Chemical Constituents and Anti-inflammatory Principles from the Fruits of <i>Forsythia suspensa</i>

Kuo, Ping Chung; Hung, Hsin Yi; Nian, Chi-Wei; Hwang, Tsong‐Long; Cheng, Ju‐Chien; Kuo, Daih‐Huang; Lee, E-Jian; Tai, Shih‐Huang; Wu, Tzi Yi

doi:10.1021/acs.jnatprod.6b01141

Cited by 45 publications

(18 citation statements)

References 47 publications

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“…Although the potency of the lignans exhibiting anti-inflammatory activity in this study was similar to bioactive lignans described in the literature [ 42 ], it is worth noting that most of the lignans with anti-inflammatory activity in this study have not been reported previously. Besides, there are no anti-inflammatory medicines act via inhibiting superoxide anion and neutrophil elastase.…”

Section: Discussionsupporting

confidence: 74%

“…Besides, butanolides and lignans were major skeletons in this study. Bioactivity results indicated that lignans could reduce superoxide anion generation in fMLP/CB-stimulated human neutrophils, and the anti-inflammatory activities of those compounds were as potent as compounds in the literature [ 42 ]. Furthermore, the structure-activity relationship (SAR) discussion of anti-inflammatory activity compounds indicated that furofuran lignan with methylenedioxy was the most active structure.…”

Section: Discussionmentioning

confidence: 99%

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Phytochemical Investigation and Anti-Inflammatory Activity of the Leaves of Machilus japonica var. kusanoi

Hwang

et al. 2020

Molecules

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In a series of anti-inflammatory screenings of lauraceous plants, the methanolic extract of the leaves of Machilus japonica var. kusanoi (Hayata) J.C. Liao showed potent inhibition on both superoxide anion generation and elastase release in human neutrophils. Bioassay-guided fractionation of the leaves of M. japonica var. kusanoi led to the isolation of twenty compounds, including six new butanolides, machinolides A–F (1–6), and fourteen known compounds (7–20). Their structures were characterized by 1D and 2D NMR, UV, IR, CD, and MS data. The absolute configuration of the new compounds were unambiguously confirmed by single-crystal X-ray diffraction analyses (1, 2, and 3) and Mosher’s method (4, 5, and 6). In addition, lignans, (+)-eudesmin (11), (+)-methylpiperitol (12), (+)-pinoresinol (13), and (+)-galbelgin (16) exhibited inhibitory effects on N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation in human neutrophils with IC50 values of 8.71 ± 0.74 μM, 2.23 ± 0.92 μM, 6.81 ± 1.07 μM, and 7.15 ± 2.26 μM, respectively. The results revealed the anti-inflammatory potentials of Formosan Machilus japonica var. kusanoi.

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Section: Discussionsupporting

confidence: 74%

Section: Discussionmentioning

confidence: 99%

Phytochemical Investigation and Anti-Inflammatory Activity of the Leaves of Machilus japonica var. kusanoi

Hwang

et al. 2020

Molecules

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“…As shown in Figure 4 , two iridoids ( 121 – 122 ), nineteen diterpenoids ( 123 – 141 ) and twenty-seven triterpenoids ( 142 – 168 ) have been confirmed in Forsythiae Fructus . Most of them were reported by Kuo et al [ 38 ] in 2017. The triterpenoid fraction contains eleven tetracyclic triterpenoids ( 142 – 152 ) and sixteen pentacyclic triterpenoids ( 136 – 151 ).…”

Section: Phytochemistrymentioning

confidence: 99%

Forsythiae Fructus: A Review on its Phytochemistry, Quality Control, Pharmacology and Pharmacokinetics

Zhao

Tong

et al. 2017

Molecules

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Forsythiae Fructus, as a traditional Chinese medicine, has been widely used both as a single herb and in compound prescriptions in Asia, mainly due to its heat-clearing and detoxifying effects. Modern pharmacology has proved Forsythiae Fructus possesses various therapeutic effects, both in vitro and in vivo, such as anti-inflammatory, antibacterial and antiviral activities. Up to now, three hundred and twenty-one compounds have been identified and sensitive analytical methods have been established for its quality control. Recently, the pharmacokinetics of Forsythiae Fructus and its bioactive compounds have been reported, providing valuable information for its clinical application. Therefore, this systematic review focused on the newest scientific reports on Forsythiae Fructus and extensively summarizes its phytochemistry, pharmacology, pharmacokinetics and standardization procedures, especially the difference between the two applied types—unripe Forsythiae Fructus and ripe Forsythiae Fructus—in the hope of providing a helpful reference and guide for its clinical applications and further studies.

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“…Forsythia suspensa (F. suspensa) exhibits anti-bacterial, anti-inflammatory, antioxidant, anti-allergy, anti-virus and anti-cancer effects [2]. So far, more than 230 compounds have been separated and identified from F. suspensa [2], including phenylethanoid glycosides [3], flavonoids [4], triterpenoids [5], lignans [6] and other compounds. Phillygenin (PG), a bisepoxylignan compound [7], is one of the major ingredients in F. suspensa and has been used as a marker for the quality control of F. suspensa in several studies.…”

Section: Introductionmentioning

confidence: 99%

Self-Microemulsifying Drug Delivery System of Phillygenin: Formulation Development, Characterization and Pharmacokinetic Evaluation

et al. 2020

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Phillygenin, as an active ingredient of Forsythia suspensa, possesses a wide range of biological and pharmacological activity. However, its development and application are restricted due to its poor bioavailability and low solubility. Our work aimed to develop a self-microemulsifying drug delivery system to improve the oral bioavailability of phillygenin. The composition of the self-microemulsifying drug delivery system was preliminary screened by the pseudo-ternary phase diagram. Subsequently, the central composite design method was employed to optimize the prescription of the self-microemulsifying drug delivery system loaded with phillygenin. The prepared self-microemulsifying drug delivery system of phillygenin was characterized in terms of morphology, droplet size distribution, polydispersity index and stability. Then, the in vitro dissolution and the oral bioavailability were analyzed. The optimized self-microemulsifying drug delivery system of phillygenin consisted of 27.8% Labrafil M1944CS, 33.6% Cremophor EL, 38.6% polyethylene glycol 400 (PEG-400) and 10.2 mg/g phillygenin loading. The prepared self-microemulsifying drug delivery system of phillygenin exhibited spherical and uniform droplets with small size (40.11 ± 0.74 nm) and satisfactory stability. The in vitro dissolution experiment indicated that the cumulative dissolution rate of the self-microemulsifying drug delivery system of phillygenin was significantly better than that of free phillygenin. Furthermore, after oral administration in rats, the bioavailability of phillygenin was significantly enhanced by the self-microemulsifying drug delivery system. The relative bioavailability of the self-microemulsifying drug delivery system of phillygenin was 588.7% compared to the phillygenin suspension. These findings suggest that the self-microemulsifying drug delivery system of phillygenin can be a promising oral drug delivery system to improve the absorption of phillygenin.

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Chemical Constituents and Anti-inflammatory Principles from the Fruits of Forsythia suspensa

Cited by 45 publications

References 47 publications

Phytochemical Investigation and Anti-Inflammatory Activity of the Leaves of Machilus japonica var. kusanoi

Phytochemical Investigation and Anti-Inflammatory Activity of the Leaves of Machilus japonica var. kusanoi

Forsythiae Fructus: A Review on its Phytochemistry, Quality Control, Pharmacology and Pharmacokinetics

Self-Microemulsifying Drug Delivery System of Phillygenin: Formulation Development, Characterization and Pharmacokinetic Evaluation

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