Synthesis and in vitro assay of hydroxyxanthones as antioxidant and anticancer agents.

In the present work, three hydroxyxanthones were synthesized in 11.15-33.42% yield from 2,6-dihydroxybenzoic acid as the starting material. The chemical structures of prepared hydroxyxanthones have been elucidated by using spectroscopic techniques. Afterward, the hydroxyxanthones were evaluated as antioxidant agents through radical scavenging assay; and anticancer agents through in vitro assays against WiDr, MCF-7, and HeLa cancer cell lines. Hydroxyxanthone 3b was categorized as a strong antioxidant agent (IC50 = 349 ± 68 µM), while the other compounds were categorized as moderate antioxidant agents (IC50 > 500 µM). On the other hand, hydroxyxanthone 3a exhibited the highest anticancer activity (IC50 = 184 ± 15 µM) and the highest selectivity (SI = 18.42) against MCF-7 cancer cells. From the molecular docking study, it was found that hydroxyxanthone 3a interacted with the active sites of Topoisomerase II protein through Hydrogen bonding with DG13 and π-π stacking interactions with DA12 and DC8. These findings revealed that hydroxyxanthones are potential candidates to be developed as antioxidant and anticancer agents in the future.

An Update on the Anticancer Activity of Xanthone Derivatives: A Review.

The annual number of cancer deaths continues increasing every day; thus, it is urgent to search for and find active, selective, and efficient anticancer drugs as soon as possible. Among the available anticancer drugs, almost all of them contain heterocyclic moiety in their chemical structure. Xanthone is a heterocyclic compound with a dibenzo-γ-pyrone framework and well-known to have "privileged structures" for anticancer activities against several cancer cell lines. The wide anticancer activity of xanthones is produced by caspase activation, RNA binding, DNA cross-linking, as well as P-gp, kinase, aromatase, and topoisomerase inhibition. This anticancer activity depends on the type, number, and position of the attached functional groups in the xanthone skeleton. This review discusses the recent advances in the anticancer activity of xanthone derivatives, both from natural products isolation and synthesis methods, as the anticancer agent through in vitro, in vivo, and clinical assays.

3,4-dimethoxychalcone novel ultraviolet-A-protection factor in conventional sunscreen cream.

UltravioletA (UVA) rays with an intensity of 95% can induce skin cancer due to the activation of reactive oxygen species (ROS). The 3,4-dimethoxychalcone (3,4-DMC) chalcone derivative has a wide wavelength, antioxidant activity, presumed has activity as sunscreen (UVA rays). Topical delivery of water-insoluble 3,4-DMC with log P 3.84 required capable, cream formulation was chosen because it was suitable for application this chemical sunscreen. This study aims to obtain the optimal formulation of 3,4-DMC in a sunscreen cream dosage form as a UVA-protection factor (UVA-PF). This study involves experimental design. The cream 3,4-DMC was evaluated physically for 4 weeks by measuring pH, viscosity, spreadability, adhesion, centrifugation, freeze-thaw, photostability, UVA-PF used TranporeTM tape, and skin irritation test on animals. The result obtained was evaluated statistically using ANOVA (SPSS version 24). The ratio UVA/UVB value of 3,4 DMC sunscreen cream having 5 stars (*****) for all concentrations, shows the product in this study can be used as an anti-UVA agent in sunscreen cream cosmetic products. The stability of the cream has pH 4.0-4.2; spreadability 5-6 cm; viscosity 4.470-5.763; and adhesion <1 s. Freeze-thaw and centrifugation were known did not affect the stability due to the absence of separation. There was no wavelength shift in the photostability test and no skin irritation due to in vivo examination using New Zealand rabbits. The 3,4-DMC as a new agent in conventional sunscreen cream dosage form has good properties as a protection against UVA rays.

The effect of variation of tetrahydropentagamavunon-0 concentration in lotion and emulgel formula toward acute dermal irritation study.

Tetrahydropentagamavunon-0 (THPGV-0) is a curcumin metabolite analog which known has a higher antioxidant activity than Vitamin E. This compound has been formulated in lotion as antiaging cosmetics, but the irritation effect is unknown yet. This study aims to analyze the effect of variation of THPGV-0 concentration in lotion and emulgel formula toward acute dermal irritation. The concentrations of THPGV-0 varied to 0.1%, 0.2%, and 0.4% in lotion/emulgel and tested for their physical properties such as organoleptic, homogeneity, pH, spreadability, and adhesion. Acute dermal irritation test is done in accordance with the In vivo Nonclinical Toxicity Test Guidelines by the Indonesian Food and Drug Administration (BPOM). This study showed that Primary Irritation Index (PII) value concentrations of 0.1%, 0.2%, and 0.4% THPGV-0 in lotion formula are 0.014, 0.014, and 0.028 (close to 0) and in emulgel formula are 0.08 at concentration of 0.1%, 0.33 at concentration of 0.2%, and 0.25 at concentration of 0.4%. PII of 0.1%, 0.2%, and 0.4% THPGV-0 in lotion and emulgel is included in negligible irritation response. Hence, the both of THPGV-0 formula in lotion and emulgel are considered safe to use on skin according to this study.