Clinical Evaluation of CO₂Laser Vaporization Therapy for Oral Lichen Planus: A Single-Arm Intervention Study

Antitumor Effects and Tumor-specificity of Guaiazulene-3-Carboxylate Derivatives Against Oral Squamous Cell Carcinoma In Vitro

“…The mean values of CC 50 , tumor-selectivity index (TS), and potency-selectivity expression (PSE) of these twelve compounds, as well as of positive controls (5-FU, CDDP, and CBDCA) obtained from these 3 independent experiments are listed in PSE=13.0±1.9) showed the highest TS values than five alkyl guaiazulene-3-carboxylates [1][2][3][4][5], two hydroxyalkyl guaiazulene-3-carboxylates [8,9], and three aminoalkyl guaiazulene-3-carboxylates [10][11][12] (Table I). Moreover, both [6,7] showed higher TS value than CDDP and CBDCA (TS mean =2.2±1.5 and 2.4±1.1, respectively), and had PSE (mean) values comparable to that of 5-FU (13.4±6.5).…”

“…Methyl guaiazulene-3-carboxylate [1], ethyl guaiazulene-3-carboxylate [2], n-propyl guaiazulene-3-carboxylate [3], isopropyl guaiazulene-3carboxylate [4], n-butyl guaiazulene-3-carboxylate [5], 2methoxyethyl guaiazulene-3-carboxylate [6], 2-ethoxyethyl guaiazulene-3-carboxylate [7], 2-hydroxyethyl guaiazulene-3carboxylate [8], 2-(2-hydroxyethoxy)ethyl guaiazulene-3-carboxylate…”

“…[9], 2-aminoethyl guaiazulene-3-carboxylate [10], 3-aminoprpyl guaiazulene-3-carboxylate [11], 4-aminobutyl guaiazulene-3carboxylate [12] ( Figure 1G) were synthesized, according to previous reports (6,17,18). N-(2-methoxyethyl)guaiazulenecarboxamide [X] was synthesized as previously described (15).…”

“…We compared their cytotoxic activity against four human oral squamous cell carcinoma (OSCC) cell lines (Ca9-22, HSC-2, HSC-3, HSC-4) and three normal oral cells (HGF, HPLF, HPC), by comparing the 50% cytotoxic concentration (CC 50 ) determined from the dose-response curve (Table I). We have adopted 48 h treatment time, based on our observation that significant (p<0.05) cytotoxicity of compounds [6,7] appeared 3 h after treatment, reaching the plateau level after 24~48 h ( Figure 2). We have repeated the same experiments 3 times.…”

“…Among the 962 papers cited in PubMed regarding azulenes, most of them have focused on its chemistry, followed by biological activity, while few papers have focused on dentistry and oral application. Sodium azulene sulfonates have been reported to be effective for the treatment of oral mucositis (5) and oral lichen planus (6), possibly due to their antioxidant and anti-inflammatory activities (7,8). In contrast, much reduced numbers of papers of guaiazulene ( Figure 1B), a lipophilic azulene derivative, have been published, approximately half of which have dealt with its chemistry.…”