Plants have served either as a natural templates for the development of new chemicals or a phytomedicine since antiquity. Therefore, the present study was aimed to appraise the polarity directed antioxidant, cytotoxic, protein kinase inhibitory, antileishmanial and glucose modulatory attributes of a Himalayan medicinal plant- Quercus dilatata. Total phenolic and flavonoid contents were determined colorimetrically and various polyphenols were identified by RP-HPLC analysis. Brine shrimp lethality, SRB and MTT assays were employed to test cytotoxicity against Artemia salina and human cancer cell lines respectively. Antileishmanial activity was determined using standard MTT protocol. Glucose modulation was assessed by α-amylase inhibition assay while disc diffusion assay was used to establish protein kinase inhibitory and antifungal spectrum. Among 14 extracts of aerial parts, distilled water-acetone extract demonstrated maximum extract recovery (10.52% w/w), phenolic content (21.37 ± 0.21 μg GAE/mg dry weight (DW)), total antioxidant capacity (4.81 ± 0.98 μg AAE/mg DW) and reducing power potential (20.03 ± 2.4 μg/mg DW). On the other hand, Distilled water extract proficiently extracted flavonoid content (4.78 ± 0.51 μg QE/mg DW). RP-HPLC analysis revealed the presence of significant amounts of phenolic metabolites (0.049 to 15.336 μg/mg extract) including, pyrocatechol, gallic acid, catechin, chlorogenic acid, p-coumaric acid, ferulic acid and quercetin. Highest free radical scavenging capacity was found in Methanol-Ethyl acetate extract (IC50 8.1 ± 0.5 μg/ml). In the brine shrimp toxicity assay, most of the tested extracts (57%) showed high cytotoxicity. Among these, Chloroform-Methanol extract had highest cytotoxicity against THP-1 cell line (IC50 3.88 ± 0.53 μg/ml). About 50% of the extracts were found to be moderately antiproliferative against Hep G2 cell line. Methanol extract exhibited considerable protein kinase inhibitory activity against Streptomyces 85E strain (28 ± 0.35 mm bald phenotype at 100 μg/disc; MIC = 12.5 μg/ disc) while, Chloroform extract displayed maximum antidiabetic activity (α-amylase inhibition of 21.61 ± 1.53% at 200 μg/ml concentration). The highest antileishmanial potential was found in Ethyl acetate-Acetone extract (12.91 ± 0.02% at 100 μg/ml concentration), while, Q. dilatata extracts also showed a moderate antifungal activity. This study proposes that multiple-solvent system is a crucial variable to elucidate pharmacological potential of Q. dilatata and the results of the present findings prospects its potential as a resource for the discovery of novel anticancer, antidiabetic, antileishmanial and antioxidant agents.

The concept of botanical therapeutics has revitalized due to wide importance of plant derived pharmaceuticals. Therefore, the ameliorative characteristics of Ajuga bracteosa were studied. Total phenolic content, flavonoid content, antioxidant capacity, reducing power and free-radical scavenging activity were determined colorimetrically. Specific polyphenols were quantified by RP-HPLC analysis. Preliminary cytotoxicity was tested using brine shrimp lethality assay while antiproliferative activity against THP-1 and Hep-G2 cell lines was determined by MTT and SRB protocols respectively. Antileishmanial potential was assessed via MTT colorimetric method. To investigate antidiabetic prospect, α-amylase inhibition assay was adopted whereas disc diffusion method was used to detect likely protein kinase inhibitory, antibacterial and antifungal activities. Among fifteen different extracts, maximum total phenolic content (10.75 ± 0.70 μg GAE/mg DW), total reducing power (23.90 ± 0.70 μg AAE/mg DW) and total antioxidant capacity (11.30 ± 0.80 μg AAE/mg DW) were exhibited by methanol extract with superlative percent extract recovery (17.50 ± 0.80% w/w). Chloroform-methanol extract demonstrated maximum flavonoid content (4.10 ± 0.40 μg QE/mg DW) and ethanol extract exhibited greatest radical scavenging activity (IC50 14.40 ± 0.20 μg/ml). RP-HPLC based quantification confirmed polyphenols such as pyrocatechol, gallic acid, resorcinol, catechin, chlorogenic acid, caffeic acid, syringic acid, p-coumaric acid, ferulic acid, vanillic acid, coumarin, sinapinic acid, trans-cinnamic acid, rutin, quercetin and kaempferol. The brine shrimp lethality assay ranked 78.60% extracts as cytotoxic (LC50 ≤ 250 μg/ml) whereas significant THP-1 inhibition was shown by methanol-acetone extract (IC50 4.70 ± 0.43 μg/ml). The antiproliferative activity against Hep-G2 hepatoma cancer cell line was demonstrated by n-hexane, ethylacetate and methanol-distilled water (IC50 8.65–8.95 μg/ml) extracts. Methanol extract displayed prominent protein kinase inhibitory activity (MIC 12.5 μg/disc) while n-hexane extract revealed remarkable antileishmanial activity (IC50 4.69 ± 0.01 μg/ml). The antidiabetic potential was confirmed by n-hexane extract (44.70 ± 0.30% α-amylase inhibition at 200 μg/ml concentration) while a moderate antibacterial and antifungal activities were unveiled. The variation in biological spectrum resulted due to use of multiple solvent systems for extraction. We also deduce that the valuable information gathered can be utilized for discovery of anticancer, antileishmanial, antioxidant and antidiabetic bioactive lead candidates.

Purpose: Jatrorrhizine (JAT) is a natural protoberberine alkaloid, possesses detoxification, bactericidal and hypoglycemic activities. However, its anti-cancer mechanism is not clear. This study aimed to investigate the mechanism of JAT through which inhibits colorectal cancer in HCT-116 and HT-29 cells. Methods: MTT assay and colony formation assay were used to check the cell proliferation ability. Cell apoptosis and cell cycle were measured by Hoechst 33342 staining and flow cytometry, respectively. Cell migration and invasion were detected by scratch wound healing assay and trans-well assay, respectively. Further, expression of related proteins was examined via Western blotting and the in vivo anti-cancer effect of JAT was confirmed by nude mice xenograft model. Results: The research showed that JAT inhibited the proliferation of HCT-116 and HT-29 cells with IC₅₀ values of 6.75±0.29 μM and 5.29±0.13 μM, respectively, for 72 hrs. It has also showed a time dependently, cell cycle arrested in S phase, promoted cell apoptosis and suppressed cell migration and invasion. In addition, JAT inhibited Wnt signaling pathway by reducing β-catenin and increasing GSK-3β expressions. Increased expression of E-cadherin, while decreased N-cadherin, indicating that JAT treatment suppressed the process of cell epithelial–mesenchymal transition (EMT). In HCT-116 nude mice xenograft model, JAT inhibited tumor growth and metastasis, and induced apoptosis of tumor cells. Conclusion: This study demonstrated that JAT efficiently inhibited colorectal cancer cells growth and metastasis, which provides a new point for clinical treatment of colorectal cancer.

Medicinal plants are rich sources of bioactive phytochemicals. Production of such chemicals usually increased under unfavorable conditions. This study investigated the phytotoxic potential of 105 medicinal plants distributed in arid/semiarid areas along Arabian Sea coast of Pakistan. Total polyphenols, flavonoids, tannins and composition of individual phenolic compounds were also determined in species which showed high phytotoxic potential. Sandwich method was used to determine the phytotoxicity of medicinal plants on the growth of lettuce seedlings. Radicle growth was inhibited more than the hypocotyl growth. In general, halophytes showed higher phytotoxic potential than non-halophytes. Capparis cartilaginea, Indigofera hochstetteri, Parkinsonia aculeata and Prosopis glandulosa showed highest degree of inhibition. Higher amount of total phenols (16.35–25.33 mg GAE g⁻¹), flavonoids (3.32-6.41 mg QE g⁻¹) and tannins (1.54–2.54 mg TAE g⁻¹) were found in these species. Pyrocatechol, quercetin, gallic, hydroxybenzoic and ferulic acids were detected as major phytotoxins, of which, gallic acid, pyrocatechol and quercetin were most abundant. These phytochemicals could be used for the production of natural, safe, healthy and eco-friendly agro-chemicals. Furthermore, these plants can be grown without encroaching agricultural lands, and can convert vast areas of arid/saline lands into economically viable resources, which also helps to halt climate change and desertification.

Phenolic compounds are very effective for the cure of various neurological and pathological diseases. Current study was conducted to estimate the Phenolic compounds through HPLC and to perform the anti-Alzheimer activity from two aquatic Leptosporangiate ferns; Marsilea quadrifolia L. and Salvinia molesta D. Crushed leaves were subjected to Microwave Assisted Extraction to prepare plant leave ethanolic extract of plants under study. Aluminum chloride induced Alzheimer’s disease model in rats by estimating behavioural and biochemical parameters were measured for ethanolic extract of both plants. Different behavioural tests were performed for neuromuscular coordination estimation and hole board test for exploratory behaviour were performed. The levels of AChE inhibitory activity and antioxidant enzymes were estimated on brain homogenates and Histopathological analysis were also performed. Phenolic compounds of leaf extracts were noted for HPLC chromatograms of standard compounds with Gallic acid (33.76 ± 0.08) higher in M. quadrifolia L. and Salicylic acid (12.45 ± 0.07) higher in S. molesta D. S Mitchel. Histopathological analysis showed that M. quadrifolia and S. molesta reversed the neurofibrillary tangles, degenerative changes, neuronal loss and neuroinflammation in the brain architecture. Both ferns at a dose of 500 mg/kg and 1000mg/kg significantly improved the Aluminium chloride induced neurotoxicity by modulating cognitive disabilities and motor dysfunctions, and normalized the biochemical alteration of acetylcholinesterase and antioxidant enzymes. In conclusion, both plants M. quadrifolia and S. molesta improved behavioural and biochemical parameters and therefore will be effective in treatment of neurodegenerative disorders via countless underlying mechanistic pathways.