMID: 

ScientificWorldJournal. 2013 ;2013:612739. Epub 2013 Nov 6. PMID: 24307875

Abstract Title: 

Tyrosinase inhibitory effect and antioxidative activities of fermented and ethanol extracts of Rhodiola rosea and Lonicera japonica.

Abstract: 

This is the first study to investigate the biological activities of fermented extracts of Rhodiola rosea L. (Crassulaceae) and Lonicera japonica Thunb. (Caprifoliaceae). Alcaligenes piechaudii CC-ESB2 fermented and ethanol extracts of Rhodiola rosea and Lonicera japonica were prepared and the antioxidative activities of different concentrations of samples were evaluated using in vitro antioxidative assays. Tyrosinase inhibition was determined by using the dopachrome method with L-DOPA as substrate. The results demonstrated that inhibitory effects (ED50 values) on mushroom tyrosinase of fermented Rhodiola rosea, fermented Lonicera japonica, ethanol extract of Lonicera japonica, and ethanol extract of Rhodiola rosea were 0.78, 4.07, 6.93, and>10 mg/ml, respectively. The DPPH scavenging effects of fermented Rhodiola rosea (ED50 = 0.073 mg/ml) and fermented Lonicera japonica (ED50 = 0.207 mg/ml) were stronger than effects of their respective ethanol extracts. Furthermore, the scavenging effect increases with the presence of high content of total phenol. However, the superoxide scavenging effects of fermented Rhodiola rosea was less than effects of fermented Lonicera japonica. The results indicated that fermentation of Rhodiola rosea and Lonicera japonica can be considered as an effective biochemical process for application in food, drug, and cosmetics.

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PMID: 

Planta Med. 2014 Feb ;80(2-3):121-9. Epub 2014 Jan 15. PMID: 24431014

Abstract Title: 

The ethanol extract of Lonicera japonica (Japanese honeysuckle) attenuates diabetic nephropathy by inhibiting p-38 MAPK activity in streptozotocin-induced diabetic rats.

Abstract: 

The anti-inflammatory potential of Lonicera japonica makes it an excellent source of novel medicinal targets to reduce inflammation in diabetic nephropathy. We aimed to investigate whether the ethanol extract of the flowering aerial parts of L. japonica exerts an ameliorative effect on diabetic renal inflammation using streptozotocin-induced diabetic rats. Diabetic rats were treated orally with the ethanol extract of the flowering aerial parts of L. japonica (100 and 200 mg/kg/day) for 8 weeks. The rats exhibited renal dysfunction, asevidenced by reduced creatinine clearance, increased blood urea nitrogen, and proteinuria, along with a marked elevation in the ratio of kidney weight to body weight; all of these abnormalities were significantly reversed by the ethanol extract of the flowering aerial parts of L. japonica. The histological examinations revealed amelioration of diabetes-induced glomerular pathological changes following treatment with the ethanol extract of the flowering aerial parts of L. japonica. It reduced the accumulation of ED-1-expressing macrophages in renal tissue of diabetic rats, almost completelyabolished T cell infiltration and attenuated the expression of proinflammatory cytokines. The ethanol extract of the flowering aerial parts of L. japonica downregulated the protein expression of p38 mitogen-activated protein kinase in the kidney of diabetic rats. The results suggest that it has theproperty to inhibit the activity of p-38 MAPK-mediated inflammatory response to halt the progression of diabetic nephropathy.

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PMID: 

PLoS One. 2014 ;9(1):e86117. Epub 2014 Jan 24. PMID: 24475077

Abstract Title: 

Flos Lonicera ameliorates obesity and associated endotoxemia in rats through modulation of gut permeability and intestinal microbiota.

Abstract: 

BACKGROUND AND AIM: Increasing evidence has indicated a close association of host-gut flora metabolic interaction with obesity. Flos Lonicera, a traditional herbal medicine, is used widely in eastern Asia for the treatment of various disorders. The aim of this study was to evaluate whether unfermented or fermented formulations of Flos Lonicera could exert a beneficial impact to combat obesity and related metabolic endotoxemia.METHODS: Obesity and metabolic endotoxemia were induced separately or together in rats through feeding a eight-week high fat diet either alone (HFD control group) or in combination with a single LPS stimulation (intraperitoneal injection, 0.75 mg/kg) (LPS control group). While, the mechanism of action of the Lonicera formulations was explored in vitro using RAW 264.7 and HCT 116 cell lines as models.RESULTS: In cell-based studies, treatment with both unfermented Flos Lonicera (UFL) and fermented Flos Lonicera (FFL) formulations resulted in suppression of LPS-induced NO production and gene expression of vital proinflammatory cytokines (TNF-α, COX-2, and IL-6) in RAW 264.7 cells, reduced the gene expression of zonula occludens (ZO)-1 and claudin-1, and normalized trans epithelial electric resistance (TEER) and horseradish peroxidase (HRP) flux in LPS-treated HCT-116 cells. In an animal study, treatment of HFD as well as HFD+LPS groupswith UFL or FFL resulted in a notable decrease in body and adipose tissue weights, ameliorated total cholesterol, HDL, triglyceride, aspartate transaminase and endotoxin levels in serum, reduced the urinary lactulose/mannitol ratio, and markedly alleviated lipid accumulation in liver. In addition,exposure of HFD as well as HFD+LPS groups with UFL or FFL resulted in significant alteration of the distribution of intestinal flora, especially affecting the population of Akkermansia spp. and ratio of Bacteroidetes and Firmicutes.CONCLUSION: This evidence collectively demonstrates that Flos Lonicera ameliorates obesity and related metabolic endotoxemia via regulating distribution of gut flora and gut permeability.

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PMID: 

PLoS One. 2014 ;9(4):e94952. Epub 2014 Apr 14. PMID: 24733024

Abstract Title: 

New cholinesterase inhibitory constituents from Lonicera quinquelocularis.

Abstract: 

A phytochemical investigation on the ethyl acetate soluble fraction of Lonicera quinquelocularis (whole plant) led to the first time isolation of one new phthalate; bis(7-acetoxy-2-ethyl-5-methylheptyl) phthalate (3) and two new benzoates; neopentyl-4-ethoxy-3, 5-bis (3-methyl-2-butenyl benzoate (4) and neopentyl-4-hydroxy-3, 5-bis (3-methyl-2-butenyl benzoate (5) along with two known compounds bis (2-ethylhexyl phthalate (1) and dioctyl phthalate (2). Their structures were established on the basis of spectroscopic analysis and by comparison with available data in the literature. All the compounds (1-5) were tested for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities in dose dependent manner. The IC50 (50% inhibitory effect) values of compounds 3 and 5 against AChE were 1.65 and 3.43µM while the values obtained against BChE were 5.98 and 9.84 µM respectively. Compounds 2 and 4 showed weak inhibition profile.

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PMID: 

Chin J Nat Med. 2014 Feb ;12(2):108-13. PMID: 24636060

Abstract Title: 

Comparison of anti-bacterial activity of three types of di-O-caffeoylquinic acids in Lonicera japonica flowers based on microcalorimetry.

Abstract: 

The anti-bacterial activities of three types of di-O-caffeoylquinic acids (diCQAs) in Lonicera japonica flowers, a traditional Chinese medicine (TCM), on Bacillus shigae growth were investigated and compared by microcalorimetry. The three types of diCQAs were 3, 4-di-O-caffeoylquinic acid (3, 4-diCQA), 3, 5-di-O-caffeoylquinic acid (3, 5-diCQA), and 4, 5-di-O-caffeoylquinic acid (4, 5-diCQA). Some qualitative and quantitative information of the effects of the three diCQAs on metabolic power-time curves, growth rate constant k, maximum heat-output power Pm, and the generation time tG, total heat output Qt, and growth inhibitory ratio I of B. shigae were calculated. In accordance with a thermo-kinetic model, the corresponding quantitative relationships of k, Pm, Qt, I and c were established. Also, the half-inhibitory concentrations of the drugs (IC50) were obtained by quantitative analysis. Based on the quantity-activity relationships and the IC50 values, the sequence of inhibitory activity was 3, 5-diCQA>4, 5-diCQA>3, 4-diCQA. The results illustrate the possibility that the caffeoyl ester group at C-5 is the principal group that has a higher affinity for the bacterial cell, and that the intramolecular distance of the two caffeoyl ester groups also has an important influence on the anti-bacterial activities of the diCQAs.

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