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Salicylic acid (SA) is widely renowned for its efficacy as a beneficial ingredient for skincare, especially for acne and uneven skin texture. The salicylic acid (SA) niosome formulation combined with the essential component of oleoresin from Dipterocarpus alatus Roxb. ex G. Don or Yang‐Na (ODA) was developed and investigated for its physical characteristics, biological effects, and stability. The findings demonstrated that SA combined with ODA in the niosome formulation F4 enhanced the entrapment efficiency of SA, as well as the physical properties and stability of the formulation. Furthermore, the release pattern of this combined formulation indicated sustained release of SA. The permeation of SA was higher in the presence of ODA compared to SA‐niosome formulations without ODA. Moreover, this F4 could downregulate the secretion of iNOS, COX‐2, and TNF‐α including anti‐Propionibacterium acnes activities. Consequently, the incorporation of ODA into the niosome formulation has the potential to improve the entrapment efficiency of SA, facilitating controlled release and enhancing permeation, nitric oxide inhibition capabilities, and anti-P. acnes activity. Therefore, F4 has the potential to be developed as a topical product for the combined treatment of inflammation and P. acnes‐associated conditions in the future. [ABSTRACT FROM AUTHOR]

Skin abrasion wounds, especially those infected with methicillin-resistant Staphylococcus aureus (MRSA), pose a risk of developing into severe lesions. MRSA is resistant to typical antibiotics, which necessitate intravenous antibiotic and/or surgical interventions. A Yang-Na (Dipterocarpus alatus Roxb. Ex G. Don) twig extract has been shown to exhibit antibacterial and wound healing properties in mice with MRSA-infected wounds. This study aimed to examine the efficacy of an ointment containing Yang-Na twig extract against MRSA-infected abrasion wounds in mice. Skin abrasion wounds induced on mice were infected with MRSA (n=10) and left untreated or treated daily with an ointment base, tetracycline ointment (160 μg/g), or Yang-Na twig ointments (20 and 40 mg/g) for 9 days, alongside a non-infected control group. MRSA infection significantly compromised skin integrity, as evidenced by weakened skin barrier strength and enhanced transepidermal water loss. The infected wounds showed signs of deterioration and substantial numbers of MRSA colonies, along with mast cell infiltration and increased mRNA expression of inflammatory-related genes (TLR-2, NF-κB, TNF-α, IL-1β, IL-6, and IL-10). Treatment with Yang-Na twig ointments restored skin integrity and improved wound appearance within a week. Mast cell infiltration and expression of inflammatory-related genes were normalized and no MRSA colonies were observed in the wounds treated with Yang-Na twig ointments. The other treatments did not achieve the same results. These findings highlight the therapeutic effects of the Yang-Na twig ointment as an antibacterial and wound healing remedy with anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

According to our preliminary study, melatonin and its N-amide derivatives (N-(2-(1-4-bromobenzoyl-5-methoxy-1H-indol-3-yl)ethyl)acetamide (BBM) and 4-bromo-N-(2-(5-methoxy-1H-indol-3-yl)ethyl)benzamide (EBM)) inhibited the marker of acute inflammation in tests in vitro and in vivo. The anti-inflammatory agent is intended for the prevention and treatment of chemotherapy-induced toxicity. In this study aimed to evaluate the effect of melatonin and its derivatives on mechanisms related to chemotherapy-induced oral mucositis by in vitro ROS and 5-FU-induced human keratinocyte cells as well as in vivo oral mucositis model. In in vitro H2O2-induced HaCaT cells, BBM had the highest level of protection (34.57%) at a concentration 50 µM, followed by EBM (26.41%), and melatonin (7.9%). BBM also protected cells against 5-FU-induced to 37.69–27.25% at 12.5–100 µM while EBM was 36.93–29.33% and melatonin was 22.5–11.39%. In in vivo 5-FU-induced oral mucositis in mice, melatonin, BBM, and EBM gel formulations protected tissue damage from 5-FU similar to the standard compound, benzydamine. Moreover, the weight of mice and food consumption recovered more quickly in the BBM group. These findings suggested that it was possible to develop BBM and EBM as new therapeutic agents for the treatment of oral mucositis. [ABSTRACT FROM AUTHOR]

The leaves, bark, and twigs of Dipterocarpus alatus have been used to treat many diseases because they contain large amounts of bioactive compounds that can protect against free radical damage. The extraction process is a key step in the utilization of bioactive compounds from plants. Therefore, the aim of this study was to determine the phytochemical compounds, antioxidant capacity and acetylcholinesterase (AChE) inhibitory activity of extracts of D. alatus leaves, bark and twig prepared using three extraction solvents with different polarities; methanol (MeOH), ethanol (EtOH) and isopropyl alcohol (IPA). The results revealed that the bark and twig extracts had a strong antioxidant activity, while the leaves had a potential AChE inhibitory activity. The strong antioxidant activity found in MeOH and EtOH extracts was related to their phenolic acid contents. A class of triterpenoid compounds, dipterocarpol and betulonic acid, which were abundant in the IPA extract, and their presence correlated with AChE inhibitory activity. Solvent polarity was therefore a critical extraction parameter affecting phytochemical content and biological activity. [ABSTRACT FROM AUTHOR]

Background: Alzheimer's disease (AD) pathogenesis is associated with amyloid-β (Aβ)-induced neuroinflammation. In AD, the activation of microglia caused by Aβ accumulation is followed by the synthesis and release of pro-inflammatory cytokines, including interleukin-1β (IL-1β) and tumor necrosis factor-α (TNFα), and ultimately leads to cognitive impairments. Clausena harmandiana (CH) is a medicinal plant in the Rutaceae family and has been used in folk medicine to relieve illnesses such as stomachache and headache, and as a health tonic. Interestingly, CH root extract (CHRE) has several anti-inflammatory and other pharmacological activities, but there are no studies in AD-like animal models. Objectives: This study aims to evaluate the effects of CHRE on cognitive impairments, increased Aβ1–42 protein levels, and neuroinflammation in Aβ1–42-induced rats. Methods: Forty-eight adult male Sprague-Dawley rats (250–300 g) were randomly divided into 6 groups (n = 8) of the sham control, V + Aβ, CB + Aβ CHRE125 + Aβ, CHRE250 + Aβ, and CHRE500 + Aβ. Sodium carboxymethylcellulose, Celebrex (10 mg/kg BW) and CHRE (125, 250, and 500 mg/kg BW) were given orally or without any treatment for 35 days. On day 21, aggregated Aβ1–42 at a concentration of 1 μg/μl were injected into both lateral ventricles (1 μl/side) of all treated rats, while sterilized normal saline were injected to untreated rats. Ten days later, the novel object recognition test was performed to assess their recognition memory. At the end of the test period, an overdose of thiopental sodium (120 mg/kg BW) and transcardial perfusion with 0.9% normal saline solution were used to euthanize all rats. Then Aβ1–42 protein levels and the expression of inflammatory markers (CD11b-positive microglia, IL-1β, and TNFα) were investigated in the cerebral cortex and hippocampus. Results: Pretreatment with CHRE at all doses could attenuate short- and long-term impairments in recognition memory. Additionally, CHRE also inhibited the increase of Aβ1–42 protein levels and the expression of inflammatory markers in both brain regions as well as receiving Celebrex. Conclusions: This suggests that preventive treatment of CHRE might be a potential therapy against cognitive impairments via reducing Aβ1–42 protein levels and neuroinflammation caused by Aβ1–42. [ABSTRACT FROM AUTHOR]

Coumarins and carbazole alkaloids are natural compounds, often with neurological properties, especially as acetylcholinesterase inhibitors. In order to screen the candidate anti-acetylcholinesterase agents, in-silico molecular docking was performed aiming to predict the binding mechanism and the results were used to identify pharmacophores of coumarins and carbazole alkaloids from Clausena harmandiana as AChE inhibitory activity. All isolated compounds are xanthoxyletin (1), dentatin (2), nordentatin (3), clausarin (4), 7-methoxymukonal (5), 7-methoxyheptaphylline (6) and heptaphylline (7) displayed the stable binding interactions with Torpedo californica acetylcholinesterase (TcAChE) enzyme via π-π interactions, hydrogen bonds and hydrophobic interactions. All compounds exhibited the interaction with the peripheral anionic site of TcAChE same manner of standard anti-alzheimer drugs. ADME prediction revealed that all compounds met the requirement of drug likeness of Lipinski's rule of five and had high CNS absorption, excepted 4 should be structure modification to improve CNS penetration. Besides 4, 6 and 7 displayed the highest acetylcholinesterase inhibitor activity among the other compounds. Interestingly, 6 had a high yield (58.01 mg/g extract) from C. harmandiana. It should be a candidate as an anti-acetylcholinesterase inhibitor agent. [ABSTRACT FROM AUTHOR]