Search

Abstract The increasing emergence and dissemination of multidrug resistant (MDR) bacterial pathogens accelerate the desires for new antibiotics. Natural products dominate the preferred chemical scaffolds for the discovery of antibacterial agents. Here, the potential of natural flavonoids from plants against MDR bacteria, is demonstrated. Structure–activity relationship analysis shows the prenylation modulates the activity of flavonoids and obtains two compounds, α‐mangostin (AMG) and isobavachalcone (IBC). AMG and IBC not only display rapid bactericidal activity against Gram‐positive bacteria, but also restore the susceptibility of colistin against Gram‐negative pathogens. Mechanistic studies generally show such compounds bind to the phospholipids of bacterial membrane, and result in the dissipation of proton motive force and metabolic perturbations, through distinctive modes of action. The efficacy of AMG and IBC in four models associated with infection or contamination, is demonstrated. These results suggest that natural products of plants may be a promising and underappreciated reservoir to circumvent the existing antibiotic resistance.

Berberine-rich extract (BRE) prepared from Berberis lycium root bark using green extraction approach and its marker compound berberine has a broad spectrum of clinical applications. Berberine's potential pharmacological effects include anticancer, antidiarrheal, antidiabetic, antimicrobial and anti-inflammatory activities. In current work, BRE and berberine were evaluated for their therapeutic prospects in inflammation models. The comparative effect of BRE and berberine against inflammation was determined through in vitro chemiluminescence technique. The in vivo anti-inflammatory evaluation of BRE and berberine (25, 75, and 125 mg/kg) compared to diclofenac (10 mg/kg) was performed in carrageenan and formaldehyde-induced inflammation in Wistar rats. Histopathological and biochemical studies were conducted to find the comparative anti-inflammatory potential of BRE and berberine on pathological hallmarks induced by formaldehyde. Moreover, the modulatory effects on inflammatory biomarkers were also investigated through qPCR. ELISA (enzyme-linked immunoassay test assay) was performed to investigate the expression of pathological protein biomarkers like TNF-α and IL-6 and levels of antioxidant enzymes were estimated in liver homogenates. Both BRE and berberine markedly (p < .001) reduced paw diameter and inflammation in carrageenan and formaldehyde-induced inflammation. The levels of antioxidant enzymes were recovered (p < .001) by BRE and berberine treatments, and compared to the formaldehyde-treated inflammation model. Both BRE and berberine remarkably downregulated the mRNA and protein expression of inflammatory biomarkers. BRE similar to berberine mitigated the level of antioxidant enzymes in liver homogenate. The undertaken study suggests that BRE, a natural, green, and therapeutically bioequivalent to berberine could be used as an economical phytomedicine in the treatment of inflammatory disorders. PRACTICAL APPLICATIONS: Anti-inflammatory drugs like NSAIDS are associated with serious adverse effects like gastrointestinal ulcer, worsening of preexisting cardiovascular disorders, and renal failure. Therefore, there is a constant demand to develop novel, inexpensive therapeutic strategies to treat the inflammatory disorder with the least harmful effects. Pure phytochemicals with anti-inflammatory potential are costly and hard to isolate, therefore green microwave-assisted extraction technique is developed to get the rich bioequivalent extract. Berberis lycium a medicinal plant with berberine as a major bioactive constituent, has wide acceptance in traditionally used medicine and as food. Pharmacological studies revealed its hepatoprotective, anticancer, antidiabetic, and antihypertensive activities. BRE was prepared by green microwave-assisted extraction and enrichment by resin column to get a higher yield of berberine. The comparative anti-inflammatory effect of BRE and berberine was determined by in vitro and in vivo studies. Results obtained from this experimental work contribute beneficial guidance that reinforces the use of the BRE to treat inflammatory disorders., (© 2022 Wiley Periodicals LLC.)

This study aimed to appraise the anti-Parkinson's potential of rhinacanthin-C (RC). RC (5, 10, and 20 mg/kg) was orally administered for 25 days in albino mice to treat haloperidol-induced parkinsonism (1 mg/kg). RC significantly (p < .05) improved the motor symptoms in block, bar, rotarod, and balance beam walking tests in treated mice. RC reduced the cataleptic effect dose-dependently. The RC therapy notably (p < .001) enhanced reduced glutathione, catalase, and superoxide dismutase levels while decreased malondialdehyde and nitrite levels in the tissue homogenates of the treated mice. The RC therapy significantly (p < .01-.001) restored the dopamine, norepinephrine, and serotonin levels in the brain tissue of treated mice as co-evidenced from brain histology. RC did not adversely affect complete blood count, and liver and kidney function tests. Taken together, these results have shown that RC is effective in treating motor and non-motor symptoms of Parkinson's disease. PRACTICAL APPLICATIONS: Rhinacanthus nasutus is a medicinally rich plant that has folklore use in several ailments. The plant possessed multiple pharmacological activities due to the presence of naphthoquinones. The major compound of this plant rhinacanthin-C was used in the present study to evaluate it's anti-Parkinson's activity. The results provide scientific evidence of the anti-Parkinson's potential of rhinacanthin-C that support the use of R. nasutus leaves in the prevention and treatment of Parkinson's disorder., (© 2021 Wiley Periodicals LLC.)

In this present study, rhinacanthins-rich extract (RRE) and rhinacanthin C (RC) the main bioactive constituent of Rhinacanthus nasutus was investigated for their protective effect against diabetic nephropathy (DN). Diabetes was induced by administering nicotinamide (100 mg/kg, i.p.)/streptozotocin (60 mg/kg, i.p.) and diabetic rats were orally administered with RRE and RC for 4 weeks. RRE and RC significantly reduced the kidney index, renal oxidative stress markers, and pro-inflammatory cytokines. Furthermore, RRE and RC increased renal levels of glutathione, superoxide dismutase, catalase, and attenuated diabetic induced renal damages. In conclusion, RRE and RC confer protective effect against DN through the inhibition of oxidative stress and inflammation and could be a potential medicinal or nutritional supplement for the prevention of DN. PRACTICAL APPLICATIONS: Rhinacanthus nasutus is a medicinal plant that is extensively used in Thai traditional medicine as an antibacterial, antifungal, antidiabetic, and anti-inflammatory agent. The plant is rich in naphthoquinones, which confer it with several excellent bioactivities. The rich extract of the leaves was prepared with three major bioactive components and the extract was evaluated for its renoprotective effect in diabetic rats. The results from this study provides valuable pharmacological information that supports the use of the plant, especially the rich extract in the prevention and treatment of diabetes and diabetic complications., (© 2019 Wiley Periodicals, Inc.)

The present study evaluated the topical anti-inflammatory potential of a standardized pomegranate rind extracts (SPRE) in parallel with its marker compound ellagic acid (EA, 13% w/w) against a mouse model of contact dermatitis. In the phenol-induced mouse ear edema, topical application of SPRE (5, 2.5, and 1 mg/ear) and EA (0.65, 0.325, and 0.13 mg/ear, equivalent to its content in SPRE) dose-dependently reduced the ear edema with the maximal inhibition of 79.12% and 73.63%, respectively. Triamcinolone (0.1 mg/ear) and diclofenac (1 mg/ear) as reference drugs inhibited the edema by 73.63% and 37.91%. Myeloperoxidase (MPO) activity in the mouse ear was also decreased by SPRE and EA up to 69.68% and 68.79%, respectively. Triamcinolone and diclofenac decreased the MPO activity by 76.66% and 80.14% similarly. The results indicated that topical application of SPRE and EA is promising for use in the treatment of inflammatory skin disorders., (Copyright © 2013 John Wiley & Sons, Ltd.)

Four phenylbutanoids, (E)-4-(3,4-dimethoxyphenyl)but-3-en-l-ol (I), (E)-4-(3,4-dimethoxyphenyl)but-3-en-l-yl acetate (II), (E)-1-(3,4-dimethoxyphenyl)butadiene (III) and (E)-3-(3,4-dimethoxyphenyl)-4-[(E)-3,4-dimethoxystyryl]cyclohex-1-ene (IV), isolated from Zingiber cassumunar, were used as standard markers for quantitative determination and preparation of phenylbutanoid-enriched Z. cassumunar extracts (PZEs). A reversed-phase HPLC method was established for the simultaneous determination of the phenylbutanoids in Z. cassumunar extracts. Systematic extraction studies to maximize phenylbutanoid content revealed that hexane was the most appropriate solvent for extraction. A one-step purification of the hexane crude extract of Z. cassumunar, using silica gel vacuum chromatography, provided the PZEs. The content of phenylbutanoids in the PZEs was up to 48.3% w/w dry weight. The anti-inflammatory activity of PZEs via inhibition of nitric oxide production by murine macrophage-like RAW264.7 cells was stronger than those of the four individual phenylbutanoids, the crude hexane extract and the essential oil of Z. cassumunar., (Copyright © 2012 John Wiley & Sons, Ltd.)

Introduction: Naphthoquinones; lawsone (1), lawsone methyl ether (2) and methylene-3,3'-bilawsone (3) are the main active compounds of Impatiens balsamina leaves., Objective: To develop and validate an HPLC method for simultaneous quantitative determination of 1-3 in I. balsamina leaf extracts., Methodology: The method utilised a Supelco® C(18) column (5 µm, 4.6 × 150 mm) at 25°C with the mixture of 2% aqueous acetic acid : methanol (gradient elution as follows: 0-10 min, 25 : 75; 10-20 min, 32 : 68; 20-35 min, 55 : 45) as the mobile phase at a flow-rate of 1 mL/min, and UV detection at 280 nm. The parameters of linearity, repeatability, reproducibility, accuracy specificity and sensitivity of the method were evaluated., Results: The recovery of the method was 96-101% and linearity (r(2) ≥ 0.9995) was obtained for all naphthoquinones. A high degree of specificity, as well as repeatability and reproducibility (RSD less than 5%), were also achieved., (Copyright © 2010 John Wiley & Sons, Ltd.)