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Objective: Drug resistance can result in mortality and morbidity due to treatment failures. Therefore, researchers are actively involved in the urgent development of new antibacterial agents which are more effective against drug-resistant bacteria. This study is aimed to prepare curcumin derivatives (CD) nanofiber and test its antibacterial activity by disk diffusion test and evaluate their role in wound healing when potentially binds with transforming growth factor-beta type 1 kinase domain (TGF-β) and Glycogen synthase kinase-3 beta (GSK3-β). Method: Molecular docking and molecular dynamic have been used to select the most potent dual-action molecules on both TGF-β and GSK3-β, most active 2 compounds have been synthesized and characterized by 1H and 13C (NMR), IR spectroscopy, Electrospinning of CD in ethanol were studied by adding Poly vinyl alcohol (PVA) as a polymer. The properties of the CD/PVA solutions measured, morphology of electrospun CD/PVA was tested by Scanning Electrode Microscope (SEM), antibacterial activity of electrospun nanofiber against Staphylococcus aureus (S. aureus) was tested by disk diffusion method.Results and Conclusions: CD nanofiber were synthesized successfully. The results showed that CD were successfully synthesized with good yield (72% and 78%) for compound1 and 2 respectively, Disc diffusion antibacterial test demonstrated an increased inhibition zone from 0.5 to 5.0 mg loaded CD with the largest inhibition zone of 8.5 ± 0.71 and 9.67 ± 0.29 mm for compound1 and 2 respectively. Hence, it can be concluded that these CD/PVA could be a new source in designing new antibacterial wound dressing for diabetic patients.

Abstract Background Canarium patentinervium leaves are used by the local indigenous people of Malaysia for wound healing. The current study is undertaken to screen the comprehensive antibacterial activity of the leaves and barks extracts, fractions and isolated compounds from this plant. Bioassay guided fractionation was also undertaken to deeply evaluate the antibacterial activity of the water fraction of the leaves extract. This is to provide preliminary scientific evidence to the ethnopharmacology usage of this plant by investigating antibacterial properties of the plant and its isolated constituents. Methods Bio-assay guided fractionation and subsequent isolation of compounds using open column chromatography. The antibacterial activity against gram positive and gram negative ATCC strain and resistant clinical strains were evaluated using microtiter broth dilution method to determine minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and time-kill assay. The chemical structure of the isolated compounds from the water fraction of the ethanol extract of leaves was elucidated using Nuclear Magnetic Resonance (NMR). Results The ethanol extract of the leaves and barks showed antimicrobial activity against all four ATCC and eight clinical isolates. The ethanol extract of the leaves and the corresponding water fraction had good activity against MRSA S. aureus. (MIC: 250 μg/ml) and had bactericidal effect on eight of the clinical strains (MSSA,MRSA, oxacillin-resistant CONS, oxacillin-sensitive CONS, Enterococcus faecalis, Klebsiela species, Kleb pneumoniae ESBL and Candida parapsilosis). Further phytochemical investigation of the water fraction of the crude ethanol extract of leaves afforded compound 7 (hyperin) and compound 8 (cynaroside) that had bactericidal activity against tested bacterial species (MIC 50 μg/ml and 100 μg/ml). The two compounds were isolated from this genus for the first time. Conclusions These results may provide a rational support for the traditional use of Canarium patentinervium Miq. in infections and wound healing, since the antimicrobial compounds isolated were also present in the leaves extract.

Common manifestation of gout is deposition of monosodium urate crystals in joints followed by cytokinine-induced inflammatory responses. Xanthin Oxidase (PDB ID: 3NVY) and proinflammatory cytokinines, eg., TAK1 (PDB ID: 7NTH) and IL-1 β (PDB ID: 5R8Q) are vastly accountable for the severity of the disease. Inhibition of these targets with phytoconstituents would be preferable option in the treatment of gout patients. In the present study, in silico molecular docking analysis of Orientin, Vitexin, Apigenin, and Harman were performed using Glide XP, Schrodinger 2017_2, with above drug targets to investigate docking score, binding free energies and druggability. The results revealed a docking score and binding energy in the range of -11.862 kcal/mol to -3.130 kcal/ mol and -53.282 kcal/mol to -32.346 kcal/mol respectively. Except Harman all the compounds have considerable docking score and binding energies, which typically indicate that they have the optimum interaction with the binding sites. ADME/T analysis performed using QikProp program of Schrödinger 2017-2 and the SwissADME online server indicated that the Vitexin and Apigenin have the physiochemical properties to be developed as drugs. These studies can be used to develop alternate therapeutic options for the treatment of gout. [ABSTRACT FROM AUTHOR]

Uterine fibroids (UFs) are extremely common neoplasm affecting up to 8 out of 10 women during middle or late reproductive years leading to significant morbidity. Some of the serious complications associated with UFs include abortion, abnormal foetal formation, obstructed labour, postpartum haemorrhage in pregnancy and premature deliveries in pregnant women whereas heavy and prolonged menstrual bleeding, pelvic pressure, anaemia, urinary incontinence, constipation and infertility were discovered in non-pregnant women. Hormonal irregulation particularly estrogen hormone followed by genetics, epigenetics, environmental factors, and lately gut microbiota have been associated in the pathogenesis of UFs. The most common indication for UFs is hysterectomy, whereas medications available were less effective in most of the cases. There are various review articles that have been published on UFs in the past decade. However, up to date review that comprehends epidemiology, pathogenesis, physiopathology and classifications of UFs is not available Thus, our goal is to explore and scrutinize every aspects within the topic to help provide absolute understanding on UFs. [ABSTRACT FROM AUTHOR]

Green cosmeceuticals are sustainable skincare products formulated using only biodegradable, naturally derived ingredients aiming to improve various skin conditions while concomitantly preserving the environment. Its rising demand is due to its generally better toxicological profiles with appreciable pharmacological effects as compared to synthetic-based cosmeceuticals with frequently reported adverse reactions. The locular gel extracted from the locular cavities of tomatoes (Solanum lycopersicum L.) is an excellent example of a plant-derived ingredient with cosmeceuticals benefits. The partially matured green tomatoes consist of locular gel (GTLG) with numerous bioactive compounds beneficial for skin health may be a potential alternative for chemical active ingredient in the formulation of green cosmeceuticals. This study was undertaken to evaluate the antioxidant and antimicrobial profiles of GTLG and to formulate a green cosmeceutical herbal facial gelcream with claims of being colour-free, sulfide-free, alcohol-free, paraben-free and SLS-free utilizing GTLG as the active ingredient. The extracted GTLG was subjected to in vitro antioxidant assays including 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), antibacterial and antifungal assays. The formulated GTLG-containing facial gel-cream was evaluated for its physicochemical properties (e.g. organoleptic characteristics, pH, spreadability, washability, viscosity) and its stability under freeze-thaw and accelerated conditions. GTLG was found to possess moderate antioxidant capacities at IC50 of 0.6405 ± 0.029mg/mL and 0.061 ± 0.013mg/mL for DPPH and ABTS assay respectively as compared to the positive control, Trolox (IC50(DPPH) = 5.237 ± 0.938µg/mL; IC50(ABTS) = 5.409 ± 0.612µg/mL). Besides, GTLG showed promising antibacterial and antifungal properties against Staphylococcus aureus and Malassezia furfur in agar well diffusion assay with zones of inhibition of 10.33±0.58mm and 16.00mm respectively. The formulation had vanishing cream properties with cosmetically appealing appearance, smooth texture, homogenous without any signs of phase separation, skinfriendly pH, and good spreadability. It possessed non-Newtonian, pseudoplastic behaviour that facilitates topical application. It was stable throughout the freeze-thaw test and under accelerated stability conditions (40 ± 2°C/75 ± 5% RH). GTLG-containing green cosmeceutical facial gel-cream with antioxidant and antimicrobial potential was successfully developed in line with SDG 3 and 12. Further pharmacological and clinical studies would be conducted to warrant them as clinically tested evidence-based formulations. [ABSTRACT FROM AUTHOR]

Acacia auriculiformisplant is widely used in traditional medicines for treatment of various diseases. The main objective of this study is to evaluate the anti-angiogenic effect of ethanolic extract and its phenolic rich fraction of A. auriculiformis bark in the chick embryo chorioallantoic membrane model. Dried powdered bark of A. auriculiformis was extracted with 70% ethanol and the resultant was partitioned with hexane, ethyl acetate and aqueous. Folin- Ciocalteu assay was used to quantify the phenolic content in fractions of A. auriculiformis bark. The anti-angiogenic effect of ethanolic extract and phenolic rich fraction were evaluated by using in-ovo chorioallantoic membrane (CAM) model. The reduction in total blood vessels number in the CAM model was considered as positive indicator of anti-angiogenic effect. Ethyl acetate fraction showed the highest phenolic content which was 621±16.20 mg of gallic acid equivalent per gram of fraction. CAM treated with ethanolic extract (250 µg, 500 µg), ethyl acetate faction (10 µg & 50 µg) and prednisone (250 µg) showed significant reduction (p<0.05) in total blood vessel (TBV) 46.4±0.89, 36.4±2.30, 47.6±3.05, 37.6±1.82 & 37.0±2.00 compared with negative control group (61.7±2.52). The anti-angiogenic effect shown by the ethanolic extract and ethyl acetate fraction of A. auriculiformis might be due to the presence of phenolic compound. A. auriculiformis can be a new source of anti-angiogenic agent in anticancer therapy. [ABSTRACT FROM AUTHOR]

Cancer has been reported to be the 4th most common causes of mortality in Malaysia, in year 2018. Although there are various cancer treatments available, side effects are always be the limitation of these treatments. Various medicinal plants have been studied extensively for their anti-angiogenic activity. Moreover, natural sources are safer and produce lesser side effects. This study aimed to search for alternative cancer treatment from medicinal plant, by examining anti-angiogenic activity of ethanolic extract and its phenolic rich fraction of Filicium decipiens (FD)in the chick embryo chorioallantoic membrane (CAM) assay. The plant extract was prepared by maceration in 70%ethanol andits fractions (hexane, ethyl acetate and aqueous) were prepared from dry ethanolic extract. Total phenolic content (TPC) of the fraction was assayed by using Folin-Ciocalteu method. CAM in-ovo method was used to evaluate the antiangiogenic activity of ethanolic extract of FD bark (250 µg, 500 µg) and its phenolic rich fraction (50 µg, 100 µg). Prednisone (250 µg) was used as positive control. Qualitative observation of reduction in the thickness of blood vessels and quantitative analysis in the reduction of the number of total blood vessels and percentage of blood vessels inhibition were measured to determine the anti-angiogenic activity of the extract and fraction. Ethyl acetate fraction contained the highest total phenolic content (349.59 mg ± 0.29) than aqueous (123.17 mg ± 0.25), hexane (175.31mg ± 0.18) fractions. Ethanolic extract (250µg, 500µg) and ethyl acetate fraction (50µg, 100µg) showed significant reduction (P<0.05) in the total number of blood vessels (43, 14, 46 and 33) compared with negative control (62). Ethanolic extract (250µg and 500µg) and ethyl acetate fraction (50µg and 100µg) showed percentage of blood vessels inhibition of 30.6%, 76.4%, 25.8% and 46.5% respectively. Reduction in the thickness of blood vessels were observed in ethanolic extract (250µg and 500µg) and ethyl acetate fraction (50µg and 100µg).Ethanolic extract and ethyl acetate fraction of FD bark showed antiangiogenic activity that may have chemotherapeutic potentials. [ABSTRACT FROM AUTHOR]

The barks and leaves extracts of Canarium patentinervium Miq. (Burseraceae Kunth.) were investigated for cyclooxygenase (COX) and 5-lipoxygenase (LOX) inhibition via in vitro models. The corresponding antioxidative power of the plant extract was also tested via nonenzyme and enzyme in vitro assays. The ethanolic extract of leaves inhibited the enzymatic activity of 5-LOX, COX-1, and COX-2 with IC50 equal to 49.66 ± 0.02 μg/mL, 0.60 ± 0.01 μg/mL, and 1.07 ± 0.01 μg/mL, respectively, with selective COX-2 activity noted in ethanolic extract of barks with COX-1/COX-2 ratio of 1.22. The ethanol extract of barks confronted oxidation in the ABTS, DPPH, and FRAP assay with EC50 values equal to 0.93 ± 0.01 μg/mL, 2.33 ± 0.02 μg/mL, and 67.00 ± 0.32 μg/mL, respectively, while the ethanol extract of leaves confronted oxidation in β-carotene bleaching assay and superoxide dismutase (SOD) assay with EC50 value of 6.04 ± 0.02 μg/mL and IC50 value of 3.05 ± 0.01 μg/mL. The ethanol extract acts as a dual inhibitor of LOX and COX enzymes with potent antioxidant capacity. The clinical significance of these data is quite clear that they support a role for Canarium patentinervium Miq. (Burseraceae Kunth.) as a source of lead compounds in the management of inflammatory diseases.

Bioassay guided fractionation of an ethanol extract of leaves of Canarium patentinervium Miq. (Burseraceae Kunth.) led to the isolation of scopoletin. The structure of this coumarin was elucidated based on spectroscopic methods including nuclear magnetic resonance (NMR-1D and 2D) and mass spectrometry. Scopoletin inhibited the enzymatic activity of 5-lipoxygenase and acetyl cholinesterase with an IC50 equal to 1.76 ± 0.01  μ M and 0.27 ± 0.02 mM, respectively, and confronted oxidation in the ABTS, DPPH, FRAP, and β -carotene bleaching assay with EC50 values equal to 5.62 ± 0.03  μ M, 0.19 ± 0.01 mM, 0.25 ± 0.03 mM and 0.65 ± 0.07 mM, respectively. Given the aforementioned evidence, it is tempting to speculate that scopoletin represents an exciting scaffold from which to develop leads for treatment of neurodegenerative diseases.