Javascript must be enabled to continue!
In Silico Evaluation of Goji Berry (Lycium barbarum) Bioactive Compounds Targeting BRAF V600E in Melanoma
View through CrossRef
Melanoma is the most aggressive form of skin cancer and is associated with high mortality, primarily due to aberrant activation of the mitogen-activated protein kinase (MAPK) pathway driven by mutations in the BRAF gene, particularly BRAF V600E. BRAF inhibitors such as vemurafenib have been used in the treatment of BRAF-mutant melanoma; however, their long-term clinical efficacy is often limited by acquired resistance and tumor adaptive mechanisms. Therefore, the exploration of natural product–based adjuvant candidates remains relevant to support melanoma therapy. This study aimed to evaluate the potential of bioactive compounds from goji berry (Lycium barbarum) as anti-melanoma candidates through an in silico approach targeting BRAF. Molecular docking was performed using the BRAF–vemurafenib complex structure (PDB ID: 3OG7), and the docking protocol was validated by redocking vemurafenib, yielding an RMSD value of 0.956 Å, which indicated the reliability of the docking procedure. Twelve bioactive compounds from Lycium barbarum were docked into the BRAF binding site, and their binding affinities, amino acid residue interactions, drug-likeness, and ADMET profiles were analyzed. The docking results showed that zeaxanthin, myricetin, quercetin, ellagic acid, galangin, kaempferol, and chlorogenic acid exhibited binding affinity values ≤ −8.0 kcal/mol, indicating favorable predicted interactions with BRAF. Among the tested compounds, quercetin showed one of the strongest binding affinities and conserved key amino acid interactions comparable to vemurafenib, whereas galangin demonstrated the most favorable drug-likeness and ADMET profile. These findings indicate two complementary prioritization criteria, in which quercetin is superior in predicted binding interaction, while galangin is superior in pharmacokinetic and drug-likeness suitability. Therefore, quercetin and galangin may serve as promising preliminary candidates for further investigation as BRAF-targeting adjuvant agents in melanoma therapy; however, experimental validation through BRAF kinase inhibition assays and melanoma cell-based studies is required to confirm their biological activity and therapeutic relevance.
Universitas Negeri Gorontalo
Title: In Silico Evaluation of Goji Berry (Lycium barbarum) Bioactive Compounds Targeting BRAF V600E in Melanoma
Description:
Melanoma is the most aggressive form of skin cancer and is associated with high mortality, primarily due to aberrant activation of the mitogen-activated protein kinase (MAPK) pathway driven by mutations in the BRAF gene, particularly BRAF V600E.
BRAF inhibitors such as vemurafenib have been used in the treatment of BRAF-mutant melanoma; however, their long-term clinical efficacy is often limited by acquired resistance and tumor adaptive mechanisms.
Therefore, the exploration of natural product–based adjuvant candidates remains relevant to support melanoma therapy.
This study aimed to evaluate the potential of bioactive compounds from goji berry (Lycium barbarum) as anti-melanoma candidates through an in silico approach targeting BRAF.
Molecular docking was performed using the BRAF–vemurafenib complex structure (PDB ID: 3OG7), and the docking protocol was validated by redocking vemurafenib, yielding an RMSD value of 0.
956 Å, which indicated the reliability of the docking procedure.
Twelve bioactive compounds from Lycium barbarum were docked into the BRAF binding site, and their binding affinities, amino acid residue interactions, drug-likeness, and ADMET profiles were analyzed.
The docking results showed that zeaxanthin, myricetin, quercetin, ellagic acid, galangin, kaempferol, and chlorogenic acid exhibited binding affinity values ≤ −8.
0 kcal/mol, indicating favorable predicted interactions with BRAF.
Among the tested compounds, quercetin showed one of the strongest binding affinities and conserved key amino acid interactions comparable to vemurafenib, whereas galangin demonstrated the most favorable drug-likeness and ADMET profile.
These findings indicate two complementary prioritization criteria, in which quercetin is superior in predicted binding interaction, while galangin is superior in pharmacokinetic and drug-likeness suitability.
Therefore, quercetin and galangin may serve as promising preliminary candidates for further investigation as BRAF-targeting adjuvant agents in melanoma therapy; however, experimental validation through BRAF kinase inhibition assays and melanoma cell-based studies is required to confirm their biological activity and therapeutic relevance.
Related Results
Chemical constituents and antioxidants of Lycium barbarum L.
Chemical constituents and antioxidants of Lycium barbarum L.
The antioxidant activity of the contents of alkaloid and hexane extracts of lycium barbarum was determined and the percentage of free radical inhibition was calculated using DPPH a...
Relationships of BRAF V600E Gene Mutation With Some Immunohistochemical Markers and Recurrence Rate in Patients With Thyroid Carcinoma
Relationships of BRAF V600E Gene Mutation With Some Immunohistochemical Markers and Recurrence Rate in Patients With Thyroid Carcinoma
Background:
The B-type rafkinase (BRAF) V600E gene mutation plays an important role in the pathogenesis, diagnosis, and prognosis of thyroid carcinoma. This stu...
The Correlation of BRAF V600E Expressions with Histopathological Variant and Lymphocyte Infiltration in Papillary Thyroid Carcinoma
The Correlation of BRAF V600E Expressions with Histopathological Variant and Lymphocyte Infiltration in Papillary Thyroid Carcinoma
BackgroundPapillary thyroid carcinoma is the most common endocrine gland malignancy that has the highest incidence rate of 60-80%. In papillarythyroid carcinoma BRAF V600E mutation...
Clinical characteristics and treatment outcomes of 65 patients with BRAF-mutated non-small cell lung cancer (NSCLC).
Clinical characteristics and treatment outcomes of 65 patients with BRAF-mutated non-small cell lung cancer (NSCLC).
e21745 Background: BRAF mutations are infrequently seen in non-small cell lung cancer (NSCLC) in Chinese population. We aimed to investigate the clinicopathologic characteristics ...
Goji Berry (Lycium Barbarum)ve Sağlık Üzerine Etkileri
Goji Berry (Lycium Barbarum)ve Sağlık Üzerine Etkileri
Goji berry (Lycium Barbarum) 2000 yıldır geleneksel Çin tıbbında kullanılan bir bitkidir. Son yıllarda bu meyve, sağlık üzerine olumlu etkilerinin araştırmalarda ortaya çıkmasıyla ...
Data from Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer
Data from Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer
<div>Abstract<p>One of the most encouraging developments in oncology has been the success of BRAF inhibitors in <i>BRAF</i>-mutant melanoma. However, in con...
Data from Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer
Data from Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer
<div>Abstract<p>One of the most encouraging developments in oncology has been the success of BRAF inhibitors in <i>BRAF</i>-mutant melanoma. However, in con...
Effect of significant incidence of Braf p.V600E mutations in esophageal cancer on potential use of tyrosine kinase inhibitors.
Effect of significant incidence of Braf p.V600E mutations in esophageal cancer on potential use of tyrosine kinase inhibitors.
e16591 Background: Routine diagnosis of esophageal cancer varies from locally advanced to metastatic at presentation. Most of these patients are cachectic at presentation and phys...

