Steroid 5-alpha reductases (SRD5As) are responsible for the conversion of testosterone to dihydrotestosterone, a potent androgen, which is the aetiologic factor of androgenetic alopecia. This study aimed to compare the SRD5A gene expression suppression activity exerted by Thai rice bran extracts and their components and investigate the interactional mechanism between bioactive compounds and SRD5A2 using molecular dynamics (MD) simulation. Bran of Oryza sativa cv. Tubtim Chumphae (TRB), Yamuechaebia Morchor (YRB), Riceberry (RRB), and Malinil Surin (MRB), all rice milling by-products, was solvent-extracted. The ethanolic extract of TRB had the highest sum of overall bioactive compounds (γ-oryzanol; α-, β-, and γ-tocopherol; phenolics; and flavonoids). Among all extracts, TRB greatly downregulated the expression of SRD5A1, SRD5A2, and SRD5A3; there were no significant differences between TRB and finasteride regarding SRD5A suppression. The linear relationship and principal component analysis supported that the α-tocopherol content was correlated with the SRD5A suppression exerted by TRB. Furthermore, MD simulation demonstrated that α-tocopherol had the highest binding affinity towards SRD5A2 by interacting with residues Phe118 and Trp201. Our findings indicate that α-tocopherol effectively downregulates the expression of SRD5A genes and inhibits SRD5A2 activity, actions that are comparable to standard finasteride. TRB, a source of α-tocopherol, could be developed as an anti-hair loss product.

The COVID-19 pandemic has intensively disrupted global health, economics, and well-being. Andrographis paniculata (Burm. f.) Nees has been used as a complementary treatment for COVID-19 in several Asian countries. This review aimed to summarize the information available regarding A. paniculata and its constituents, to provide critical points relating to its pharmacological properties, safety, and efficacy, revealing its potential to serve as a source of lead compounds for COVID-19 drug discovery. A. paniculata and its active compounds possess favorable antiviral, anti-inflammatory, immunomodulatory, and antipyretic activities that could be beneficial for COVID-19 treatment. Interestingly, recent in silico and in vitro studies have revealed that the active ingredients in A. paniculata showed promising activities against 3CLpro and its virus-specific target protein, human hACE2 protein; they also inhibit infectious virion production. Moreover, existing publications regarding randomized controlled trials demonstrated that the use of A. paniculata alone or in combination was superior to the placebo in reducing the severity of upper respiratory tract infection (URTI) manifestations, especially as part of early treatment, without serious side effects. Taken together, its chemical and biological properties, especially its antiviral activities against SARS-CoV-2, clinical trials on URTI, and the safety of A. paniculata, as discussed in this review, support the argument that A. paniculata is a promising natural source for drug discovery regarding COVID-19 post-infectious treatment, rather than prophylaxis.

The edible bamboo mushroom Dictyophora indusiata, which is rich in food nutrients and has medicinal values, has been investigated for nutrition compositional analysis. Then, three parts (whole mushroom: WE; peel and green mixture: PGE; and core: CE) were determined for antioxidant, MMP-2 inhibition, and anti-inflammatory properties. WE depicted the highest bioactive contents among others. The CE and WE with non-cytotoxic effect on fibroblasts gave high MMP-2 inhibitory activity (44.93% and 30.32%, respectively), compared with L-ascorbic acid (50.65%). For the anti-inflammatory activity, all D. indusiata extracts significantly inhibited the nitric oxide (NO), interleukin (IL)-1β, IL-6, and tumour necrosis factor (TNF)-α secretion compared with the LPS treatment in all-time intervals (P < 0.05). Moreover, WE extract containing various bioactive compounds (polyphenolic, monosaccharide, mucopolysaccharide, allantoin, and alkaloid contents) showed similar anti-inflammatory activity to the standard diclofenac. It can be concluded that WE could be served as functional food ingredients and potential to be healthpromoting products.

Diatoms, as single cell eukaryotic microalgae, are rich sources of lipids, which have either beneficial or detrimental effects on the prevention and treatment of many diseases. Gas chromatography-mass spectrometry (GC-MS) identified diatom lipids with high levels of essential fatty acids (EFAs), especially polyunsaturated FAs (PUFAs) containing both omega-3 and omega-6. Nutritional values of FAs indicated possible applications in the pharmaceutical, nutraceutical, and functional food industries. Diatom FAs showed antioxidative potential on harmful radicals by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) scavenging, with high inhibition of the angiotensin-converting enzyme (ACE) that causes cardiovascular disease (CVD) and hypertension. A computational molecular docking simulation confirmed the inhibition mechanisms of FAs on ACE, with comparable levels of binding free energy to chemically synthesized ACE drugs. Findings suggested that diatom lipids showed potential for use as alternative ACE inhibitors or food supplement for CVD prevention.

This study aims to investigate the antioxidant and anti-cancer activities of Clerodendrum chinense leaf ethanolic extract. The phenylethanoid glycoside-enriched extract, namely verbascoside and isoverbascoside, was determined in the ethanolic C. chinense leaf extract using the validated HPLC method. The ethanolic extract showed DPPH and ABTS free radical scavenging activities with the IC50 values of 334.2 ± 45.48 μg/mL and 1012.77 ± 61.86 µg/mL, respectively, and a FRAP value of 88.73 ± 4.59 to 2480.81 ± 0.00 µM. C. chinense leaf extract exhibited anti-proliferative activity against A549 lung cancer cells in a dose- and time-dependent manner, with the IC50 value of 340.63 ± 89.43, 210.60 ± 81.74, and 107.08 ± 28.90 µg/mL after treatment for 24, 48, and 72 h, respectively. The IC50 values of verbascoside, isoverbascoside, and hispidulin were 248.40 ± 15.82, 393.10 ± 15.27, and 3.86 ± 0.87 µg/mL, respectively, indicating that the anti-proliferative effects of the C. chinense leaf extract mainly resulted from hispidulin and verbascoside. The selectivity index (SI) of C. chinense leaf extract against A549 lung cancer cells vs. normal keratinocytes were 2.4 and 2.8 after incubation for 24 and 48 h, respectively, suggesting the cytotoxic selectivity of the extract toward the cancer cell line. Additionally, the C. chinense leaf extract at 250 µg/mL induced late apoptotic cells up to 21.67% with enhancing reactive oxygen species (ROS) induction. Furthermore, the lung cancer cell colony formation was significantly inhibited after being treated with C. chinense leaf extract in a dose-dependent manner. The C. chinense leaf extract at 250 µg/mL has also shown to significantly inhibit cancer cell migration compared with the untreated group. The obtained results provide evidence of the anti-lung cancer potentials of the C. chinense leaf ethanolic extract.

INTRODUCTION Thai purple rice is attracting attention for its antioxidant effects and health benefits 1 3. The purple color of this rice is due to the deposition of large amounts of the anthocyanin pigment. Certain compounds in the rice have been recognized as health-enhancing substances because of their antioxidant, anti-inflammatory, and anticancer effects 1 3. Although the total contents of useful chemicals in such foodstuffs have been determined via analyses of powdered food crops, we have very limited knowledge about the distribution and concentration of useful chemicals within the crops. Free radicals are generated in plants as a result of antioxidant scavenging activities and biochemical processes 4 7. In most cases, stable paramagnetic species are found in the pigmented colored regions of plant seed coats 5 7. These pigmented regions usually contain various organic compounds such as antioxidants. Electron paramagnetic resonance EPR can be used for the nondestructive detection of free radicals. The EPR spectrum appears either as an asymmetric line shape or as a series of multiple overlapping lines, depending on the sample being assessed 4 7. The X-band 9 GHz EPR imaging EPRI technique exhibits good spatial resolution and sensitivity.

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Since the pandemic of severe acute respiratory syndrome coronavirus (SARS-CoV-2) in December 2019, the infection cases have quickly increased by more than 511 million people. The long epidemic outbreak over 28 months has affected health and economies worldwide. An alternative medicine appears to be one choice to alleviate symptoms and reduce mortality during drug shortages. Dendrobium extract is one of the traditional medicines used for COVID-19 infection. Several compounds in Dendrobium sp. had been reported to exert pharmacological activities to treat common COVID-19-related symptoms. Herein, in silico screening of 83 compounds from Dendrobium sp. by using the SARS-CoV-2 spike protein receptor-binding domain (RBD) as a drug target was performed in searching for a new lead compound against SARS-CoV-2 infection. Four hit compounds showing good binding affinity were evaluated for antiviral infection activity. The new lead compound DB36, 5-methoxy-7-hydroxy-9,10-dihydro-1,4-phenanthrenequinone, was identified with the IC50 value of 6.87 ± 3.07 µM. The binding mode revealed that DB36 bound with the spike protein at the host receptor, angiotensin-converting enzyme 2 (ACE2) binding motif, resulted in antiviral activity. This study substantiated the use of Dendrobium extract for the treatment of SARS-CoV-2 infection and has identified new potential chemical scaffolds for further drug development of SARS-CoV-2 entry inhibitors.