Background: Diabetes mellitus is a metabolic disease, characterized by hyperglycemia due to disturbance in both insulin secretion and function. One of theurapeutic approaches is to reduce blood glucose levels by inhbiting α-/β-glucosidase and α-amylase involved in carbohydrate digestion. Thus, inhibition of these enzymes play important role in the treatment of diabetes mellitus. Roselle (Hibiscus sabdariffa L.) has been known to have several medicinal properties and potency as an antidiabetics agents. This reseacrh aimed to observe antidiabetic properties of roselle ethanol extract (REE) towards α-glucosidase, β-glucosidase and α-amylase. Materials and Methods: REE was done with maceration technique using diluent of 70% ethanol. Antidiabetic properties were measured by inhibitory activity of α-amylase, α-glucosidase and β-glucosidase. Results: REE was able to inhibit α-/β-glucosidase and α-amylase in the highest concentration with inhibition percentage of 72.68, 47.34 and 73.08% respectively, and were comparable with Acarbose of 81.49, 50.97, 73.08%. The median inhibitory concentration (IC 50 ) of α-/β-glucosidase and α-amylase of REE were 15.81, 41.77, 18.09 µg/mL respectively, and Acarbose were 9.45, 22.57, 3.64 µg/mL respectively. Conclusion: REE inhibits α-/β-glucosidase and α-amylase.

Background: Mangosteen (Garcinia mangostana Linn.) is tropical fruit that known to contain bioactive compounds which has particular function as antioxidant, anti-inflammatory and antibacterial. Mangosteen rind extract is known to have high contents of xanthone compounds which have antioxidant and free radical scavenging activities. This study was done to determine the contents of xanthone derivatives using Liquid Chromatography Mass Spectrometry (LC-MS/MS) and antioxidant activity of six different maturity levels of mangosteen rind extract using Electron spin resonance (ESR). Method: Mangosteen was classified based on the maturity level by its visual characteristic and divided into six criteria of maturity. The mangosteen rinds were extracted through maceration and freeze drying method. Qualitative analysis of xanthone was obtained using LC-MS/MS. Antioxidant activity was determined using ESR spectrometer. To evaluate antioxidant activity, using 2,2-diphenyl-1-picrylhydrazyl (DPPH) was used as free radical scavenger method. Results: The LC-MS/MS analysis showed that the highest concentrations are filled by mangosteen rind with maturity level 6. Moreover, each maturity levels of mangosteen rind extract has different g value compared to DPPH free radical. Different g value indicated the different type of free radical and decreasing g value indicated the declining intensity of free radical. The higher decreasing of g value was mangosteen rind with maturity level 4, 5 and 6. Conclusion: Mangosteen rind extract contains xanthone and its derivatives and ESR analysis showed that different maturity levels on mangosteen rind has different antioxidant activity as indicated by declining free radical intensity.

Background: Hypothyroidism is a common side effect found in patients with multidrug-resistant tuberculosis taking ethionamide. The mechanism of ethionamide-induced hypothyroidism is potentially caused by the structure of ethionamide compounds chemically similar to thioamide, such as propylthiouracil (C7H8N2S), which inhibits thyroid hormone synthesis. However, hypothyroidism is caused not only by a lack of production but also by signaling alteration. Thyroid hormone action is mediated by thyroid hormone receptors (TRs), members of the nuclear receptor superfamily that regulate their target genes. Unfortunately, there are limited studies on the potential interaction of ethionamide with TRs. Objective: In the present study, we want to elaborate on the potential interaction of ethionamide with TRs which might alter the thyroid hormone genomic regulation. Methods: Molecular docking studies were used to evaluate the potential interaction between ethionamide with TRα and TRβ. Results: The molecular docking results on TRα showed more than one hydrogen bond-steric interaction formed from the ethionamide-amino acid residue interaction. Ethionamide-TRβ interaction showed more than one steric interaction, but the hydrogen bonds are not visualized. The docking score between ethionamide and TRα is −7.373 kcal/ mol and higher than its interaction with TRβ. Conclusion: These findings indicate that ethionamide can interact with TRα and TRβ. However, the ethionamide-TRα interaction is stronger than ethionamide-TRβ interaction. Our study reports a novel mechanism of action of ethionamide-induced hypothyroidism.

Selective inhibitors of CYP isoforms gaining importance in the treatment of cancers caused by hormonal imbalance. Metabolites of estradiol and polyaromatic hydrocarbons generated due to CYP1B1 activity were reported to be oncogenic. The selective CYP1B1 inhibitors could have the potential therapeutic utility in controlling the cancer due to these oncogens. Due to the CYP isoforms high sequence similarity the design of selective CYP inhibitor is difficult. Recently our group has reported two novel chemical classes (scaffolds) that are specific towards CYP1B1. The chemical architecture of these compounds should give valuable information for its selectivity and potency against CYP1B1. Overlay of our compounds and ANF by Shape and electrostatic based similarity and molecular docking displayed different orientations. Moreover the study has shown the overlay of three atom bridge of selective inhibitor superimposed on-O-CHlinking aryl groups rather than-CO-CH=CHof ANF. Molecular docking simulation revealed that the selective inhibitors are either establishing H-bonding interaction with Asp333 or π-π staking interaction Phe231 and Phe268. Molecular docking simulation has provided much more information rather than simple shape and electrostatic based similarity study. Crucial H-bonding interactions and π-π staking interactions responsible for selectivity towards CYP1B1 were identified. Two atom linker between the aryl groups matter, cyclization simply ensures the planarity of ANF and quinazolines.

Mangosteen has several important elements for biological activities such as antioxidant, anti-inflammatory, anti-bacterial and anti-cancer. There are γ-mangostin, αmangostin, flavonoids, saponins, and tannins which could stimulate the collagen deposition and accelerate wound healing process. Burn injury cause deep wound in the skin and often cause cicatrix and keloid scar on the skin. However, there is limited information about role of mangosteen in skin wound healing after burn injury. Fifty 10 week-old male rats, were subjected to burn injury using automatic temperature control. Burn injury was created by direct contact of hot plate (170°C) for 15 seconds on rats' inter scapula region. We elaborated the role of extract mangosteen in skin wound healing by applying daily gel contain with active compound derived from mangosteen. There was no significant weight change during treatment period. We observed that there was significant increase of Epidermal Growth Factors (EGF) expression in 14 as shown in immunohistochemistry and confirmed by western blot protein results. Taken together, mangosteen peel extractmediated changes in the expression of growth factors in burned rat skins. Mangosteen peel extract might have a role in the acceleration of skin wound healing.