Review on the Pharmacological Properties of Phillyrin

Phillyrin is an effective lignan glycoside extracted from a traditional Chinese medicine Forsythia suspensa (Thunb.) Vahl (Oleaceae). It mainly exists in the roots, stems, leaves and fruits of the plant, with the highest content in the leaves. In terms of its medicinal application, there are a large number of experimental data proving its pharmacological effects in vitro and in animal models, such as anti-inflammatory, anti-obesity, anti-tumor, etc. Furthermore, pharmacokinetic experiments have also shown phillyrin’s high effectiveness and low toxicity. Despite more than one thousand studies in the literature on phillyrin retrievable from Web of Science, PubMed, and CNKI, few reviews on its pharmacological activities have been presented conclusively. In this paper, we aimed to summarize the pharmacological and pharmacokinetic characteristics of phillyrin from the current literature, focusing on its anti-inflammatory, anti-aging, antiviral, antibacterial, hepatoprotective and anti-cancer effects, hoping to come up with new insights for its application as well as future studies.

[1]  Jie Zhou,et al.  Phillyrin ameliorates diabetic nephropathy through the PI3K/Akt/GSK-3β signalling pathway in streptozotocin-induced diabetic mice , 2021, Human & experimental toxicology.

[2]  Mina Lee,et al.  Bioactivity-Guided Extract Optimization of Osmanthus fragrans var. aurantiacus Leaves and Anti-Inflammatory Activities of Phillyrin , 2021, Plants.

[3]  Zilin Chen,et al.  Identification and quantification of the bioactive components in Osmanthus fragrans roots by HPLC-MS/MS , 2020, Journal of pharmaceutical analysis.

[4]  D. Zhong,et al.  Sulfation predominates the pharmacokinetics, metabolism, and excretion of forsythin in humans: major enzymes and transporters identified , 2020, Acta pharmacologica Sinica.

[5]  R. Bauer,et al.  Challenges at the Time of COVID-19: Opportunities and Innovations in Antivirals from Nature , 2020, Planta Medica.

[6]  Xiaolong Yao,et al.  Phillyrin protects mice from traumatic brain injury by inhibiting the inflammation of microglia via PPARγ signaling pathway. , 2020, International immunopharmacology.

[7]  Dong Zhang,et al.  Phillyrin Relieves Lipopolysaccharide-Induced AKI by Protecting Against Glycocalyx Damage and Inhibiting Inflammatory Responses , 2019, Inflammation.

[8]  Mei Liu,et al.  Phillyrin Attenuates Osteoclast Formation and Function and Prevents LPS-Induced Osteolysis in Mice , 2019, Front. Pharmacol..

[9]  Fatma S. A. Saadeldeen,et al.  The Mechanism of Phillyrin from the Leaves of Forsythia suspensa for Improving Insulin Resistance , 2019, BioMed research international.

[10]  Yan-Yan Chen,et al.  A Ferulic Acid Derivative FXS-3 Inhibits Proliferation and Metastasis of Human Lung Cancer A549 Cells via Positive JNK Signaling Pathway and Negative ERK/p38, AKT/mTOR and MEK/ERK Signaling Pathways , 2019, Molecules.

[11]  Qing He,et al.  Combining use of Phillyrin and autophagy blocker alleviates laryngeal squamous cell carcinoma via AMPK/mTOR/p70S6K signaling , 2019, Bioscience reports.

[12]  W. Chu,et al.  Phillyrin is an effective inhibitor of quorum sensing with potential as an anti-Pseudomonas aeruginosa infection therapy , 2019, The Journal of veterinary medical science.

[13]  A. Dzutsev,et al.  Cell‐Type‐Specific Responses to Interleukin‐1 Control Microbial Invasion and Tumor‐Elicited Inflammation in Colorectal Cancer , 2019, Immunity.

[14]  Zhaoyi Wang,et al.  Phytochemistry, pharmacology, quality control and future research of Forsythia suspensa (Thunb.) Vahl: A review. , 2018, Journal of ethnopharmacology.

[15]  Hong-Bo Xiao,et al.  Phillyrin lowers body weight in obese mice via the modulation of PPAR/-ANGPTL 4 pathway. , 2017, Obesity research & clinical practice.

[16]  Xiangjun Zhou,et al.  Protective Effect of Phillyrin on Lethal LPS-Induced Neutrophil Inflammation in Zebrafish , 2017, Cellular Physiology and Biochemistry.

[17]  Z. Lun,et al.  Evaluating the safety of forsythin from Forsythia suspensa leaves by acute and sub-chronic oral administration in rodent models. , 2017, Asian Pacific journal of tropical medicine.

[18]  Q. Hu,et al.  Identification of flavonoids from Flammulina velutipes and its neuroprotective effect on pheochromocytoma-12 cells. , 2016, Food chemistry.

[19]  Jing Yang,et al.  Protective effects of phillyrin against influenza A virus in vivo , 2016, Archives of pharmacal research.

[20]  Lantong Zhang,et al.  Metabolic profile of phillyrin in rats obtained by UPLC-Q-TOF-MS. , 2016, Biomedical chromatography : BMC.

[21]  J. Arthur,et al.  Subverting Toll-Like Receptor Signaling by Bacterial Pathogens , 2015, Front. Immunol..

[22]  W. Liu,et al.  Pharmacokinetic of 5 components after oral administration of Fructus Forsythiae by HPLC-MS/MS and the effects of harvest time and administration times. , 2015, Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.

[23]  Jian-Guo Jiang,et al.  Active ingredients from natural botanicals in the treatment of obesity , 2014, Obesity reviews : an official journal of the International Association for the Study of Obesity.

[24]  K. Nho,et al.  An ethyl acetate fraction derived from Houttuynia cordata extract inhibits the production of inflammatory markers by suppressing NF-кB and MAPK activation in lipopolysaccharide-stimulated RAW 264.7 macrophages , 2014, BMC Complementary and Alternative Medicine.

[25]  Yingli Lu,et al.  Phillyrin, a Natural Lignan, Attenuates Tumor Necrosis Factor α-Mediated Insulin Resistance and Lipolytic Acceleration in 3T3-L1 Adipocytes , 2014, Planta Medica.

[26]  L. Soromou,et al.  Phillyrin attenuates LPS-induced pulmonary inflammation via suppression of MAPK and NF-κB activation in acute lung injury mice. , 2013, Fitoterapia.

[27]  Jin Zhang,et al.  Microwave-assisted extraction followed by RP-HPLC for the simultaneous extraction and determination of forsythiaside A, rutin, and phillyrin in the fruits of Forsythia suspensa. , 2013, Journal of separation science.

[28]  Qing-Hua Zhang,et al.  Phillyrin produced by Colletotrichum gloeosporioides, an endophytic fungus isolated from Forsythia suspensa. , 2012, Fitoterapia.

[29]  E. Degerman,et al.  From PDE3B to the regulation of energy homeostasis. , 2011, Current opinion in pharmacology.

[30]  R. Elias,et al.  Chionanthus Virginicus L.: Phytochemical Analysis and Quality Control of Herbal Drug and Herbal Preparations , 2011, Natural product communications.

[31]  I. Khan,et al.  Quantitative determination of 10 phenylpropanoid and lignan compounds in Lancea tibetica by high-performance liquid chromatography with UV detection. , 2011, Planta medica.

[32]  J. Kwak,et al.  Cytotoxic phenolic compounds from Chionanthus retusus , 2009, Archives of pharmacal research.

[33]  M. Kikuchi,et al.  Lignan glycosides from the leaves of Osmanthus heterophyllus , 2008, Journal of Natural Medicines.