Thailand has vast areas of tropical forests with many indigenous plants, but limited information is available on their phytochemical profile and in vitro inhibitions of enzymatic and nonenzymatic reactions. This study investigated phenolic profiles using liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS), antioxidant activities, and in vitro inhibitory activities of 10 indigenous plants on key enzymes related to obesity (lipase), diabetes (α-amylase and α-glucosidase), and Alzheimer's disease (cholinesterases and β-secretase). The nonenzymatic anti-glycation reaction was also investigated. The 10 indigenous plants were Albizia lebbeck (L.) Benth, Alpinia malaccensis (Burm.) Roscoe, Careya arborea Roxb., Diplazium esculentum (Retz.) Swartz, Kaempferia roscoeana Wall., Millettia brandisiana Kurz., Momordica charantia , Phyllanthus emblica L., Zingiber cassumunar Roxb, and Zingiber citriodorum J. Mood & T. Theleide. Preparations were made by either freeze-drying or oven-drying processes. Results suggested that the drying processes had a minor impact on in vitro inhibitions of enzymatic and nonenzymatic reactions ( P. emblica was the most potent antioxidant provider with high anti-glycation activity (>80% inhibition using the extract concentration of ≤6 mg/mL), while D. esculentum effectively inhibited β-secretase activity (>80% inhibition using the extract concentration of 10 mg/mL). C. arborea exhibited the highest inhibitory activities against lipase (47-51% inhibition using the extract concentration of 1 mg/mL) and cholinesterases (>60% inhibition using the extract concentration of 2 mg/mL), while Mi. brandisiana dominantly provided α-amylase and α-glucosidase inhibitors (>80% inhibition using the extract concentration of ≤2 mg/mL). Information obtained from this research may support usage of the oven-drying method due to its lower cost and easier preparation step for these studied plant species and plant parts. Furthermore, the information on in vitro inhibitions of enzymatic and nonenzymatic reactions could be used as fundamental knowledge for further investigations into other biological activities such as cell culture or in vivo experiments of these health-beneficial plants.

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Industrial hemp is characterized by a huge amount of by-products, such as inflorescences, that may represent high-quality sources of biomolecules with pharmaceutical interest. In the present study, we have evaluated the phytochemical profile, including terpene and terpenophenolic compounds, of the essential oils (EOs) of Futura 75 , Carmagnola selezionata and Eletta campana hemp varieties. The EOs were also tested for antifungal properties toward Trichophyton mentagrophytes, Trichophyton rubrum, Arthroderma crocatum, Arthroderma quadrifidum, Arthroderma gypseum, Arthroderma curreyi, and Arthroderma insingulare . In parallel, we investigated the inhibitory effects of the EOs against tyrosinase, and the production of prostaglandin E 2 in isolated mouse skin exposed to hydrogen peroxide. In human H1299 lung adenocarcinoma cells, we also evaluated the influence of the EOs on the gene expression of angiotensin-converting enzyme 2 (ACE2) and transmembrane protease serine 2 (TMPRSS2), which are involved in SARS-CoV-2 entry in human host. E -caryophyllene and α-pinene were the prominent terpenes in the EOs, whereas the cannabidiolic acid was the terpenophenol present at higher concentration. The EOs inhibited the growth of all tested dermatophytes species. In isolated skin specimens, EOs prevented the hydrogen-peroxide-induced synthesis of prostaglandin E 2 , consistent with the intrinsic antityrosinase activity. Finally, in H1299 cells, all tested EOs reduced the gene expression of ACE-2 and TMPRSS2, as well. Therefore, the present findings highlight the rationale for the use of the present EOs against infectious diseases.

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The emergence of combinatorial chemistries and the increased discovery of natural compounds have led to the production of expansive libraries of drug candidates and vast numbers of compounds with potentially interesting biological activities. Despite broad interest in high throughput screening (HTS) across varied fields of biological research, there has not been an increase in accessible HTS technologies. Here, we present a simple microarray sandwich system suitable for screening chemical libraries in cell-based assays at the benchtop. The microarray platform delivers chemical compounds to isolated cell cultures by 'sandwiching' chemical-laden arrayed posts with cell-seeded microwells. In this way, an array of sealed cell-based assays was generated without cross-contamination between neighbouring assays. After chemical exposure, cell viability was analyzed by fluorescence detection of cell viability assays on a per microwell basis using a standard microarray scanner. We demonstrate the efficacy of the system by generating four hits from toxicology screens towards MCF-7 human breast cancer cells. Three of the hits were identified in a combinatorial screen of a library of natural compounds in combination with verapamil, a P-glycoprotein inhibitor. A fourth hit, 9-methoxy-camptothecin, was identified by screening the natural compound library in the absence of verapamil. The method developed here miniaturizes existing HTS systems and enables the screening of a wide array of individual or combinatorial libraries in a reproducible and scalable manner. We anticipate broad application of such a system as it is amenable to combinatorial drug screening in a simple, robust and portable platform.

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Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) induces apoptosis in many transformed cells but not in normal cells and, hence, has been expected as a new anticancer strategy. During our studies on search for bioactive natural products from various natural resources such as plants and microorganisms, we recently identified several natural products which exhibited activities related to TRAIL signaling. Dimeric sesquiterpenoids isolated from Zingiberaceous plant, Curcuma parviflora, showed enhancement activity of gene expression of TRAIL-receptor and TRAIL-receptor protein level. Several new isoflavone natural products, named brandisianins, were isolated from Leguminosaeous plant, Millettia brandisiana, by our screening study targeting TRAIL-receptor expression enhancement activity. A dihydroflavonol (BB1) that was extracted from Compositaeous plant, Blumea balsamifera, and fuligocandin B, a new anthranilylproline-indole alkaloid isolated from myxomycete were found to exhibit reversal effect of TRAIL resistance activity.

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In a screening study for natural products with tumor-selective apoptosis-inducing properties, six new isoflavonoids (1- 6), named brandisianins A-F, respectively, have been isolated from a MeOH extract of the dried leaves of Millettia brandisiana, together with five known compounds. The structures of the new compounds were elucidated by spectroscopic data interpretation. Among these compounds, brandisianin D (4) exhibited death-receptor 5 expression enhancement activity in a luciferase assay based in DLD-1/ SacI cells. The results suggest that brandisianin D (4) might overcome TRAIL-resistance by an increase in DR5 expression.

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