Anake Kijjoa

Ultraviolet (UV)-induced oxidative stress is a major cause of skin photoaging, prompting interest in multifunctional antioxidants of marine origin for topical photoprotection. Astaxanthin, a xanthophyll carotenoid predominantly obtained from the microalga Haematococcus pluvialis, exhibits antioxidant, anti-inflammatory, and matrix-metalloproteinase (MMP)-modulating activities relevant to skin protection. This study aimed to formulate and systematically characterize oil-in-water (O/W) sunscreen emulsions containing 1%, 2.5%, and 5% (w/w) natural astaxanthin-containing extract (AstaReal^® P4AF), in combination with an inorganic titanium dioxide (TiO₂) UV filter, and to evaluate the influence of astaxanthin concentration on formulation performance and biological tolerability. Formulations were characterized in terms of viscosity, antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, mechanical and adhesive performance using back-extrusion and adhesion tests, in vitro sun protection factor (SPF), UVA protection, water resistance (WR), and local tissue tolerability using the in ovo chorioallantoic membrane (CAM) model. Viscosity increased with AstaReal^® P4AF concentration at both temperatures (from 3801.9 to 5704.6 mPa·s at 25 °C, and from 1931.8 to 5118.9 mPa s at 36 °C), with the 5% AstaReal^® P4AF formulation showing the greatest thermal stability. DPPH radical scavenging activity increased markedly with AstaReal^® P4AF concentration up to 2.5% (33.15% at 1% and 63.04% at 2.5%) and remained comparable at 5% (62.62%), versus 22.05% for the placebo formulation. Back-extrusion analysis revealed a non-linear, concentration-dependent effect on consistency and firmness, peaking at 2.5% AstaReal^® P4AF, while adhesion parameters remained statistically unaffected across concentrations. SPF and UVA protection factor decreased with increasing AstaReal^® P4AF concentration (74.37 to 35.02 and 37.62 to 19.78, respectively), whereas WR was improved at the highest concentration. CAM histopathological scoring indicated that AstaReal^® P4AF incorporation did not increase tissue injury relative to the formulation base. These findings indicate that AstaReal^® P4AF concentration critically influences the physicochemical and photoprotective balance of sunscreen emulsions, supporting further optimization toward a multifunctional, marine-derived ingredient.

Background/Objectives: Delayed onset muscle soreness (DOMS) is a common and recurrent symptom in athletes following intensive or eccentric exercise. This study evaluated the efficacy of a topical gel of Derris scandens stem extract on pain and countermovement jump (CMJ) performance in athletes with exercise-induced DOMS and assessed skin irritation in healthy volunteers. Methods: Genistein-7-O-[α-rhamnosyl-(1→6)-β-glucopyranoside] (GG), a chemical marker of D. scandens, was quantified by HPLC. In a randomized, double-blind, active-controlled trial, athletes applied D. scandens gel (5%) or diclofenac gel (1%) to the painful site twice daily for 7 days. Pain was recorded daily using a visual analog scale, and CMJ was evaluated on days 1, 2, 4, and 8. Changes from the pre-treatment assessment were compared between groups. Results:D. scandens gel caused no skin irritation in healthy volunteers. Twenty-five athletes completed the trial (D. scandens, n = 13; diclofenac, n = 12). Pain scores decreased and CMJ recovered over the treatment period in both groups, with a significant effect of time but no significant treatment-by-time interaction or treatment effect. Pain reduction from day 2 to day 8 did not differ between groups (MD, 1.75; 95% CI, −1.01 to 4.51; p = 0.203), nor did CMJ recovery (MD, 1.96 cm; 95% CI, −2.01 to 5.93; p = 0.315). No adverse events were reported. Conclusions: Topical D. scandens gel was well tolerated, and both treatment groups showed reductions in DOMS-related pain and recovery of CMJ performance over the treatment period. Between-group differences were not statistically significant. Trial registration: Thai Clinical Trials Registry TCTR20180608003.

Nelumbo nucifera Gaertn. is a rich source of bioactive compounds, and has been extensively investigated for its antioxidant and anti-inflammatory properties. However, despite its broad pharmacological potential, detailed molecular-level insights into the interactions of its phenolic and flavonoid constituents with key skin-aging-related enzymes remain limited. Therefore, this study employed an integrated in silico and in vitro approach to systematically evaluate the anti-aging potential of phenolic and flavonoid compounds derived from N. nucifera. Molecular docking was performed to investigate their binding interactions with tyrosinase, elastase, and collagenase. Compounds exhibiting the most promising inhibitory profiles were further subjected to molecular dynamics (MD) simulations for 100 ns and density functional theory (DFT) analyses at the B3LYP/6-31G(d,p) level of theory to elucidate their structural stability and electronic properties. The computational results revealed favorable binding affinities, stable complex formation, and electrostatic features supporting hydrogen bond interactions. In vitro enzyme inhibition assays demonstrated that hesperidin exhibited inhibitory activity against tyrosinase, collagenase, and elastase, with IC₅₀ values of 3.43 mM, 2.26 mM, and 0.55 mM, respectively. Kojic acid was used as a positive control for tyrosinase, while epigallocatechin gallate (EGCG) was used as a positive control for both collagenase and elastase. Additionally, hesperidin exhibited enzyme-inhibitory activity and preliminary intrinsic UV absorption. This compound warrants further investigation, specifically regarding its stability and performance within standardized cosmeceutical formulations.

Gyrinops vidalii (Thymelaeaceae), a critically endangered agarwood-producing species native to Thailand and Laos and remains phytochemically unexplored. In this study, the chemical constituents and biological activities of the ethyl acetate (EtOAc) fraction of methanol extract of G. vidalii leaves were investigated. Phytochemical analysis led the isolation of mangiferin (1), iriflophenone 3-C-β-D-glucoside (2), aquilarinenside E (3), iriflophenone 2-O-α-L-rhamnoside (4), 5,7,4′-trimethoxyflavone (5), blumenol A (6), loliolide (7), 4-hydroxybenzoic acid methyl ester (8), and 4-hydroxybenzoic acid (9). Compound 1 exhibited potent DPPH radical scavenging activity with an SC₅₀ value of 19.35 μM), whereas iriflophenone (3a), obtained by acid hydrolysis of 3, and 5 showed promising α-glucosidase inhibitory activity with IC₅₀ values 100.06 and 174.57 μM, respectively. Molecular docking demonstrated favorable binding of both compounds within the α-glucosidase active site through hydrogen bonding, aromatic, and hydrophobic interactions, with binding energies of −7.4 and −8.0 kcal/mol, respectively. Predicted ADMET properties further supported the drug-like potential of both compounds, indicating favorable aqueous solubility, high intestinal absorption, and no predicted hepatotoxicity, while differences were observed in their predicted blood–brain barrier permeability. This study represents the first phytochemical investigation of G. vidalii, provides scientific support for its traditional use, and expands the chemotaxonomic knowledge of the closely related genera Gyrinops and Aquilaria.

An unreported bicyclic sesquiterpene acid, verruculosic acid (1), was isolated together with the previously reported labdane diterpenes, (+)-agathic acid (2a) and hypoxyterpenoid A (2b), one 3-nor-2,3-seco-labdane, penioxalicin (3), and 5-carboxyphthalide (4), from a sea grass-associated fungus, Penicillium verruculosum KUFA1509. The structures of the isolated compounds were elucidated by detailed analyses of 1D and 2D NMR and HRMS data. The absolute configurations of the stereogenic carbons in 1 and 2a were established by X-ray crystallography. The crystal structure of 2a, which was obtained for the first time, was used to prove its structure and confirm its stereochemistry. The crystal structure of 3 was also obtained; however, the value of its flack parameter does not allow us to determine the absolute configuration. Compound 2b exhibited stronger inhibitory activity than the positive control, diclofenac sodium, against LPS-induced nitric oxide (NO) production in RAW264.7 macrophages, while 1 and 2a were slightly less active than the positive control. In contrast, 3 exhibited much weaker activity than 2a. Compounds 1–4 were also assayed for antibacterial activity against reference and multidrug-resistant strains, but none exhibited antibacterial activity against the tested strains. Thus, the labdane skeleton could be considered as a potential scaffold for the development of anti-inflammatory agents through NO inhibition.

Benjalokawichian (BLW) is a classic antipyretic polyherbal remedy used in Thai traditional medicine (TTM) to reduce toxic fever (TF). This study aimed to shed light on the mechanisms of action and identify bioactive components of BLW responsible for TF treatment. The methods that combine network pharmacology, molecular docking, and the inhibition of nitric oxide (NO) production in LPS-induced RAW 264.7 were employed for these objectives. Network pharmacology served as a means to identify 15 potential bioactive compounds, 88 possible therapeutic targets, and 4 hub genes related to BLW. Among the significant targets, TNF, PTGS2, STAT3, and NFKB1 were closely linked to the metabolic pathways of phenylalanine, arachidonic acid, and tyrosine, which are vital in managing infections, inflammation, proliferation, and apoptosis in the TF microenvironment. Additionally, molecular docking analysis indicated that core compounds displayed strong binding affinities for the key targets, with binding energies ranging between −4.5 and −11.1 kcal/mol. The in vitro assay demonstrated that BLW extract significantly inhibited NO production in LPS-activated RAW 264.7 macrophages, presenting an IC₅₀ value of 69.10 μg/mL, and no cytotoxic effects on RAW 264.7 macrophages. Furthermore, the biomarker compounds of BLW extract, viz., perforatic acid and peucenin-7-methyl ether were found to decrease NO production in a dose-dependent manner. In summary, this research indicates that BLW provides therapeutic benefits for TF via a complex interplay of different compounds, targets, and pathways. These findings serve as a foundation for further research into the mechanisms of action of a polyherbal remedy toward TF to provide scientific evidences for its clinical use.

Benjalokawichian (BLW) or Ha-Rak is a classic antipyretic polyherbal remedy used in Thai traditional medicine (TTM) to reduce toxic fever (TF). This study aimed to shed light to the mechanisms of action and identify bioactive components of BLW responsible for TF treatment. The approaches that integrate network pharmacology, molecular docking, and inhibition of nitric oxide (NO) production in LPS-induced RAW264.7 were used for these purposes. Network pharmacology was used as a tool to identify 17 potential bioactive compounds, 88 potential therapeutic targets, and 4 hub genes for BLW. Among the key targets, TNF, PTGS2, STAT3, and NFKB1 were closely associated with the phenylalanine, arachidonic acid and tyrosine metabolic pathways, which play critical roles in infections, inflammation, proliferation and apoptosis in the TF microenvironment. On the other hand, molecular docking analysis suggested that core compounds exhibited strong binding affinities for key targets, with binding energies ranging from -4.5 to -11.1 kJ/mol. In vitro assay showed that BLW extract exhibited strong inhibition of NO production in LPS-induced RAW264.7 macrophages, with an IC50 value of 69.10 μg/mL, and no cytotoxicity against RAW264.7 macrophages was observed. Furthermore, the biomarker compounds of BLW extract, viz. perforatic acid and peucenin-7-methyl ether were found to decrease NO production in a dose-dependent manner. Overall, this study demonstrates that BLW exerts its therapeutic effects on TF through a complex network of various compounds, targets, and pathways. These findings serve as a foundation for further research into the mechanisms of action of a polyherbal remedy toward TF to provide scientific evidences for its clinical use.

Depression adversely impacts daily life, with age‐related neurodegeneration being a significant contributing factor. Neurodegenerative alterations, often accelerated by oxidative stress, underlie depressive progression in advanced age. Our previous research has reported that Alternanthera philoxeroides (Mart.) Griseb (AP) exhibits promising antioxidant properties for counteracting age‐related dementia. However, other mechanisms, such as those related to aging‐induced depression, have not been investigated. The present study investigated the therapeutic potential of AP against D‐galactose (D‐gal)‐induced geriatric depression in male mice, with a specific emphasis on its antioxidative properties and neurogenesis‐mediated mechanisms of action. AP extract showed radical scavenging activity by transferring hydrogen atoms and single electrons. Moreover, AP treatment significantly restored the endogenous defensive system and neuronal regeneration, prevented lipid peroxidation in mood‐regulating brain regions, and reduced serum corticosterone levels, alleviating depressive‐like behaviors. Nuclear magnetic resonance (NMR)–based metabolomic pathway analysis revealed that neurotransmitter synthesis, energy production, and protein synthesis were the pathways modulated by AP. Thus, AP extract demonstrated neuroprotective and antidepressive effects in aging‐induced depression, offering a promising source for the treatment of depression in elderly patients. Further research is required to establish its role in treating aging‐related neurodegenerative diseases.

The resin extract of Garcinia nigrolineata (GNR-E), a tropical plant used in Southeast Asian traditional medicine, was evaluated for its antidepressant-like effects in a chronic mild stress (CMS) mouse model, with imipramine as a reference drug. GNR-E dose-dependently alleviated CMS-induced anhedonia (sucrose preference test) and behavioral despair (forced swimming and tail suspension tests). Neurochemical analyses revealed that GNR-E increased serotonin (5-HT) and norepinephrine (NE) levels, reduced expression of their transporters (SERT, NET) and receptors (5-HT1A, 1B, 2A, 2C, 7; α2A, 2C) in the frontal cortex and hippocampus, and normalized HPA-axis hyperactivity by lowering serum corticosterone and modulating glucocorticoid receptor (GR) and SGK-1 mRNA expression. In vitro, GNR-E inhibited monoamine oxidase (MAO)-A and -B (Ki = 2.33 and 1.55 µg/mL, respectively). Phytochemical analysis identified xanthones, particularly cowanin, as key constituents. These findings highlight GNR-E’s potential as a novel plant-based antidepressant, warranting further investigation into its active compounds and clinical applications.