Machine Learning and In Vitro Chemical Screening of Potential α-Amylase and α-Glucosidase Inhibitors from Thai Indigenous Plants

Diabetes mellitus is a major predisposing factor for cardiovascular disease and mortality. α-Amylase and α-glucosidase enzymes are the rate-limiting steps for carbohydrate digestion. The inhibition of these two enzymes is clinically used for the treatment of diabetes mellitus. Here, in vitro study and machine learning models were employed for the chemical screening of inhibiting the activity of 31 plant samples on α-amylase and α-glucosidase enzymes. The results showed that the ethanolic twig extract of Pinus kesiya had the highest inhibitory activity against the α-amylase enzyme. The respective ethanolic extract of Croton oblongifolius stem, Parinari anamense twig, and Polyalthia evecta leaf showed high inhibitory activity against the α-glucosidase enzyme. The classification analysis revealed that the α-glucosidase inhibitory activity of Thai indigenous plants was more predictive based on phytochemical constituents, compared with the α-amylase inhibitory activity (1.00 versus 0.97 accuracy score). The correlation loading plot revealed that flavonoids and alkaloids contributed to the α-amylase inhibitory activity, while flavonoids, tannins, and reducing sugars contributed to the α-glucosidase inhibitory activity. In conclusion, the ethanolic extracts of P. kesiya, C. oblongifolius, P. anamense, and P. evecta have the potential for further chemical characterization and the development of anti-diabetic recipes.

Antifungal mono- and dimeric nitrogenous bisabolene derivatives from a sponge in the order Bubarida from Futuna Islands

An abundant sponge of the order Bubarida was selected for further chemical investigation following biological and chemical screening of sponges collected from Futuna Islands in the Indo-Pacific. Ten new nitrogenous...

Improving Particle Collection Efficiency of Sampling Wipes used for Trace Chemical Detection

Improvement of the particle collection efficiency of sampling wipes is desirable for optimizing the performance of many wipe-based chemical analysis techniques used for trace chemical screening applications. In this note,...

Preparation and Evaluation of Nanophytosomes of Aqueous Extract of Leaves of Momordica charantia

Though there was not enough data available throughout the phytosome research, authors tried maximum to provide all inputs for the preparation of phytosomes. The objectives of the present research work focused on the investigation of phyto chemical constituents of aqueous extract, preparation of nanophytosomes of aqueous extract. Momorica charantia plants were collected locally from the village of Muhavur. The leaves were separated from the plant and the leaves were washed with water and then again washed with chloroform to remove soil particles and the leaves were spread and dried in the shade for 4 days. The aqueous extract of Momorica charantia obtained was subjected to qualitative analysis to test the presence of various phytochemicals. Particle size of prepared nanophytosomes was analyzed by photon correlation spectroscopy using a Shimadzu particle size analyzer (SALD 2101, Japan). Diluted nanophytosomal suspension was placed into the sample dispersion unit while stirring at room temperature (in order to reduce the inter particle aggregation). All analyses has been performed in triplicate. Nanophytosomes of Momordica charantia aqueous extract was effectively prepared and tested. The aqueous extract was evaluated phyto chemical screening followed by all characterization studies. Phytochemical screening study remaining that the extract consists of flavanoids. The characterization study showed that the phytosomes are having nano size, good stability properties with round to spherical shape with smooth surfaces.

Novel chemical inhibitor against SOD1 misfolding and aggregation protects neuron-loss and ameliorates disease symptoms in ALS mouse model

Amyotrophic Lateral Sclerosis (ALS) is a fatal neurodegenerative disease characterized by selective death of motor neurons. Mutations in Cu, Zn-superoxide dismutase (SOD1) causing the gain of its toxic property are the major culprit of familial ALS (fALS). The abnormal SOD1 aggregation in the motor neurons has been suggested as the major pathological hallmark of ALS patients. However, the development of pharmacological interventions against SOD1 still needs further investigation. In this study, using ELISA-based chemical screening with wild and mutant SOD1 proteins, we screened a new small molecule, PRG-A01, which could block the misfolding/aggregation of SOD1 or TDP-43. The drug rescued the cell death induced by mutant SOD1 in human neuroblastoma cell line. Administration of PRG-A01 into the ALS model mouse resulted in significant improvement of muscle strength, motor neuron viability and mobility with extended lifespan. These results suggest that SOD1 misfolding/aggregation is a potent therapeutic target for SOD1 related ALS.

Mycochemical composition and antioxidant potential of Macrolepiota africana (Heim) Heinem. (Agaricaceae), an edible mushroom from Gabon

Macrolepiota africana is a fungus used as food in Gabon for its culinary properties. However, its nutritional value, mycochemical contents, antioxidant properties and health potential still unknown. The present study investigated the phytochemicals and antioxidant properties of this mushroom species. This chemical screening was followed by a study of the antioxidant activity and a prediction of additional pharmacological activities of M. africana. Using standard methodology, the mycochemical analyses were carried out on aqueous, hydro-ethanolic and ethanolic fungi extracts. The antioxidant activity of the mushroom extracts was determined using DPPH radical scavenging assay. Apart from Digitoxigenine, flavonol and gitoxigenine that were not found in any of the extracts, all other tested mycochemical were found in atleast one of the extracts. Alkaloids, flavonoids, polyphenols, oses and holosides, proanthocyanidins and coumarins were found in all extracts at different intensity. Saponosids, sterols and triterpenes, tannins gallics, reducing sugar, anthracenosides and digitoxine were found in two extracts while tannins catechics, flavone and gitoxine were detected only in one extract. The dosage of phenolic compounds confirmed the richness of this fungus in total polyphenols, its moderate richness in proanthocyanidins, the lack of flavonoids in the aqueous extract and the moderate richness of the hydro-ethanolic and ethanolic extracts in flavonoids. Regarding the antioxidant activities, the results obtained for the DPPH trapping test showed that the different extracts had low to moderate antioxidant activity with antioxidant activity index (IAA) ranged 0.29 to 0.97 respectively in aqueous and ethanolic extracts. The presence of these mycochemical compounds along with the identified antioxidant activities shows that this M. africana have some pharmacological potential.

PHYTOCHEMICAL STUDY AND ANTIBACTERIAL ACTIVITY OF ETHANOLIC AND AQUEOUS EXTRACTS OF BARKS OF MYRIANTHUS HOLSTII ENGL. (CECROPIACEAE)

The aim of this work is to study phytochemicals and evaluate the antibacterial activity of aqueous and ethanolic extracts of Myrianthus holstii bark on three reference and five clinical strains derived from biological products. The results obtained show that the gives the best extraction yield. Chemical screening revealed the presence of polyphenols, alkaloids, flavonoids, saponosides, quinones, anthocyanins, tannins, terpenoids and sterols in both extracts. The results obtained show that the strains tested have a variable sensitivity for the two extracts and their concentrations. Diffusion and dilution methods on Muller-Hinton were used to evaluate the antibacterial activity of the extracts. The diameters of the inhibition zones are between 8 and 16 mm for the ethanolic extract starting from 25 mg/mL and between 8 and 12 mm for the aqueous extract at 50 mg/mL. The results revealed that these extracts have a dose-dependent antibacterial activity on the bacterial strains used. However, the 70% ethanolic extract has a better antibacterial potential on the strains compared with the aqueous extract, namely on S. aureus (CMI=3.12 mg/mL), E. coli ATCC (CMI=12.5 mg/mL) and S. aureus Meti-R (CMI=12.5 mg/mL). Also, this extract is bactericidal on all strains studied and its MIC ranges from 3.12 to 100 mg/mL after 24 and 48 hours of incubation. This study showed that extracts of Myrianthus holstii could be used in the treatment of infectious diseases.

Obesogens: How They Are Identified and Molecular Mechanisms Underlying Their Action

Adult and childhood obesity have reached pandemic level proportions. The idea that caloric excess and insufficient levels of physical activity leads to obesity is a commonly accepted answer for unwanted weight gain. This paradigm offers an inconclusive explanation as the world continually moves towards an unhealthier and heavier existence irrespective of energy balance. Endocrine disrupting chemicals (EDCs) are chemicals that resemble natural hormones and disrupt endocrine function by interfering with the body’s endogenous hormones. A subset of EDCs called obesogens have been found to cause metabolic disruptions such as increased fat storage, in vivo. Obesogens act on the metabolic system through multiple avenues and have been found to affect the homeostasis of a variety of systems such as the gut microbiome and adipose tissue functioning. Obesogenic compounds have been shown to cause metabolic disturbances later in life that can even pass into multiple future generations, post exposure. The rising rates of obesity and related metabolic disease are demanding increasing attention on chemical screening efforts and worldwide preventative strategies to keep the public and future generations safe. This review addresses the most current findings on known obesogens and their effects on the metabolic system, the mechanisms of action through which they act upon, and the screening efforts through which they were identified with. The interplay between obesogens, brown adipose tissue, and the gut microbiome are major topics that will be covered.

Phytochemical Evaluation of Mentha Species including Antioxidant Activity

Mentha arvensis is a belonging to the family of Lamiaceae; Wild mint is often used as a domestic herbal remedy, being valued especially for its antiseptic properties and its beneficial effect on the digestion. The phytochemical screening of hydro alcoholic extracts presenting the flavonoids, resins, triterpenoids, tannins and phenolic groups. The percentage of antioxidant potential is 91.28, by DPPH method. The estimation value of total phenol content is 936±71, and total flavonoid conent is 479±66. The crude drug evaluated by the various physical methods, and all the results are within the limit of world health organisation prescribed. The antioxidant potential is evaluation by DPPH method. The phyto chemical screening based upon the colour reaction and estimated the chief phyto constituents like phenolic content and flavonoid. This work identification and characterisation of the purity and quality of the monograph of the Mentha arvensis. This work is more useful to further researchers.