RESUMEN

The formation of advanced glycation end product (AGE) is a risk factor for diabetic retinopathy. Since the current treatment for diabetic retinopathy is accompanied by side effects, preliminary findings have suggested Peperomia pellucida (L.) Kunth as a potential alternative therapeutic option for diabetic retinopathy. This study aimed to elucidate the anti-inflammatory mechanism of P. pellucida in the AGE-stimulated human retinal pigment epithelial cell line ARPE-19. Phytochemical analysis revealed phenylpronanoids, terpenes, and fatty acids in P. pellucida. Through in vitro cell viability assay, the P. pellucida methanolic extract (IC50 = 8.70 mg/mL) and ethyl acetate fraction (IC50 = 7.34 mg/mL) were considered as non toxic for ARPE-19. AGE induced an inflammatory response in ARPE-19 by upregulating the gene (2.4-5.8-fold) and protein (1.4-2.3-fold) expression of signal transducer and activator of transcription 3 (STAT3), interleukin-8 (IL-8), monocyte chemoattractant protein-1, matrix metalloproteinase 2, and vascular endothelial growth factor. At 1.5 mg/mL, P. pellucida methanolic extract suppressed IL-8 expression (p < 0.05), implying its anti-inflammatory action at the early inflammatory stage through the Janus kinase (JAK)-STAT3 pathway. The methanolic extract also restored the ARPE-19 viability under AGE-induced inflammatory stress. The downregulation of inflammatory biomarkers along the JAK-STAT3 pathway suggested P. pellucida as a promising anti-inflammatory source for diabetic retinopathy.

RESUMEN

The extraction of plant bioactive compounds from Platycladus orientalis (L.) Franco remains a great challenge due to the different chemical groups. This study aimed to compare the bioactive compounds with enzyme inhibitory effect from P. orientalis via solvent partitioning method. Dried leaf samples were macerated and fractionated with six solvents of different polarities. The phenolic, flavonoid, tannin, saponin, alkaloid and pharmacological activities including anti-inflammatory, anti-diabetic, antioxidant and anti-glycation potential were compared across the six plant fractions. Toxicity assessment was performed with an in vivo brine shrimp model. The varying levels of bioactive compounds in ethyl acetate (phenolics, flavonoids), hexane (saponins, tannins) and chloroform (alkaloids) fractions clearly demonstrated the significant impact of solvent polarity on the extraction of bioactive compounds. The reducing potential (r = 0.67), IC50 of α-amylase inhibition (r = -0.71), IC50 of advanced glycation end-product inhibition (r = -0.93) and dicarbonyl compound inhibition (r = 0.57) in the plant fractions were correlated (p<0.05) with the flavonoids. Besides, the alkaloid, saponin and tannin were associated with cyclooxygenase-1 inhibitory activity. Principal component analysis confirmed that solvent polarity (23.9%) and plant extraction yield (37.1%) collectively contributed to 61% of bioactivity variation in P. orientalis. Among the six plant fractions, ethyl acetate fraction exhibited relatively high anti-inflammatory, anti-diabetic, antioxidant and anti-glycation potential while the non-toxic methanolic and aqueous fractions displayed optimal hyaluronidase and lipoxygenase inhibitory activities, respectively. The current study has identified semi-polar ethyl acetate fraction of P. orientalis as a good alternative source of bioactive compounds for future pharmaceutical product development.

Asunto(s)

RESUMEN

Peperomia pellucida (L.) Kunth is a medicinal plant used to manage inflammatory illnesses such as conjunctivitis, and gastrointestinal and respiratory tract disorders in tropical and subtropical regions. However, little is known about its pharmacological mechanism of action against eye diseases. This review aims to critically discuss the phytochemistry, pharmacology and toxicology of P. pellucida as well as its roles in the treatment of cataract, glaucoma and diabetic retinopathy. Recent developments in the uses of P. pellucida for healthcare and nutraceutical products by the pharmaceutical industry are also covered in this review. For this review, a literature search was performed with PubMed, ScienceDirect, SciFinder Scholar and Scopus databases, using relevant keywords. Among the various phytochemicals identified from P. pellucida, ß-caryophyllene, carotol, dillapiole, ellagic acid, pellucidin A, phytol and vitexin exhibit strong pharmacological activities within the mitogen-activated protein kinase and nuclear factor-κB signalling pathways in inflammatory eye diseases. The antihypertensive, anti-inflammatory, antioxidant, antihyperglycemic and anti-angiogenic activities displayed by P. pellucida extracts in many in vitro, in vivo and clinical studies suggest its potential role in the management of inflammatory eye diseases. P. pellucida extract was non-toxic against normal cell lines but displayed mild toxicity in animal models. The growing public interest in P. pellucida has inspired the nutraceutical and pharmaceutical industries to process the plant into health products. Although the potential pharmacological mechanisms against eye diseases have been summarized, further studies of the interactions among constituent phytochemicals from P. pellucida within various signalling pathways shall support the use of the plant as an alternative therapeutic source.

Asunto(s)