Chemistry and pharmacology of the herb pair Flos Lonicerae japonicae-Forsythiae fructus

Guo, Yiping; Lin, Ligen; Wang, Yitao

doi:10.1186/s13020-015-0044-y

Cited by 39 publications

(26 citation statements)

References 70 publications

(52 reference statements)

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“…TCMs as well as purified natural products also provide a rich resource for novel antiviral drug development. Several herbal medicines and natural products have shown antiviral activities against viral pathogens (8)(9)(10)(11). Among these, the roots of Scutellaria baicalensis Georgi (Huangqin in Chinese) are frequently used in TCM for the prophylaxis and treatment of hepatitis and respiratory disorders (12)(13)(14).…”

Section: Introductionmentioning

confidence: 99%

Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL proteasein vitro

Yao

Zhao

et al. 2020

Preprint

138

150

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Human infections with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) cause coronavirus disease 19 and there is currently no cure. The 3C-like protease (3CLpro), a highly conserved protease indispensable for replication of coronaviruses, is a promising target for development of broad-spectrum antiviral drugs. To advance the speed of drug discovery and development, we investigated the inhibition of SARS-CoV-2 3CLpro by natural products derived from Chinese traditional medicines. Baicalin and baicalein were identified as the first non-covalent, non-peptidomimetic inhibitors of SARS-CoV-2 3CLpro and exhibited potent antiviral activities in a cell-based system. Remarkably, the binding mode of baicalein with SARS-CoV-2 3CLpro determined by X-ray protein crystallography is distinctly different from those of known inhibitors. Baicalein is perfectly ensconced in the core of the substrate-binding pocket by interacting with two catalytic residues, the crucial S1/S2 subsites and the oxyanion loop, acting as a "shield" in front of the catalytic dyad to prevent the peptide substrate approaching the active site. The simple chemical structure, unique mode of action, and potent antiviral activities in vitro, coupled with the favorable safety data from clinical trials, emphasize that baicalein provides a great opportunity for the development of critically needed anti-coronaviral drugs.

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Section: Introductionmentioning

confidence: 99%

Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL proteasein vitro

Yao

Zhao

et al. 2020

Preprint

138

150

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“…More than 100 compounds have been identified from FF, and the major constituents of FF include quercetin, rutaecarpine, forsythiaside A, betulinic acid, and forsythialan A [16]. Recent pharmacological research indicates that forsythiaside, forsythin, and rutin are responsible for the biological activities of FF [26][27][28].…”

Section: Resultsmentioning

confidence: 99%

“…(F. suspensa) Vahl is widely distributed in China, Japan, Korea, and many European countries. The dried fruit of this plant, Forsythiae fructus (FF), locally named "Yeon-Gyo", is a well-known herbal medicine in Korea for the treatment of inflammatory diseases, diuretics, and infectious diseases [16]. FF has many bioactive components such as triterpenoids, lignans, its inhibition.…”

Section: Introductionmentioning

confidence: 99%

Forsythiae Fructus Induces VEGF Production via p38 MAPK Activation in Human Keratinocytes

김미선¹,

Choi²,

박선규³

et al. 2016

Journal of the Society of Cosmetic Scientists of Korea

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Cutaneous microvasculature plays a critical role in age-associated skin changes. A considerable reduction of number and size of vessels has been observed in the upper dermis of elderly skin. Forsythiae fructus (FF), the dried fruit of plant Forsythia suspensa (F. suspensa), has been traditionally used as an herbal medicine to treat inflammatory diseases and bacterial diseases. However, its regulatory effect on angiogenic responses has not been elucidated in skin. Therefore, we analyzed secretory profiles upon treatment of FF extract using array designed to detect angiogenesis-associated mediators in human keratinocytes. Because keratinocyte-derived VEGF (vascular endothelial growth factor) has been regarded as a potent factor for new microvasculature under the epidermis, we further investigated the effect of FF extract on VEGF production. We observed that the VEGF expression of mRNA and protein level was increased by about 2 folds in a dose-dependent manner after FF extract treatment. In signaling experiments, FF extract induced rapid p38 MAPK activation within 5 min, and the activation was totally abrogated by pretreatment with a p38 MAPK specific inhibitor. The FF-induced VEGF upregulation was also significantly attenuated by a p38 MAPK

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“…[5] The genus Echinops comprises 125 -130 species and belongs to the Asteraceae/Compositae family distributed in semi-arid zones of tropical and northern Africa, Mediterranean basin and temperate regions up to Central Asia. [6] Chemical investigation on some Echinops species demonstrated the presence of polyacetylene thiophenes, [7] alkaloids, [8] flavone glycosides [9] and benzothiophene glycosides. [10] In Tunisia, this genus is represented by two species Echinops strigosus L. and Echinops spinosissimus TURRA.…”

Section: Introductionmentioning

confidence: 99%

Hexane Extract of Echinops spinosissimus Turra subsp. spinosus from Tunisia: A Potential Source of Acetylated Sterols – Investigation of its Biological Activities

Bouattour

Fakhfakh

Dammak

et al. 2016

Chemistry & Biodiversity

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The hexane extract of Echinops spinosissimus Turra subsp. spinosus flower heads was analyzed for its fatty acid and sterol composition. Its physicochemical characteristics were also studied. The saponification, iodine and peroxide values were determined as 255 mg KOH/g, 42.57 g I /100 g and 110 m equiv. O /kg of oil, respectively. The oleic (C18:1; 61.14%), palmitic (C16:0; 21.36%) and linoleic (C18:2; 10.45%) acids were the dominant fatty acids. This extract was also found to contain high levels of β-sitosterol and stigmasterol (44.97% and 34.95% of total sterols, respectively). On the other hand, the identification of terpenoid compounds was investigated by using GC/MS, which revealed fourteen major terpenoids mainly taraxasterol, lupeol, pseudotaraxasterol, lup-22(29)-en-3-yl acetate, taraxasteryl acetate, α-amyrin, β-amyrin, pseudotaraxasteryl acetate, hop-20(29)-en3-β-ol, α-amirenone, along with β-sitosterol and stigmasterol. Moreover, we have evaluated the in vitro antibacterial and antifungal activities of the unsaponifiable matter and a fraction isolated from this extract. These activities were conducted using the diffusion disc methods and broth microdilution assay. The resulted fraction from this extract showed the highest antibacterial activity with significant minimum inhibitory concentrations (MIC) values 125.0 μg/ml against Staphylococcus aureus, Micrococcus luteus and Bacillus cereus. However, it did exhibit no substantial antifungal activity.

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Chemistry and pharmacology of the herb pair Flos Lonicerae japonicae-Forsythiae fructus

Cited by 39 publications

References 70 publications

Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL proteasein vitro

Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL proteasein vitro

Forsythiae Fructus Induces VEGF Production via p38 MAPK Activation in Human Keratinocytes

Hexane Extract of Echinops spinosissimus Turra subsp. spinosus from Tunisia: A Potential Source of Acetylated Sterols – Investigation of its Biological Activities

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