This review aims to summarize the anticancer effects of the natural monoterpene phenol derivative of cymenethymol and its derivatives as well as further molecular docking study to correlate the interaction of thymol and biomacromolecules that involved in cancer cell growth. For this, an up‐to‐date (till July 2018) literature study were made through using PubMed, Science Direct, Web of Science, Scopus, The American Chemical Society, http://clinicaltrials.gov, and Google Scholar databases. Literature study demonstrated that thymol, melasolv (3,4,5‐Trimethoxycinnamate thymol ester), and Mannich bases of thymol have potential anticancer effects in various test systems, including mice, rats and cultured cancer cells through various anticancer pathways such as antioxidant/oxidative stress induction, apoptosis, anti‐inflammatory/immunomodulatory, anti‐genotoxicity, chemo‐, and radiopreventive ways. A few earlier scientific evidences showed that thymol is less toxic to mammalian systems. In silico study of thymol and its derivatives against 17 essential proteins revealed that 6BVH (PARP‐1) and 5LIH (protein kinase C) are the most efficient receptor protein for interaction and binding of thymol and melaslov for the cancer prevention and initiation. On the basis of the summary of this review and docking study, it is evident that thymol may be one of promising plant‐derived cancer chemotherapeutic agents. © 2018 IUBMB Life, 71(1):9–19, 2019

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.

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Dengue fever is a dangerous infectious endemic disease that affects over 100 nations worldwide, from Africa to the Western Pacific, and is caused by the dengue virus, which is transmitted to humans by an insect bite of Aedes aegypti. Millions of citizens have died as a result of dengue fever and dengue hemorrhagic fever across the globe. Envelope (E), serine protease (NS3), RNA-directed RNA polymerase (NS5), and non-structural protein 1 (NS1) are mostly required for cell proliferation and survival. Some of the diterpenoids and their derivatives produced by nature possess anti-dengue viral properties. The goal of the computational study was to scrutinize the effectiveness of diterpenoids and their derivatives against dengue viral proteins through in silico study. Methods: molecular docking was performed to analyze the binding affinity of compounds against four viral proteins: the envelope (E) protein, the NS1 protein, the NS3 protein, and the NS5 protein. Results: among the selected drug candidates, triptolide, stevioside, alepterolic acid, sphaeropsidin A, methyl dodovisate A, andrographolide, caesalacetal, and pyrimethamine have demonstrated moderate to good binding affinities (−8.0 to −9.4 kcal/mol) toward the selected proteins: E protein, NS3, NS5, and NS1 whereas pyrimethamine exerts −7.5, −6.3, −7.8, and −6.6 kcal/mol with viral proteins, respectively. Interestingly, the binding affinities of these lead compounds were better than those of an FDA-approved anti-viral medication (pyrimethamine), which is underused in dengue fever. Conclusion: we can conclude that diterpenoids can be considered as a possible anti-dengue medication option. However, in vivo investigation is recommended to back up the conclusions of this study.

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Citrus medica L. is rich in numerous vital bioactive constituents, though it is an underutilized among the citrus genus. Therefore, the aim of the present investigation was to evaluate the protective role of the C. medica fruit (CMF) methanol extract against carbofuran (CF)-induced toxicity in experimental rats. In addition, this work aims at detecting and measuring polyphenolic compounds by means of high-performance liquid chromatography (HPLC) and evaluation of the antioxidant activity of this extract. For this, studies dealing with serum hematological and biochemical parameters, liver endogenous antioxidants, as well as hepatic histo-architectural features have been carried out to assess the protective ability of CMF against CF-induced toxicity. Additionally, total phenol, flavonoid, and antioxidant capability were measured and the antioxidant action was investigated using DPPH and nitric oxide radical scavenging assays as well as reducing power assessments. HPLC results revealed the presence of benzoic acid, cinnamic acid, gallic acid, quercetin, and salicylic acid in CMF extract. Furthermore, results showed that CMF has considerable total phenol, flavonoid, and antioxidant capability and exhibits significant free radical scavenging and reducing potentialities. On the other hand, CF intoxication of rats significantly altered the hematological and serum biochemical parameters with hepatocytes disruption. Carbofuran also caused an upsurge in malondialdehyde (MDA) level and a decline in hepatic cellular antioxidant enzymes levels in rats compared to the control group. Co-administration of CMF amended the anomalies and improved the histo-architectural arrangement of hepatocytes in treated groups. CMF also inhibited the alteration of endogenous antioxidant enzymes and MDA levels as compared to the carbofuran treated group and returned them to their normal state. Taken all together, results from this investigation highlight the protective role of CMF against CF-induced toxicity which might be attributed to the polyphenolic constituents of the extract.

In order to investigate the effect of polymers on release mechanism of poorly soluble drugs from solid dispersions, Clonazepam was used as a model drug for these purposes. Five types of solid dispersions were prepared using polyethylene glycol 6000 (PEG-6000), Kollicoat IR, Kollidon VA 64 and Poloxomer in different drug-tocarrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solvent evaporation method was used for preparation of solid dispersions. The in-vitro dissolution study with temperature of 37° C and a paddle method, 100 rpm was used in 1000 ml of distilled water as dissolution medium in each dissolution basket for the pure drug and solid dispersions. For pure Clonazepam showed very slow dissolution rate and the solid dispersion considerably enhanced the dissolution rate. Decreased crystalline and increased amorphous fraction of the drug was probably done by wettability and dispersibility. The highest improvement in wettability and dissolution rate of Clonazepam was observed in PEG-6000, Poloxomer and Kollidon VA 64 (1:10 ratio).