In vitro metabolism of helenalin and its inhibitory effect on human cytochrome P450 activity

Šadibolová, Michaela; Juvonen, Risto O.; Auriola, Seppo; Boušová, Iva

doi:10.1007/s00204-021-03218-6

Cited by 2 publications

(2 citation statements)

References 60 publications

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“…Its anti-inflammatory mechanism diverges from that of non-steroidal anti-inflammatory drugs (NSAIDs), attributed mainly to its potent inhibition of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling [6,15]. Furthermore, helenalin-exposed T-Helper Cluster of Differentiation 4+ (TCD4+) cells have shown reduced interleukin-2 (IL-2) production and CD25 expression, suggesting helenalin's potential as an anti-inflammatory therapy [18][19][20]. This is particularly significant in chronic inflammation diseases, where conventional treatments carry risks of adverse events and non-adherence [7,8,[21][22][23][24] Dry Eye Disease (DED) is commonly defined as a "multifactorial disease of the tears and ocular surface that results in symptoms of discomfort, visual disturbance, and tear film instability with potential damage to the ocular surface.…”

Section: Introductionmentioning

confidence: 99%

Enhancing Ocular Surface in Dry Eye Disease Patients: A Clinical Evaluation of a Topical Formulation Containing Sesquiterpene Lactone Helenalin

Ng,

Altamirano-Vallejo,

Navarro-Partida

et al. 2024

Pharmaceuticals

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The aim of this work was to assess the tolerability, safety, and efficacy of an ophthalmic topical formulation containing helenalin from Arnica montana and hyaluronic acid 0.4% (HA) in patients with mild-to-moderate Dry Eye Disease (DED) exhibiting positive Matrix Metalloproteinase 9 (MMP-9) test results. Tolerability and safety were evaluated in 24 healthy subjects. Participants were instructed to apply one drop of the formulation three times a day in the study eye, for 2 weeks, followed by a clinical follow-up of 21 days. Efficacy was studied in 48 DED patients randomized into Study (Group 1/receiving the studied formulation) or Control (Group 2/Receiving HA 0.4% eye lubricant) groups for 1 month. Assessments included an MMP-9 positivity test, conjunctival impression cytology (CIC), Ocular Surface Disease Index (OSDI), non-invasive film tear breakup time (NIBUT), non-invasive average breakup time (NIAvg-BUT), ocular surface staining, Schirmer’s test, and meibomiography. A crossover design with an additional 1-month follow-up was applied to both groups. Healthy subjects receiving the studied formulation exhibited good tolerability and no adverse events. Regarding the efficacy study, Group 1 exhibited a statistically significant reduction in the MMP-9 positivity rate compared to Group 2 (p < 0.001). Both Group 1 and Group 2 exhibited substantial improvements in OSDI and NIBUT scores (p < 0.001). However, Group 1 demonstrated a significant improvement in NI-Avg-BUT and Schirmer’s test scores (p < 0.001), whereas Group 2 did not (p > 0.05). Finally, after the crossover, the proportion of MMP-9-positive subjects in Group 1 increased from 25% to 91.6%, while Group 2 showed a significant decrease from 87.5% to 20.8%. Overall, the topical formulation containing sesquiterpene helenalin from Arnica montana and hyaluronic acid was well tolerated and exhibited a favorable safety profile. Our formulation reduces DED symptomatology and modulates the ocular surface inflammatory process; this is evidenced by the enhancement of CIC, the improvement of DED-related tear film status, and the reduction of the MMP-9 positivity rate.

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Section: Introductionmentioning

confidence: 99%

Enhancing Ocular Surface in Dry Eye Disease Patients: A Clinical Evaluation of a Topical Formulation Containing Sesquiterpene Lactone Helenalin

Ng,

Altamirano-Vallejo,

Navarro-Partida

et al. 2024

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

“…Its anti-inflammatory mechanism diverges from that of non-steroidal antiinflammatory drugs (NSAIDs), attributed mainly to its potent inhibition of nuclear transcriptional factor-ß (NF-ß) signaling (6,16). Helenalin-exposed TCD4 cells have shown reduced interleukin-2 (IL-2) production and CD25 expression, suggesting helenalin's potential as an anti-inflammatory therapy (19)(20)(21). This is particularly significant in chronic inflammation diseases, where conventional treatments carry risks of adverse events and nonadherence (7,9,10,(22)(23)(24) Dry eye disease (DED), characterized by ocular surface inflammation due to hyperosmolarity, is associated with excessive reactive oxygen species (ROS) production, oxidative stress, and inflammation mediated by lymphocytes.…”

Section: Introductionmentioning

confidence: 99%

Modulating Matrix Metalloproteinase-9 and Enhancing Ocular Surface Health in Dry Eye Disease Patients: A Clinical Evaluation of A Topical Formulation Containing Sesquiterpene Lactone Helenalin

Ng,

Altamirano-Vallejo,

Sanchez-Aguilar

et al. 2023

Preprint

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Purpose: To assess the tolerability, safety, and efficacy of an ophthalmic topical formulation containing helenalin from Arnica montana and hyaluronic acid 0.4% (HA) in patients with mild to moderate dry eye disease (DED) exhibiting positive Matrix Metalloproteinase 9 (MMP-9) test results. Methods: Tolerability and safety were evaluated in 24 healthy subjects. Participants were in-structed to routinely apply one drop of the formulation three times a day in the study eye, for a period of two weeks, followed by a clinical follow-up of 21 days. Efficacy was studied in 48 DED patients randomized into Study (Group 1/ receiving the study formulation) or Control (Group 2/ Receiving HA 0.4% eye lubricant) groups, for 4 weeks. Assessments included MMP-9 positivity, conjunctival impression cytology (CIC), Ocular Surface Disease Index (OSDI), non-invasive tear film breakup time (NIF-BUT), non-invasive average breakup time (NIAvg-BUT), ocular surface staining, Schirmer's test, and meibomiography. A crossover design with a four-week follow-up was applied to the control group. Results: Healthy subjects receiving the study formulation exhibited good tolerability and no ad-verse events. Group 1 showed significant MMP-9 reduction (25% positivity rate) unlike Group 2 (87.5% positivity rate). Group 1 displayed improved CIC (33.3% vs. 0% SSD) compared to Group 2 (29.1%). OSDI and NIF-BUT scores improved in both groups (p < 0.001). Only Group 1 showed improved NIAvg-BUT and Schirmer’s test scores (p < 0.001), while Group 2 did not (p > 0.05). MMP-9-positive subjects shifted from 25% to 91.6% in Group 1 and 87.5% to 20.8% in Group 2 after the follow-up. Conclusion: The topical formulation containing helenalin from Arnica montana and hyaluronic acid is well tolerated and has a good safety profile. Our formulation reduces DED sympto-matology and modulates the ocular surface inflammatory process; this is evidenced by the en-hancement of CIC, the improvement of DED-related tear film status, and the reduction of MMP-9 positivity rate.

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In vitro metabolism of helenalin and its inhibitory effect on human cytochrome P450 activity

Cited by 2 publications

References 60 publications

Enhancing Ocular Surface in Dry Eye Disease Patients: A Clinical Evaluation of a Topical Formulation Containing Sesquiterpene Lactone Helenalin

Enhancing Ocular Surface in Dry Eye Disease Patients: A Clinical Evaluation of a Topical Formulation Containing Sesquiterpene Lactone Helenalin

Modulating Matrix Metalloproteinase-9 and Enhancing Ocular Surface Health in Dry Eye Disease Patients: A Clinical Evaluation of A Topical Formulation Containing Sesquiterpene Lactone Helenalin

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