Background: The purpose of the current study is to identify the phytochemicals as well as to determine the level of antioxidant, cytotoxic, antimicrobial and in vivo analgesic, anti-inflammatory and antidiarrheal activity of leaf methanolic extract of Colocasia affinis Schott (LMCA). Methods: To appraise the antioxidant activities the extensively used total phenol, flavonoid, total antioxidant capacity, ferric reducing antioxidant power, cupric reducing antioxidant capacity and DPPH scavenging assay have been used. Cytotoxic potential was determined by brine shrimp lethality test whereas antimicrobial activity was assessed by disc diffusion method. Acetic acid induced writhing and formalin induced paw licking methods were employed to evaluate analgesic activity. To gauge anti-inflammatory activity, xylene-induced ear edema and carrageenan induced paw edema methods were used. Castor oil induced diarrhea and magnesium sulfate induced enteropooling methods were used to figure out antidiarrheal activity evaluation. Results: Phytochemical screening affirmed the presence of alkaloids, flavonoids and tannins in the extract. LMCA contains marked amount of total phenol (3.89 ± 2.36 mg/g), total flavonoid (905.50 ± 2.12 mg/g) and total antioxidant (245.83 ± 2.36 mg/g). Remarkable cupric reducing power and ferric reducing power capability were observed. In DPPH radical scavenging assay, the extract showed moderate scavenging potential (IC 50 395.97 μg/ml), whereas IC 50 value of standard ascorbic acid was 32.75 μg /ml. The extract showed a significant result in cytotoxicity test. In disk diffusion antimicrobial assay LMCA manifested broad spectrum of activity. In acetic acid induced writhing test, the highest dose (1000 mg/kg) showed 57.69% inhibition of abdominal constrictions compared to Diclofenac Sodium (74.62%). In case of formalin induced analgesic activity test the extract exhibited preeminent effect (LMCA 1000 mg/kg showed 58.64% inhibition). The extract inhibited 86.36% xylene induced ear edema (at dose 1000 mg/kg) where Aspirin inhibited 88.81%. In carrageenan induced test LMCA 1000 mg/kg manifested eloquent inhibition of inflammation at 6th hour (50.59%). The highest dose 1000 mg/kg of LMCA showed significant (80.95%) reduction in diarrhea and noticeable reduction of intestinal fluid secretion (24.29%). Conclusion: To recapitulate, it is suggested that the leaf of Colocasia affinis Schott might be a potential source of useful bioactive molecules.

Background:The greatest disadvantage in the presently available potent synthetic anti-inflammatory drugs lies in their toxicity and reappearance of symptoms after discontinuation. Hence, people are returning to the natural products with the hope of safety and security. Several species of Mikania have been reported to have anti-inflammatory properties.Aim:The present study aims to assess the anti-inflammatory activity of the ethanolic extract of the leaves and stem of Mikania scandens in vivo and in vitro.Materials and Methods:The in vitro bioassay consisted of assaying the effect of the extracts against denaturation of protein (egg albumin) and measuring the absorbance. In vivo anti-inflammatory activity was checked by measuring the percentage inhibition of carrageenan-induced rat paw edema after oral administration of the extracts to male Wistar rats.Results:The plant extracts revealed the presence of tannins, alkaloids, steroids and flavonoids in both the leaf and stem extracts. The in vitro study of leaf extracts of M. scandens demonstrated that at 16000 μg/ml concentration a better anti-inflammatory activity was exhibited which is more than the stem extracts. Similarly in the in vivo study, carrageenan induced inflammation was significantly antagonized by M. scandens leaf extract, with inhibition of 50% at 1000 mg/kg.Conclusion:The ethanolic extract of both leaf and stem of M. scandens showed potent anti-inflammatory activity. In comparison the leaf extract found to be more potent in both the conditions in vivo and in vitro, comparing with the standard drug diclofenac sodium and traditional control rumalaya perhaps due to the presence of phytochemicals like alkaloids and flavonoids in the plant.

A series of 30 non-covalent imidazo[1,2-a]quinoxaline-based inhibitors of epidermal growth factor receptor (EGFR) were designed and synthesized. EGFR inhibitory assessment (against wild type) data of compounds revealed 6b, 7h, 7j, 9a and 9c as potent EGFRWT inhibitors with IC50 values of 211.22, 222.21, 193.18, 223.32 and 221.53 nM, respectively, which were comparable to erlotinib (221.03 nM), a positive control. Furthermore, compounds exhibited excellent antiproliferative activity when tested against cancer cell lines harboring EGFRWT; A549, a non-small cell lung cancer (NSCLC), HCT-116 (colon), MDA-MB-231 (breast) and gefitinib-resistant NSCLC cell line H1975 harboring EGFRL858R/T790M. In particular, compound 6b demonstrated significant inhibitory potential against gefitinib-resistant H1975 cells (IC50 = 3.65 μM) as compared to gefitinib (IC50 > 20 μM). Moreover, molecular docking disclosed the binding mode of the 6b to the domain of EGFR (wild type and mutant type), indicating the basis of inhibition. Furthermore, its effects on redox modulation, mitochondrial membrane potential, cell cycle analysis and cell death mode in A549 lung cancer cells were also reported.

Ponicidin, an ent-kaurane diterpenoid derived from Rabdosia rubescens, exhibits antitumor activities against several types of cancers. This review summarizes the botanical sources, biological activities, and biopharmaceutical profile of ponicidin. Additionally, a molecular docking study has been undertaken to correlate the interaction of this diterpenoid with biomacromolecules found in the literature. For this purpose, an up-to-date (till December 2018) literature survey was conducted using a number of databases such as PubMed, Science Direct, Web of Science, Scopus, the American Chemical Society, Clinicaltrials.gov, and Google Scholar. Findings suggest that ponicidin exerts antioxidant and anticancer activity in various test systems, including experimental animals and cultured cancer cells. Research findings revealed that anticancer mechanisms of ponicidin include antioxidant/oxidative stress induction, cytotoxic, apoptotic inductive, chemosensitizer, antiangiogenic, and antiproliferative effects. In silico study suggests that 5ITD (PI3K) was the best protein with which ponicidin interacts to exert its anticancer effect. In conclusion, ponicidin might be a promising plant-derived cancer chemotherapeutic agent.Abbreviations: Akt, protein kinase B; GSK-3β, glycogen synthase kinase 3 beta; MEK/MAPK, mitogen-activated protein kinase; NF-κB, nuclear factor kappa light chain enhancer of activated B cells; PARP, poly-ADP ribose polymerase; PI3K, phosphoinositide 3-kinases; STAT3, signal transducers and activators of transcription 3; TNFα, tumor necrosis factor alpha; γ H2AX, gamma-H2A histone family member X. .

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