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During the COVID-19 (coronavirus disease 2019) outbreak, many people were infected, and the symptoms may persist for several weeks or months for recovering patients. This is also known as "long COVID" and includes symptoms such as fatigue, joint pain, muscle pain, et cetera. The COVID-19 virus may trigger hyper-inflammation associated with cytokine levels in the body. COVID-19 can trigger inflammation in the joints, which can lead to osteoarthritis (OA), while long-term COVID-19 symptoms may lead to joint damage and other inflammation problems. According to several studies, sesame has potent anti-inflammatory properties due to its major constituent, sesamin. This study examined sesamin's anti-inflammatory, anti-osteoarthritis, and anti-COVID-19 effects. Moreover, in vivo and in vitro assays were used to determine sesamin's anti-inflammatory activity against the RAW264.7 and SW1353 cell lines. Sesamin had a dose-dependent effect (20 mg/kg) in a monoiodoacetic acid (MIA)-induced osteoarthritis rat model. Sesamin reduced paw swelling and joint discomfort. In addition, the findings indicated that sesamin suppressed the expression of iNOS (inducible nitric oxide synthase) and COX-2 (cyclooxygenase-2) in the RAW264.7 cell line within the concentration range of 6.25–50 μM. Furthermore, sesamin also had a suppressive effect on MMP (matrix metalloproteinase) expression in chondrocytes and the SW1353 cell line within the same concentration range of 6.25–50 μM. To examine the anti-viral activity, an in silico analysis was performed to evaluate sesamin's binding affinity with SARS-CoV-2 RdRp (severe acute respiratory syndrome coronavirus 2 RNA-dependent RNA polymerase) and human ACE2 (angiotensin-converting enzyme 2). Compared to the controls, sesamin exhibited strong binding affinities towards SARS-CoV-2 RdRp and human ACE2. Furthermore, sesamin had a higher binding affinity for the ACE2 target protein. This study suggests that sesamin shows potential anti-SARS-CoV-2 activity for drug development. [ABSTRACT FROM AUTHOR]

Parkinson's disease (PD) is one of the large-scale health issues detrimental to human quality of life, and current treatments are only focused on neuroprotection and easing symptoms. This study evaluated in silico binding activity and estimated the stability of major metabolites in the roots of R. palmatum (RP) with main protein targets in Parkinson's disease and their ADMET properties. The major metabolites of RP were subjected to molecular docking and QSAR with α-synuclein, monoamine oxidase isoform B, catechol o-methyltransferase, and A2A adenosine receptor. From this, emodin had the greatest binding activity with Parkinson's disease targets. The chemical stability of the selected compounds was estimated using density functional theory analyses. The docked compounds showed good stability for inhibitory action compared to dopamine and levodopa. According to their structure–activity relationship, aloe-emodin, chrysophanol, emodin, and rhein exhibited good inhibitory activity to specific targets. Finally, mediocre pharmacokinetic properties were observed due to unexceptional blood–brain barrier penetration and safety profile. It was revealed that the major metabolites of RP may have good neuroprotective activity as an additional hit for PD drug development. Also, an association between redox-mediating and activities with PD-relevant protein targets was observed, potentially opening discussion on electrochemical mechanisms with biological functions. [ABSTRACT FROM AUTHOR]

Osmanthus fragrans (Thunb.) Lour. flowers (OF-F) have been traditionally consumed as a functional food and utilized as folk medicine. This study evaluated the antioxidant, anti-inflammatory and cytotoxic effects of OF-F extracts on prostate cancer cells (DU-145) and determined possible protein-ligand interactions of its compounds in silico. The crude OF-F extracts—water (W) and ethanol (E) were tested for phytochemical screening, antioxidant, anti-inflammatory, and anti-cancer. Network and molecular docking analyses of chemical markers were executed to establish their application for anticancer drug development. OF-F-E possessed higher total polyphenols (233.360 ± 3.613 g/kg) and tannin (93.350 ± 1.003 g/kg) contents than OF-F-W. In addition, OF-F-E extract demonstrated effective DPPH scavenging activity (IC50 = 0.173 ± 0.004 kg/L) and contained a high FRAP value (830.620 ± 6.843 g Trolox/kg). In cell culture experiments, OF-F-E significantly reduced NO levels and inhibited cell proliferation of RAW-264.7 and DU-145 cell lines, respectively. Network analysis revealed O. fragrans (Thunb.) Lour. metabolites could affect thirteen molecular functions and thirteen biological processes in four cellular components. These metabolites inhibited key proteins of DU-145 prostate cancer using molecular docking with rutin owning the highest binding affinity with PIKR31 and AR. Hence, this study offered a new rationale for O. fragrans (Thunb.) Lour. metabolites as a medicinal herb for anticancer drug development. [ABSTRACT FROM AUTHOR]

Perilla frutescens (L.) Britt. is extensively cultivated in East Asia as a dietary vegetable, and nutraceuticals are reportedly rich in bioactive compounds, especially with anticancer activities. This study explored the in vitro cytotoxic effects of P. frutescens parts' (stems, leaves, and seeds) extracts on prostate cancer cells (DU-145) and possible interactions of putative metabolites to related prostate cancer targets in silico. The ethanol extract of P. frutescens leaves was the most cytotoxic for the prostate cancer cells. From high-performance liquid chromatography analysis, rosmarinic acid was identified as the major metabolite in the leaf extracts. Network analysis revealed interactions from multiple affected targets and pathways of the metabolites. From gene ontology enrichment analysis, P. frutescens leaf metabolites could significantly affect 14 molecular functions and 12 biological processes in five cellular components. Four (4) KEGG pathways, including for prostate cancer, and six (6) Reactome pathways were shown to be significantly affected. The molecular simulation confirmed the interactions of relevant protein targets with key metabolites, including rosmarinic acid. This study could potentially lead to further exploration of P. frutescens leaves or their metabolites for prostate cancer treatment and prevention. [ABSTRACT FROM AUTHOR]

Background: This study describes the isolation of major chemical constituent from the bark of Uvaria rufa Blume, commonly known as "allagat or susong kalabaw", an indigenous Philippine medicinal plant that belongs to the family Annonaceae. It is a short climbing shrub that grows in low and medium-altitude forests in the country. Materials and Methods: The bark samples of U. rufa were air-dried for three months without exposure to sunlight. The samples were ground in a blender, then, soaked in CH2Cl2 and in ethanol for three days and then, filtered. The crude extract of U. rufa was chromatographed on a gravity column dry packed with silica gel and was fractionated by silica gel chromatography using increasing proportion of acetone in CH2Cl2 at 10% increment. The purified isolates were subjected to NMR for structure elucidation. Their structures were identified mainly by using ¹H-NMR and by comparing current NMR data with those reported in the literature. Results: The results showed that the air-dried bark dichloromethane extract of the plant afforded glutinol. Glutinol and ethanolic extract exhibited anti-mitotic activity (18.33 % and 18.93 %, respectively), comparable to methotrexate (19.07 %), a well-known anti-cancer drug and even more potent in which they surpassed by 0.74 % and 0.14 %. Conclusion: The dichloromethane extract of the bark of U. rufa afforded glutinol that can be one the main metabolites responsible for the anti-mitotic activity of the plant. It may also contained other substances that might have great potential as novel therapeutic agents for cancer. [ABSTRACT FROM AUTHOR]

Background: This study describes the isolation of chemical constituents from the leaves and bark of Phyllanthus acidus, a medicinal plant widely used for the treatment of several ailments. Materials and Methods: The crude extract of P. acidus was chromatographed on a gravity column dry packed with silica gel and was fractionated by increasing proportions of acetone in CH2Cl2. The purified isolates were subjected to NMR for structure elucidation. Their structures were identified mainly by using 1H-NMR and by comparing current NMR data with those reported in the literature. Results: The results showed that the air-dried leaves extracts of the plant afforded mixture of β-sitosterol and stigmasterol while the bark yielded mixture of phyllanthol, α-amyrin, β-amyrin and lupeol. Conclusion: The air-dried of DCM extract of P. acidus resulted in the isolation of the mixture of phyllanthol, α- amyrin, β-amyrin and lupeol from the bark and mixture of β-sitosterol and stigmasterol from the leaves of the plant. It is important to conduct detailed pharmacological and toxicity investigations as well as clinical studies using different doses or concentrations to verify its traditional uses. [ABSTRACT FROM AUTHOR]

Background: Asystasia gangetica, also referred to as Chinese Violet is an invasive weed that has been revealed to contain biologically active components and manifest pharmacological effects. Phytochemical analysis on different extracts of A. gangetica reported that the plant contains steroids, sugars, phenolics, flavonoids, saponins, tannins and amino acids, alkaloids, terpenoids, quinines and carbohydrates and bioassay techniques performed using the plant material manifested its antioxidant, anti-asthmatic and antidiabetic properties. Materials and Methods: To further understand how the existing and the potential abilities of A. gangetica possibly work, the total phenolics, total flavonoids, total condensed tannins and total polysaccharide content of different extracts of A. gangetica have been analyzed as well as its antioxidation properties using DDPH and FRAP assays. The effect of combining A. gangetica extract to the methanolic extract of Morus alba leaves on the potency of the antioxidation properties of both plant materials was also explored. Results: Evaluation of the results revealed that A. gangetica ethanol extract is the extract most abundant in polyphenol, DCM extract in flavonoids and condensed tannins, while only a few extracts had polysaccharides. Ethanol extract has the most promising DPPH free radical scavenging activity, while methanol extract was reported to have the highest Trolox equivalent. No significant synergistic effect was observed in the combination of A. gangetica and M. alba extracts. Conclusion: These findings provide information on the A. gangetica extracts as antioxidant agents and as a source of natural products. Consequently, the results provide a new direction for medical research. [ABSTRACT FROM AUTHOR]

Background: This study aimed to isolate the bioactive components from the aerial parts of Premna odorata Blanco and to evaluate the hypoglycemic potentials of the crude extracts, sub-fractions and final isolate. Materials and Methods: The plant material underwent a series of enzyme assay-guided isolation and purification having the fractions assayed for inhibitory activity against a-amylase using 3,5-dinitrosalicylic acid (DNS) colorimetric method for each stage. H.1 isolate was tested for a-amylase and a-glucosidase inhibitory activity and glucose uptake by yeast cells. Phytochemical characterization and 1H and 13C NMR spectral analysis were done for the structure elucidation of H.1. Results: In vitro amylase studies revealed that at 100 µg/mL concentrations, hexane crude extract, fraction F (20%/80% and 10%/90% n-hexane/dichloromethane fractions) and F.3 (10:1 v/v petroleum ether/ethyl acetate sub-fraction) exhibited 34.38±0.116%, 71.86± 4.909% and 42.16±1.257% inhibition against a-amylase (at 1000 µg/mL concentration), respectively. H.1 isolate exerted significant inhibition (p < 0.05) of 55.99± 2.202% and 72.43±3.988% against a-amylase and a-glucosidase enzyme (both at 1000 µg/mL concentration), respectively and significant glucose uptake of 13.85± 0.368%. The purified isolate was spectroscopically confirmed as a 5:1 mixture of ß-sitosterol (H.1a) and stigmasterol (H.1b). Conclusion: The compounds have significant inhibitory activity against carbohydrate-hydrolyzing enzymes and may be potentially developed as adjuvant pharmacotherapy for type 2 diabetes. [ABSTRACT FROM AUTHOR]

The use of foodstuff as natural medicines has already been established through studies demonstrating the pharmacological activities that they exhibit. Knowing the nutritional and pharmacological significance of foods enables the understanding of their role against several diseases. Among the foods that can potentially be considered as medicine, is sesame or Sesamum indicum L., which is part of the Pedaliaceae family and is composed of its lignans such as sesamin, sesamol, sesaminol and sesamolin. Its lignans have been widely studied and are known to possess antiaging, anticancer, antidiabetes, anti-inflammatory and antioxidant properties. Modern chronic diseases, which can transform into clinical diseases, are potential targets of these lignans. The prime example of chronic diseases is rheumatic inflammatory diseases, which affect the support structures and the organs of the body and can also develop into malignancies. In line with this, studies emphasizing the anti-inflammatory and anticancer activities of sesame have been discussed in this review. [ABSTRACT FROM AUTHOR]