Antidermatophyte Activity of the Gentiopicroside-Rich n-Butanol Fraction from &lt;b&gt;&lt;i&gt;Gentiana siphonantha&lt;/i&gt;&lt;/b&gt; Maxim. Root on a Guinea Pig Model of Dermatophytosis

Zhou, Wenna; Ouyang, Jie; Wang, HongLun; Wang, Xiaoyan

doi:10.1159/000492384

Cited by 10 publications

(4 citation statements)

References 36 publications

(43 reference statements)

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“… 6 Gentiopicroside is a well-known chemical constituent present as a major constituent in G. lutea roots, it has various biological effects like antifungal, antibacterial, anti-inflammatory, hepatoprotective, and free radical-scavenging activities. 7 In our research, we focused on the wound healing activity of GPS that might be attributed to its free radical scavenger property, antimicrobial effect, and enhancing the synthesis of collagen fibers via supporting the vascularity, suppressing cell damage, and improving cellular migration/proliferation. 8 Furthermore, the antimicrobial activity of GPS has been individually investigated against Staphylococcus aureus because it is a broadly distributed pathogenic bacteria that are responsible for different diseases.…”

Section: Introductionmentioning

confidence: 99%

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

Almukainzi

El‐Masry

Negm

et al. 2022

IJN

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Purpose Gentiopicroside (GPS), an adequate bioactive candidate, has a promising approach for enhancing wound healing due to its antioxidant and antimicrobial properties. Its poor aqueous solubility negatively affects oral absorption accompanied by low bioavailability due to intestinal/hepatic first-pass metabolism. Our aim in this study is to fabricate GPS into appropriate nanocarriers (PLGA nanospheres, NSs) to enhance its solubility and hence its oral absorption would be improved. Methods Normal and ODS silica gel together with Sephadex LH20 column used for isolation of GPS from Gentiana lutea roots. Crude GPS would be further processed for nanospheres fabrication using a single o/w emulsion solvent evaporation technique followed by in vitro optimization study to examine the effect of two formulation variables: polymer (PLGA) and stabilizer (PVA) concentrations on the physical characterizations of prepared NSs. Possible GPS-PLGA chemical and physical interactions have been analyzed using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The optimum GPS-PLGA NSs have been chosen for antimicrobial study to investigate its inhibitory action on Staphylococcus aureus compared with unloaded GPS NSs. Also, a well-designed in vivo study on streptozotocin-induced diabetic rats has been performed to examine the wound healing effect of GPS-PLGA NSs followed by histological examination of wound incisions at different day intervals throughout the study. Results The optimum GPS PLGA NSs (F5) with well-controlled particle size (250.10±07.86 nm), relative high entrapment efficiency (83.35±5.71), and the highest % cumulative release (85.79±8.74) have increased the antimicrobial activity as it exhibited a higher inhibitory effect on bacterial growth than free GPS. F5 showed a greater enhancing impact on wound healing and a significant stimulating effect on the synthesis of collagen fibers compared with free GPS. Conclusion These findings demonstrate that loading GPS into PLGA NSs is considered a promising strategy ensuring optimum GPS delivery for potential management of wounds.

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Section: Introductionmentioning

confidence: 99%

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

Almukainzi

El‐Masry

Negm

et al. 2022

IJN

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“…In order to identify the changes in the apparent structure of T. rubrum (CMCC(F)T1d), SEM observation was performed in accordance with previous research [30]. After exposure to PB (0:5 × MIC, 1 × MIC, and 2 × MIC) and TBF (1 × MIC), T. rubrum cells were fixed at 4 °C with 2.5% (v/v) glutaraldehyde in PBS (0.01 M, pH 7.2) for 4 h. The fixed samples were washed with the same buffer twice each for 10 min and dehydrated through a graded ethanol series (50%, 70%, 80%, 90%, 95%, and 100%) for 15 min at room temperature.…”

Section: Scanning Electron Microscopy (Sem)mentioning

confidence: 99%

Isoflavaspidic Acid PB Extracted from Dryopteris fragrans (L.) Schott Inhibits Trichophyton rubrum Growth via Membrane Permeability Alternation and Ergosterol Biosynthesis Disruption

Zhang

Liu

Shen

et al. 2022

BioMed Research International

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Isoflavaspidic acid PB (PB), a phloroglucinol derivative extracted from aerial parts of Dryopteris fragrans (L.) Schott, had antifungal activity against several dermatophytes. This study was aimed at exploring the antifungal mechanism of PB against Trichophyton rubrum (T. rubrum). The effectiveness of PB in inhibiting T. rubrum growth was detected by time-kill kinetics study and fungal biomass determination. Studies on the mechanism of action were investigated using scanning electron microscopy (SEM), transmission electron microscopy (TEM), sorbitol and ergosterol assay, nucleotide leakage measurement, and UPLC-based test and enzyme-linked immunosorbent assay. Fungicidal activity of PB was concentration- and time-dependent at 2 × MIC (MIC: 20 μg/mL) after 36 h. The total biomass of T. rubrum was reduced by 64.17%, 77.65%, and 84.71% in the presence of PB at 0.5 × MIC , 1 × MIC , and 2 × MIC , respectively. SEM analysis showed that PB changed mycelial morphology, such as shrinking, twisting, collapsing, and even flattening. TEM images of treated cells exhibited abnormal distributions of polysaccharide particles, plasmolysis, and cytoplasmic content degradation accompanied by plasmalemma disruption. There were no changes in the MIC of PB in the presence of sorbitol. However, the MIC values of PB were increased by 4-fold with exogenous ergosterol. At 4 h and 8 h, PB increased nucleotide leakage. Besides, ergosterol content in T. rubrum membrane treated with PB at 0.5 × MIC , 1 × MIC , and 2 × MIC was decreased by 9.58%, 15.31%, and 76.24%, respectively. There was a dose-dependent decrease in the squalene epoxidase (SE) activity. And the reduction in the sterol 14α-demethylase P450 (CYP51) activity was achieved after PB treatments at 1 × MIC and 2 × MIC . These results suggest that PB displays nonspecific action on the cell wall. The membrane damaging effects of PB were attributed to binding with ergosterol to increase membrane permeability and interfering ergosterol biosynthesis involved with the reduction of SE and CYP51 activities. Further study is needed to develop PB as a natural antifungal candidate for clinical use.

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“…Gentiopicroside (GPS, C 16 H 20 O 9 , Figure 1(a)) is a secoiridoid glucoside that is isolated from the roots of perennial herbs in the Gentianaceae family, such as Gentiana straminea Maxim., Gentiana macrophylla Pall., Gentiana manshurica Kitag., Gentiana dahurica Fisch., and Gentiana scabra Bge., which are used widely as medicinal herbs in China for the treatment of rheumatoid arthritis, hemiplegia, arthralgia, stroke, and hypertension [19]. GPS has been proven to display potential protective effects against osteoarthritis, hepatitis, diabetic renal fibrosis, osteoclastogenesis, and alcoholic hepatosteatosis [20].…”

Section: Introductionmentioning

confidence: 99%

Gentiopicroside Produces Endothelium-Independent Vasodilation by Deactivating the PI3K/Akt/Rho-Kinase Pathway in Isolated Rat Thoracic Aorta

Xing

Nong

Qin

et al. 2021

BioMed Research International

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Gentiopicroside (GPS), a main active secoiridoid glucoside derived from the roots of perennial herbs in the Gentianaceae family, has antispasmodic and relaxant effects. However, the vasorelaxant effects of GPS on aortic rings and the molecular mechanisms involved in these effects are not yet clear. Therefore, we investigated whether GPS inhibits phenylephrine- (PE-) or KCl-induced contractions in isolated rat thoracic aortic rings. The present study found that GPS produced a dose-dependent relaxation in aortic rings precontracted with PE or KCl and significantly reduced CaCl2-, narciclasine- (Rho-kinase activator-), and phorbol-12,13-diacetate- (PKC activator-) induced vasocontractions. Pretreatment with NG-Nitroarginine methyl ester hydrochloride (L-NAME, NOS inhibitor), methylene blue (sGC inhibitor), indomethacin (COX inhibitor), 4-aminopyridine (KV channel inhibitor), and glibenclamide (KATP channel inhibitor) had no influence on the vasorelaxant effect of GPS, while BaCl2 (Kir channel inhibitor), tetraethylammonium chloride (KCa channel inhibitor), ruthenium red (RYR inhibitor), and heparin (IP3R inhibitor) significantly reduced GPS-induced vasorelaxation. Moreover, GPS pretreatment remarkably inhibited the influx of Ca2+ in vascular smooth muscle cells stimulated using KCl or PE-containing CaCl2 solution. Western blot analysis confirmed that GPS treatment inhibited PE-induced increases in the protein levels of p-Akt, p-myosin light chain (MLC), and p-myosin-binding subunit of myosin phosphatase 1 (MYPT1) in the aortic rings. Additionally, the vasorelaxation activity of GPS was attenuated upon pretreatment with LY294002 (PI3K/Akt inhibitor), Y27632 (Rho-kinase inhibitor), and verapamil (L-type Ca2+ channel inhibitor). These findings demonstrate that GPS exhibits endothelium-independent vasorelaxant effects through inhibition of voltage-dependent, receptor-operated, and inositol triphosphate receptor (IP3R)/ryanodine receptor- (RYR-) mediated Ca2+ channels as well as the PI3K/Akt/Rho-kinase signaling pathway.

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Antidermatophyte Activity of the Gentiopicroside-Rich n-Butanol Fraction from <b><i>Gentiana siphonantha</i></b> Maxim. Root on a Guinea Pig Model of Dermatophytosis

Cited by 10 publications

References 36 publications

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

Gentiopicroside PLGA Nanospheres: Fabrication, in vitro Characterization, Antimicrobial Action, and in vivo Effect for Enhancing Wound Healing in Diabetic Rats

Isoflavaspidic Acid PB Extracted from Dryopteris fragrans (L.) Schott Inhibits Trichophyton rubrum Growth via Membrane Permeability Alternation and Ergosterol Biosynthesis Disruption

Gentiopicroside Produces Endothelium-Independent Vasodilation by Deactivating the PI3K/Akt/Rho-Kinase Pathway in Isolated Rat Thoracic Aorta

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