Diabetes mellitus is a group of metabolic disorders characterized by hyperglycemia caused by resistance to insulin action, inadequate insulin secretion, or excessive glucagon production. Numerous studies have linked diabetes mellitus and oxidative stress. People with diabetes usually exhibit high oxidative stress due to persistent and chronic hyperglycemia, which impairs the activity of the antioxidant defense system and promotes the formation of free radicals. Recently, several studies have focused on exploring natural antioxidants to improve diabetes mellitus. Fibraurea tinctoria has long been known as the native Borneo used in traditional medicine to treat diabetes. Taxonomically, this plant is part of the Menispermaceae family, widely known for producing various alkaloids. Among them are protoberberine alkaloids such as berberine. Berberine is an isoquinoline alkaloid with many pharmacological activities. Berberine is receiving considerable interest because of its antidiabetic and antioxidant activities, which are based on many biochemical pathways. Therefore, this review explores the pharmacological effects of Fibraurea tinctoria and its active constituent, berberine, against oxidative stress and diabetes, emphasizing its mechanistic aspects. This review also summarizes the pharmacokinetics and toxicity of berberine and in silico studies of berberine in several diseases and its protein targets.
1 August 2024 in Drug Design, Development and Therapy
Purpose: This study aimed to isolate and characterize palmatine from Fibraurea tinctoria Lour stems, quantify its content, and determine its antioxidant and antidiabetic activities. Patients and Methods: Palmatine was isolated from the methanol extract of Fibraurea tinctoria Lour stems by silica gel column chromatography. Structural elucidation of the isolated compounds was performed using spectral data analysis and comparison with the literature. High-Performance Liquid Chromatography (HPLC) was used to quantitatively determine palmatine in the crude methanol extract and fractions. The DPPH and non-enzymatic SOD mimic methods were used to assess the antioxidant activity of the methanol extract, fractions, and isolated compounds. The antidiabetic activity was evaluated in silico by the molecular docking method of alpha-glucosidase and DPP-IV enzymes. Palmatine was used as a test ligand and was compared with berberine and its native ligand or standard compounds. Results: The isolated compound was identified as palmatine. Quantification of palmatine compound by HPLC showed that palmatine was found in the extract and all fractions. In the in vitro antioxidant activity test using the DPPH method, fraction 4 showed the highest activity, with an IC50 value of 91 ppm. In contrast, using the non-enzymatic SOD mimic method, the methanol extract, fraction 5, and isolated compound (palmatine) exhibited very strong antioxidant activity, with IC50 values of 18, 20, and 28 ppm, respectively. The in silico antidiabetic activity of palmatine is thought to have the potential to inhibit these two enzymes. Conclusion: These results showed that Fibraurea tinctoria Lour stems have potential as an antioxidant and antidiabetic agent. Further research on phytochemical and pharmacological is required to validate the use of this plant species for the treatment of various diseases, especially diabetes mellitus.
Fibraurea tinctoria Lour has long been used by the indigenous ethnic groups of Kalimantan in the traditional treatment of malaria, jaundice, and diabetes mellitus. This study aimed to evaluate the drug‐likeness and ADMET properties of the active compounds berberine, palmatine, and jatrorrhizine and to assess the acute toxicity of the plant extract using in silico and in vivo approaches. In silico analysis was performed using the pkCSM, ProTox‐II, and SwissADME online web servers to predict drug‐likeness and ADMET of compounds from Fibraurea tinctoria Lour. The in vivo acute toxicity of the extract was evaluated according to the Organization for Economic Cooperation and Development (OECD) 425 guideline. In silico studies have demonstrated that berberine, palmatine, and jatrorrhizine exhibit favorable drug‐likeness and pharmacokinetic properties but indicate potential oral toxicity. In contrast, the in vivo acute toxicity study revealed no toxicity or adverse effects, with an LD 50 greater than 5000 mg/kg. These findings indicate that despite the in silico prediction showing the potential toxicity of these three compounds, the extract exhibited relative safety based on in vivo tests and has the potential for further pharmacological development.
Oxidative stress has long been associated with increased risk for several diseases. Antioxidant is a molecule that inhibits the oxidation of other molecules and delays or prevents oxidative damage. Natural phenolic and flavonoid compounds are plant secondary metabolites directly contributing to antioxidant activity. Fibraurea tinctoria Lour, often called the yellow root, is a plant that has long been known in the traditional medicine of the native tribes of West Kalimantan to treat several diseases, including malaria, jaundice, and diabetes. This study aimed to quantify the total phenolic (TPC) and flavonoid (TFC) contents and antioxidant activity of the ethanol extract of yellow root stems. Yellow root stems were extracted by maceration in 96% ethanol for four days. The total phenolic, flavonoid, and antioxidant activities were measured using the Folin-Ciocalteu, AlCl3, and DPPH methods. Phytochemical screening showed that the ethanol extract of yellow root stems contains phenolics, flavonoids, alkaloids, saponins, tannins, and steroids/triterpenoids. The total phenol and flavonoid contents were 40.2 mg GAE/g extract and 61.2 mg QE/g extract, respectively. The ethanol extract of yellow root stems showed moderate DPPH scavenging activity, with an IC50 of 152.13 ppm. From this study, it can be concluded that this plant could be a potential source of natural antioxidants.
16 January 2023 in Poltekita: Jurnal Pengabdian Masyarakat
Riskesdas data in 2018 showed that the number of tooth decays in West Kalimantan province was 49.55% and that in Pontianak City was 39.52%. The results of a preliminary survey conducted on 5th-grade students of SDN 09 Pontianak found an average of three deciduous teeth and four adult teeth affected by dental caries. One way to prevent dental caries is to brush the teeth using toothpaste that contain active antibacterial ingredients. One herb widely used as an active ingredient in toothpaste is siwak. This community service activity aims to increase knowledge and skills in making herbal toothpaste to reduce the dental plaque index. This activity uses health counseling methods through lectures, leaflet distribution, and training on making herbal toothpaste from siwak. This activity was conducted in collaboration with SDN 09 Pontianak and was held on Friday, June 24, 2022, with 53 participants. From this activity, the participants received education on the benefits of herbal toothpaste for dental and oral health. In addition, this training activity can increase creativity and skills in creating herbal toothpaste and foster an entrepreneurial spirit. After this activity, it will continue with training activities with the theme of entrepreneurship as part of efforts to downstream and commercialize herbal toothpaste products.