α-mangostin (Amg), a compound isolated from the mangosteen rind (Garcinia mangostana, L.), has demonstrated promising anticancer activity. However, its low solubility and selectivity against cancer cells limit its efficacy. To address this issue, researchers have developed chitosan/alginate polymeric nanoparticles (NANO-AMCAL) to enhance the effectiveness of Amg. In vitro studies have demonstrated that NANO-AMCAL is highly active against breast cancer cells. Therefore, an in vivo study was conducted to evaluate the efficacy of NANO-AMCAL in treating breast cancer in Wistar rats (Rattus norvegicus) and determine the effective dose. The rats were divided into seven treatment groups, including positive control, negative control, pure Amg, and NANO-AMCAL 5 mg, 10 mg, and 20 mg. The rats were injected subcutaneously with a carcinogenic agent, 7,12-dimethylbenz(a)anthracene (DMBA) and were evaluated for weight and tumor volume every three days during treatment. Surgery was performed on day 14, and histopathological studies were carried out on breast and lung cancer tissues. The results showed that NANO-AMCAL significantly enhanced the anticancer activity of Amg in treating breast cancer in Wistar rats. NANO-AMCAL containing 0.33 mg of Amg had a healing effect three times better than 20 mg pure Amg and was comparable to tamoxifen. The effective dose of NANO-AMCAL for anti-breast cancer treatment in Wistar rats was found to be 20 mg, which exhibited a good healing response, and the tumor volume continued to decrease up to 17.43% on the 14th day. Furthermore, histopathological tests showed tissue repair and no metastases. These findings suggest that NANO-AMCAL may be a promising therapeutic option for breast cancer treatment.
Background: Recurrent Aphthous Stomatitis (RAS) is a common ulcerative disease of the oral mucosa which is characterized by pain, and recurrent lesions in the oral cavity. This condition is quite painful, causing difficulty in eating, speaking and swallowing. Topical medications have been used for this condition, but the obstacle in using topical medications is the difficulty of achieving drug effects due to saliva wash out. This problem can be overcome by film hydrogel formulation which can protect the ulcer and reduce the pain to some extent. α-mangostin is a xanthone isolated from the rind of the mangosteen fruit. One of the activities of α-mangostin is anti-inflammatory effects, which operate through the characteristic mechanism of inhibiting the inflammatory response. This protocol study aims to investigate the efficacy of an α-mangostin hydrogel film with a chitosan alginate base for recurrent aphthous stomatitis (RAS) in comparison with a placebo over a period of 7 days. Study design: This is a two-arm, double blinding, randomized controlled trial enrolling patients with RAS. The efficacy test of α-mangostin Hydrogel Film will be tested against the placebo. Patients with RAS will be allocated randomly into the two arms and the hydrogel film will be administered for 7 days. The diameter of ulcer and visual analog scale (VAS) score will be used as the primary efficacy endpoint. The outcome measure will be compared between the two arms at the baseline, day 3, day 5, and at the end of 7 days. Discussion: The purpose of this clinical research is to provide scientific evidence on the efficacy of α-mangostin hydrogel film with a chitosan alginate basis in treating recurrent aphthous stomatitis. The trial is expected to improve our capacity to scientifically confirm the anti-inflammatory effectiveness of α-mangostin compounds in a final formulation that is ready to use. Trial registration: NCT06039774 (14 September 2023).
α-Mangostin, initially identified in 1855, is a xanthone derivative compound predominantly located in the pericarp of the mangosteen fruit (Garcinia mangostana L). This compound is known for its beneficial properties as an antioxidant and anti-inflammatory agent, still holding promise for potential benefits in other related pathologies. In the investigative process, computational studies have proven highly valuable in providing evidence and initial screening before progressing to preclinical and clinical studies. This review aims to present the pharmacological findings and mechanisms of action of α-mangostin based on computational studies. The compilation of this review is founded on the analysis of relevant articles obtained from PubMed, Scopus, and ScienceDirect databases. The study commences with an elucidation of the physicochemical characteristics, drug-likeness, pharmacokinetics, and toxicity profile of α-mangostin, which demonstrates that α-mangostin complies with the Lipinski's Rule of Five, exhibits favorable profiles of absorption, distribution, metabolism, and excretion, and presents low toxicity. Subsequent investigations have revealed that computational studies employing various software tools including ArgusLab, AutoDock, AutoDock Vina, Glide, HEX, and MOE, have been pivotal to comprehend the pharmacology of α-mangostin. Beyond its well established roles as an antioxidant and anti-inflammatory agent, α-mangostin is now recognized for its pharmacological effects in Alzheimer's disease, diabetes, cancer, chronic kidney disease, chronic periodontitis, infectious diseases, and rheumatoid arthritis. Moreover, α-mangostin is projected to have applications in pain management and as a potent mosquito larvicide. All of these findings are based on the attainment of adequate binding affinity to specific target receptors associated with each respective pathological condition. Consequently, it is anticipated that these findings will serve as a foundation for future scientific endeavours, encompassing both in vitro and in vivo studies, as well as clinical investigations, to better understand the pharmacological effects of α-mangostin.