Total Bioactive Contents, Metabolic Profiling, Docking Studies, Antioxidant and Enzyme Inhibition Activities of Convolvulus Arvensis L. and Multivariate Analysis to Unravel a Potential Herb as Natural Resource for Pharmaceutical Industry.

Convolvulus arvensis L. is an evergreen herb growing in various regions of Pakistan. Despite of several medicinal properties associated to this herb, it was not investigated scientifically for its bioactive compounds and detailed pharmaceutical properties. Therefore, its methanolic extract was divided into hexane (CA-H), chloroform (CA-C), ethyl acetate (CA-E) and butanol (CA-B) soluble fractions. CA-H and CA-C were found rich in phenolics (30.73±0.63 and 20.15±0.59 mg GAE/g of the extract, respectively), and the same fractions exhibited significant antioxidant activities (DPPH: 5.23±0.11 & 12.34±0.17 mg TE/g extract, respectively; ABTS: 36.82±0.04 & 56.74±0.61 mg TE/g extract, respectively). Also in CUPRAC activity assay, CA-H and CA-C exhibited highest activities as 87.30±0.46 and 56.74±0.61 mg TE/g extract, respectively, while CA-C was most active in FRAP activity assay with value of 40.21±2.19 mg TE/g extract. Total antioxidant capacity (1.23±0.033 mmol TE/g extract) was also found higher for CA-C, while CA-H activity was also comparable, however, CA-H showed higher metal chelating activity (22.74±0.001 mg EDTAE/g extract) than that of CA-C (17.55±0.22 mg EDTAE/g extract). These activities clearly revealed a direct relation between antioxidant potential and phenolic contents of CA-H and CA-C. In AChE and BChE inhibitory assay, CA-H and CA-E showed better inhibition (AChE: 8.24±0.77 & 4.46±0.007 mg GALAE/g extract; BChE: 5.40±0.02 & 1.92±0.24 mg GALAE/g extract) as compared to other fractions, whereas, against tyrosinase, CA-B was most active (37.35±0.53 mg KAE/g extract). CA-H and CA-C also showed higher inhibitory potential (0.98±0.08 & 0.58±0.01 mmol ACAE/g extract) against α-Amylase; while against α-Glucosidase, CA-E was the most active fraction. UHPLC/MS analysis of the methanolic extract of C. arvensis disclosed the presence of 62 compounds as sterols, triterpenes, flavonoids, fatty acids, alkaloids and coumarins. In Multivariate Analysis, the total phenolic contents were correlated strongly with all antioxidant assays except FRAP and DPPH. Regarding enzyme inhibitory properties, only AChE, BChE and α-amylase were correlated with the total phenolic contents in the extracts. Docking analyses confirmed these findings, as identified compounds had high binding free energy and inhibition constants with the enzymes studied. It was finally concluded that C. arvensis is a potential industrial crop, which can be a component of nutraceuticals and functional foods, if evaluated for its toxicity.

Dereplication and Quantification of Major Compounds of Convolvulus arvensis L. Extracts and Assessment of Their Effect on LPS-Activated J774 Macrophages.

Convolvulus arvensis is used in Pakistani traditional medicine to treat inflammation-related disorders. Its anti-inflammatory potential was evaluated on hexane, dichloromethane, ethyl acetate, methanol, and aqueous extracts of whole plant on pro-inflammatory mediators in LPS-activated murine macrophage J774 cells at the non-cytotoxic concentration of 50 µg/mL. Ethyl acetate (ARE) and methanol (ARM) extracts significantly decreased mRNA levels of IL-6, TNF-α, MCP-1, COX-2, and iNOS. Furthermore, both extracts dose dependently decreased IL-6, TNF-α, and MCP-1 secretion. Forty-five compounds were putatively identified in ARE and ARM by dereplication (using HPLC-UV-HRMSn analysis and molecular networking), most of them are reported for the first time in C. arvensis, as for example, nineteen phenolic derivatives. Rutin, kaempferol-3-O-rutinoside, chlorogenic acid, 3,5-di-O-caffeoylquinic acid, N-trans-p-coumaroyl-tyramine, and N-trans-feruloyl-tyramine were main constituents identified and quantified by HPLC-PDA in ARE and ARM. Furthermore, chlorogenic acid, tyramine derivatives, and the mixture of the six identified major compounds significantly decreased IL-6 secretion by LPS-activated J774 cells. The activity of N-trans-p-coumaroyl-tyramine is shown here for the first time. Our results indicate that ARE, ARM and major constituents significantly inhibited the expression of pro-inflammatory mediators, which supports the use of this plant to treat inflammatory diseases.

Neuroprotective effect of Convolvulus pluricaulis Choisy in oxidative stress model of cerebral ischemia reperfusion injury and assessment of MAP2 in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Convolvulus pluricaulis Choisy commonly known as Shankhapushpi, is traditionally prescribed for nerve debility, loss of memory, epilepsy and as nervine tonic. Plant also proved to have diverse pharmacological activity but the neuroprotection in ischemic stroke were not found. AIM OF THE STUDY: To investigate the effect of Convolvulus pluricaulis against bilateral common carotid artery (BCCA) occlusion induced cerebral ischemic reperfusion injury. MATERIALS AND METHODS: The neuroprotective activity of Convolvulus pluricaulis against bilateral common carotid artery (BCCA) occlusion induced cerebral ischemic reperfusion (I/S) injury. Sprague-Dawley rats of either sex (200-250 g) were divided into nine groups of 8 rats each. Sham and control group, saline treated 10 ml/kg orally. Third group treated with Quercetin 25 mg/kg orally and fourth to ninth groups treated with chloroform and ethanol extract of Convolvulus pluricaulis 100, 200, and 400 mg/kg (p.o.) respectively. Control, Quercetin and extract treated groups underwent 30 min BCCA occlusion and 24 h reperfusion on 10th day but sham underwent same surgery without BCCA occlusion and 24 h reperfusion on 10th day. The antioxidant enzymatic and non-enzymatic levels were estimated by UV spectroscopic method and cerebral infarction area, Blood brain barrier disruption, microtubule-associated protein 2 immunohistochemical and histopathological studies were carried out. RESULTS: The results of the study indicate that the chloroform and ethanol extract of Convolvulus pluricaulis showed neuroprotective activity by a significant decrease in lipid peroxidation (p < 0.001) and an increase in superoxide dismutase (p < 0.01, p < 0.001), catalase (p < 0.01, p < 0.001), glutathione (p < 0.001), and total thiol (p < 0.001) levels in extract-treated groups as compared to control group. Measurement of cerebral infarction area, blood brain barrier disruption, microtubule-associated protein 2 immunohistochemical and histopathological studies further supported the protective effect of the extract. CONCLUSIONS: Present study revile that Convolvulus pluricaulis has potent neuroprotection against bilateral common carotid artery (BCCA) occlusion induced cerebral ischemic reperfusion injury.

ISSR fingerprinting for the assessment of the bindweed biocontrol agent Stagonospora convolvuli LA39 after field release.

AIMS: To develop a molecular identification method based on ISSR fingerprints to monitor the fungal leaf pathogen Stagonospora convolvuli LA39 used to biologically control bindweeds after a field release. METHODS AND RESULTS: The developed method proved to be suitable to clearly distinguish LA39 from resident Stagonospora spp. and was applied in two field experiments. First, the environmental persistence of LA39 was assessed in an overwintering experiment. LA39 could be re-isolated from infected bindweed 1 year after field application, but with very low frequency of occurrence. Secondly, LA39 was applied in an area with natural bindweed infestation and re-isolated from infected bindweed. The dispersal of LA39 during one season was poor (4-5 m). CONCLUSIONS: ISSR fingerprinting has been shown to be a valuable tool to monitor the environmental fate of S. convolvuli in the field. It is concluded that an LA39-based mycoherbicide will have minimal environmental impact caused by the restricted mobility, poor proliferation and poor persistence over seasons of LA39. SIGNIFICANCE AND IMPACT OF THE STUDY: Studies about the dispersal and survival of biocontrol agents after field release as well as the development of methods needed for this purpose are indispensable for a comprehensive risk assessment for biocontrol agents.