Attenuation of dermal wounds through topical application of ointment containing phenol enriched fraction of Caesalpinia mimosoides Lam.

Bhat, Pradeep; Upadhya, Vinayak; Hegde, Ganesh; Hegde, Harsha V.; Roy, Subarna

doi:10.3389/fphar.2022.1025848

Cited by 3 publications

(11 citation statements)

References 66 publications

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“…The cell migration activity of all the samples against L929 cells was performed through scratch wound assay as described in our previous study (Bhat et al, 2022). The cells were seeded in 24-well plates (TC plate, sterile, 24 F wells, Tarsons) containing complete medium, followed by incubation.…”

Section: In Vitro Wound-healing Activity Through Scratch Wound Assaymentioning

confidence: 99%

“…The antimicrobial property of all the samples was performed using tube dilution assay against bacterial and fungal pathogens causing wound infections (Bhat et al, 2022) ). Peptone water was used to prepare the bacterial and fungal suspension cultures and they were incubated for 18-24 h at 37 °C.…”

Section: In Vitro Antimicrobial Assaymentioning

confidence: 99%

“…The experimental rats were anesthetized through the open mask method before wound creation (Bhat et al, 2022). A day prior to starting the experiment, the fur from the dorsal area of the animals was cleanly shaved with an electric shaver and disinfected with 70% ethanol.…”

Section: Circular Excision Wound Modelmentioning

confidence: 99%

“…In our earlier studies, the wound-healing activity of crude ethanol extract of C.mimosoides was scientifically evaluated (Bhat et al, 2016). Further, phenolic enrichment of bioactive crude ethanol extract was performed through a sequential liquid-liquid partition process, and the resulting phenol-enriched fraction (PEF) was evaluated for wound-healing properties, followed by antioxidant, antimicrobial, and anti-inflammatory activities (Bhat et al, 2022). The effective wound-healing activity of PEF over crude ethanol extract has created an interest to take it for further bioassay-guided fractionation process to get a pure and biologically active compound, "ethyl gallate" (EG).…”

Section: Introductionmentioning

confidence: 99%

“…The powdered material [1 kg dry weight (d.w.)] was sequentially extracted with the solvents (n-hexane, chloroform, acetone, ethanol, and water) of increasing polarity and dielectric constants through the hot percolation method using Soxhlet apparatus (Bhat et al, 2016). The active ethanol extract with potent wound-healing activity was further processed for the enrichment of phenols using liquid-liquid partition procedure as described in our earlier publication (Bhat et al, 2022). The resulting PEF was further dried using a rotary evaporator (Heidolph Laborota 4000), with a yield of 28.90 ± 0.64% (d.w.), and it was stored at 4 °C in a refrigerator for further experimental use.…”

Section: Introductionmentioning

confidence: 99%

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Ethyl gallate isolated from phenol-enriched fraction of Caesalpinia mimosoides Lam. Promotes cutaneous wound healing: a scientific validation through bioassay-guided fractionation

et al. 2023

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The tender shoots of Caesalpinia mimosoides Lam. are used ethnomedically by the traditional healers of Uttara Kannada district, Karnataka (India) for the treatment of wounds. The current study was aimed at exploring phenol-enriched fraction (PEF) of crude ethanol extract of tender shoots to isolate and characterize the most active bio-constituent through bioassay-guided fractionation procedure. The successive fractionation and sub-fractionation of PEF, followed by in vitro scratch wound, antimicrobial, and antioxidant activities, yielded a highly active natural antioxidant compound ethyl gallate (EG). In vitro wound healing potentiality of EG was evidenced by a significantly higher percentage of cell migration in L929 fibroblast cells (97.98 ± 0.46% at 3.81 μg/ml concentration) compared to a positive control group (98.44 ± 0.36%) at the 48th hour of incubation. A significantly higher rate of wound contraction (98.72 ± 0.41%), an elevated tensile strength of the incised wound (1,154.60 ± 1.42 g/mm2), and increased quantity of connective tissue elements were observed in the granulation tissues of the 1% EG ointment treated animal group on the 15th post-wounding day. The accelerated wound healing activity of 1% EG was also exhibited by histopathological examinations through Hematoxylin and Eosin, Masson’s trichome, and Toluidine blue-stained sections. Significant up-regulation of enzymatic and non-enzymatic antioxidant contents (reduced glutathione, superoxide dismutase, and catalase) and down-regulation of oxidative stress marker (lipid peroxidation) clearly indicates the effective granular antioxidant activity of 1% EG in preventing oxidative damage to the skin tissues. Further, in vitro antimicrobial and antioxidant activities of EG supports the positive correlation with its enhanced wound-healing activity. Moreover, molecular docking and dynamics for 100 ns revealed the stable binding of EG with cyclooxygenase-2 (−6.2 kcal/mol) and matrix metalloproteinase-9 (−4.6 kcal/mol) and unstable binding with tumor necrosis factor-α (−7.2 kcal/mol), suggesting the potential applicability of EG in inflammation and wound treatment.

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Section: In Vitro Wound-healing Activity Through Scratch Wound Assaymentioning

confidence: 99%

Section: In Vitro Antimicrobial Assaymentioning

confidence: 99%

Section: Circular Excision Wound Modelmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Ethyl gallate isolated from phenol-enriched fraction of Caesalpinia mimosoides Lam. Promotes cutaneous wound healing: a scientific validation through bioassay-guided fractionation

et al. 2023

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Integrative Computational Approaches to Assess Anti-Influenza Activity in Caesalpinia mimosoides Lamk Hydroethanolic Extract

Klamrak,

Rahman,

Nopkuesuk

et al. 2024

Preprint

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In a recent study, we used chemical analysis to show that the Caesalpinia mimosoides aqueous extract, which contains a high concentration of simple phenolics, has strong anti-influenza activity. We determined through molecular docking methods that its potential target inhibitor is the neuraminidase. Therefore, our study objectives were to evaluate whether the aqueous-ethanol extract (30% v/v) of this plant species exhibits greater antiviral activity than the aqueous plant extract. The C. mimosoides hydroethanolic extract exhibited potent antioxidant activity in the DPPH assay, with an IC50 value of 15.01 µg/mL, comparable to authentic quercetin (IC50 = 12.72 µg/mL) and approximately 4.91 times greater than standard gallic acid (IC50 = 3.06 µg/mL). Through untargeted metabolomic analyses (UPLC-ESI(±)-QTOF-MS/MS) and subsequent stepwise computational metabolomics analyses, we identified the extract as primarily containing simple phenolics (e.g., gallic acid, ellagic acid, shikimic acid, and chlorogenic acid), flavonoid derivatives (e.g., quercetin, taxifolin, myricitrin, and afzelin), and other bioactive components, including dicarboxylic acids and germacrone. The polyphenol-rich extract showed strong anti-influenza activity, with an IC50 of 2.33 µg/mL against the influenza A/PR/8/34 virus and no cytotoxic effects, as indicated by a CC50 greater than 50 µg/mL. This represents an approximately 3.35-fold increase in effectiveness compared to its corresponding aqueous extract (IC50 = 7.81 µg/mL). Furthermore, the extract demonstrated no hemolytic activity, even at a maximum concentration of 2,000 µg/mL, suggesting its potential as a safe antiviral agent. Molecular docking analyses revealed that the identified phytochemicals can simultaneously interact with the "drug-target binding sites" of neuraminidase (NA) and the PB2 subunit of influenza RNA polymerase, indicating their potential polypharmacological effects. Given the consistent efficacy of polyphenols in targeting various viral machinery proteins, we are currently investigating the anti-SARS-CoV-2 properties of our established plant extract to expand its potential applications.

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Unveiling the Potent Antiviral and Antioxidant Activities of an Aqueous Extract from Caesalpinia mimosoides Lamk: Cheminformatics and Molecular Docking Approaches

Klamrak,

Nabnueangsap,

Narkpuk

et al. 2023

Foods

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Our group previously demonstrated that Caesalpinia mimosoides Lamk exhibits many profound biological properties, including anticancer, antibacterial, and antioxidant activities. However, its antiviral activity has not yet been investigated. Here, the aqueous extract of C. mimosoides was prepared from the aerial parts (leaves, stalks, and trunks) to see whether it exerts anti-influenza (H1N1) effects and to reduce the organic solvents consumed during extraction, making it a desirable approach for the large-scale production for medical uses. Our plant extract was quantified to contain 7 g of gallic acid (GA) per 100 g of a dry sample, as determined using HPLC analysis. It also exerts potent antioxidant activities comparable to those of authentic GA. According to untargeted metabolomics (UPLC-ESI(-)-QTOF-MS/MS) with the aid of cheminformatics tools (MetFrag (version 2.1), SIRIUS (version 5.8.3), CSI:FingerID (version 4.8), and CANOPUS), the major metabolite was best annotated as “gallic acid”, phenolics (e.g., quinic acid, shikimic acid, and protocatechuic acid), sugar derivatives, and dicarboxylic acids were deduced from this plant species for the first time. The aqueous plant extract efficiently inhibited an influenza A (H1N1) virus infection of MDCK cells with an IC50 of 5.14 µg/mL. Of equal importance, hemolytic activity was absent for this plant extract, signifying its applicability as a safe antiviral agent. Molecular docking suggested that GA interacts with conserved residues (e.g., Arg152 and Asp151) located in the catalytic inner shell of the viral neuraminidase (NA), sharing the same pocket as those of anti-neuraminidase drugs, such as laninamivir and oseltamivir. Additionally, other metabolites were also found to potentially interact with the active site and the hydrophobic 430-cavity of the viral surface protein, suggesting a possibly synergistic effect of various phytochemicals. Therefore, the C. mimosoides aqueous extract may be a good candidate for coping with increasing influenza virus resistance to existing antivirals.

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Attenuation of dermal wounds through topical application of ointment containing phenol enriched fraction of Caesalpinia mimosoides Lam.

Cited by 3 publications

References 66 publications

Ethyl gallate isolated from phenol-enriched fraction of Caesalpinia mimosoides Lam. Promotes cutaneous wound healing: a scientific validation through bioassay-guided fractionation

Ethyl gallate isolated from phenol-enriched fraction of Caesalpinia mimosoides Lam. Promotes cutaneous wound healing: a scientific validation through bioassay-guided fractionation

Integrative Computational Approaches to Assess Anti-Influenza Activity in Caesalpinia mimosoides Lamk Hydroethanolic Extract

Unveiling the Potent Antiviral and Antioxidant Activities of an Aqueous Extract from Caesalpinia mimosoides Lamk: Cheminformatics and Molecular Docking Approaches

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