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Pain is an unpleasant sensation that has complex and varying causative etiology. Modern drug discovery focuses on identifying potential molecules that target multiple pathways with a safer profile compared to those with a single target. The current treatment of pain and inflammation with the available therapeutics has a number of major side effects. Pain is one of the major clinical problems that need functional therapeutics which act on multiple targets and with low toxicity. Curcumin, a naturally occurring polyphenolic compound from Curcuma longa, has been used for years in Ayurvedic, Chinese, and in many other systems of traditional medicine. Pre-clinical data published thus far demonstrated that curcumin possesses multi-target biological functions, suggesting its potential use to cure different diseases. However, there is no or very brief systematic review of its potential use in pain and inflammation with underlying mechanisms for such activities. Accordingly, the aim of the current review was to update the pre-clinical data of curcumin and its multiple targeting pathways for analgesic and anti-inflammatory effects, and to further propose a molecular mechanism(s). A literature study was conducted using different known databases, including Pubmed, SciFinder, Google Scholar, and Science Direct. Available pre-clinical data suggest the ameliorating effect of curcumin in pain and inflammation is rendered through the modulation of pain pathways, including inhibition of a number of pro-inflammatory mediators, inhibition of oxidative stress and cyclooxygenase-2 (COX-2), down-regulation of Ca2+/calmodulin-depend protein kinase II (CaMKIIα) and calcium channels like transient receptor potential (TRP), modulation of metabotropic glutamate receptor-2 (mGlu2), modulation of monoamine system, inhibition of JAK2/STAT3 signaling pathway, remodeling of extracellular matrix proteins, inhibition of apoptosis, inhibition of JNK/MAPK and ERK/CREB signaling pathway, and activation of the opioid system. Taken all together, it is evident that curcumin is one of the promising, safe, and natural polyphenolic molecules that target multiple molecular pathways in pain and can be beneficial in the treatment and management of pain and inflammation.

When tested in the acetic acid-induced writhing and formalin-induced paw-licking tests, the ethanol extract of Vernonia patula (VP) aerial parts showed significant antinociceptive activity. In neuropharmacological tests, it also significantly delayed the onset of sleep, increased the duration of sleeping time, and significantly reduced the locomotor activity and exploratory behaviour of mice. Five phenolic compounds, namely gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol, were detected in VP following HPLC-DAD analysis. The presence of these phenolic compounds in VP provides some support for the observed antinociceptive and sedative effects. A computational study was performed to predict the binding affinity of gallic acid, vanillic acid, caffeic acid, quercetin and kaempferol towards the cannabinoid type 1 (CB1) receptor. Caffeic and vanillic acid showed the highest probable ligand efficiency indices towards the CB1 target. Vanillic acid displayed the best blood brain barrier penetration prediction score. These findings provide some evidence for the traditional use of VP to treat pain.

Gallic acid (GA) is a bioactive phytoconstituent that has been reported to prevent a number of diseases. However, there is no systematic review to-date on its anti-diabetic and cardioprotective potential including molecular mechanisms for such activities. This review aims to summarize the anti-diabetic and cardioprotective effects of GA and further propose a molecular mechanism of its anti-diabetic effects. Accumulation of associated literature was conducted through the use of databases including Google Scholar, PubMed, Web of Science, Science Direct and Scopus databases. Articles published until December 2018 were extracted and all the retracted articles were sorted based on the inclusion and exclusion criteria and relevant articles were further consulted for necessary information. We have found substantial investigations in animals and cultured cells that supports anti-diabetic and cardioprotective effects of GA with several underlying mechanisms including antioxidant enzyme systems and non-enzymatic defense mechanisms. The reported antioxidant activity of GA as well as the modulation of some key proteins linked to diabetes could be a part of the mechanisms by which GA showed anti-diabetic effect. In summary, it is evident that GA is one of the promising dietary phytochemicals that could be beneficial for the treatment and management of diabetes and associated myocardial damage.

Traditionally, sesame oil (SO) has been used as a popular food and medicine. The review aims to summarize the antioxidant and antiinflammatory effects of SO and its identified compounds as well as further fatty acid profiling and molecular docking study to correlate the interaction of its identified constituents with cyclooxygenase-2 (COX-2). For this, a literature study was made using Google Scholar, Pubmed, and SciFinder databases. Literature study demonstrated that SO has potential antioxidant and antiinflammatory effects in various test systems, including humans, animals, and cultured cells through various pathways such as inhibition of COX, nonenzymatic defense mechanism, inhibition of proinflammatory cytokines, NF-kB or mitogen-activated protein kinase signaling, and prostaglandin synthesis pathway. Fatty acid analysis of SO using gas chromatography identified known nine fatty acids. In silico study revealed that sesamin, sesaminol, sesamolin, stigmasterol, Δ5-avenasterol, and Δ7-avenasterol (-9.6 to -10.7 kcal/mol) were the most efficient ligand for interaction and binding with COX-2. The known fatty acid also showed binding efficiency with COX-2 to some extent (-6.0 to -8.4 kcal/mol). In summary, it is evident that SO may be one of promising traditional medicines that we could use in the prevention and management of diseases associated with oxidative stress and inflammation.

Agathisflavone (AGF) is a biflavonoid with a number of important biological and pharmacological activities, such as antioxidant, antimicrobial, and neuroprotective effects. However, its toxicological effects have not been fully investigated. Accordingly, the aim of this study was to investigate the toxicological effects of AGF in mice. For this purpose, the median lethal dose 50% (LD50) was determined along with the anatomic and histopathological parameters (weight, alimentation, excretion, biochemical, and hematological) in fertile untouched female Swiss mice. Results suggest that during the treatment, no deaths were reported at 300 and 2000 mg/kg (n = 03/group, p.o.). Moreover, AGF did not cause significant change in the above mentioned parameters in test animals when compared with the control group (0.05% Tween 80 dissolved in 0.9% saline). Taken all together, this non-clinical toxicological study revealed that AGF has an LD50 larger than 2000 mg/kg and did not change significantly the hematological, biochemical, histopathological, behavioral, as well as physiological parameters in the female mice.

Amaranthus spinosus is a common vegetable of Bangladesh and well-known for its ethnomedicinal uses. In this study, we have evaluated the ability of powdered supplementation, methanol extract, and aqueous extract of A. spinosus in attenuating in high-carbohydrate-high-fat (HCHF) diet-induced obesity and associated metabolic disorders in female obese rates. Several parameters have been analyzed in this study including body weight, organ weight, fat deposition, glycemic status, lipid levels, hepatic and renal biomarkers, hepatic antioxidant status, and hepatosteatosis. All three samples of A. spinosus significantly reduced weight gain, organ weight, and abdominal fat deposition. Improved glucose tolerance and lipid parameters were seen in obese rats administered with A. spinosus powder, methanol extract, and aqueous extract. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and creatine kinase levels were normalized by the test samples. A. spinosus boosted hepatic antioxidant levels including reduced glutathione (GSH), superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx). Histopathology of liver tissue revealed increased fat infiltration and higher steatosis score in HCHF diet-fed obese rats which was brought down by A. spinosus. Analyzing all the results it can be concluded that this medicinal herb is beneficial in the management of obesity and obesity-induced metabolic disorders, making it a prospective food supplement.

Background Mushrooms have been recognized both as medicine and nutritional food in many countries for thousands of years, owing to the presence of significant amounts of carbohydrates, proteins, lipids, fibers, and antioxidants. This study aims at evaluating the nutritional contents and antioxidant potentials of seven types of mushrooms cultivated in Bangladesh. Methods Proximate composition analysis of the collected mushrooms was performed to determine moisture content, pH, lipid, crude fibre, total ash, protein, carbohydrate content, and calorific value. Antioxidant potential of collected mushrooms were evaluated by mean of eight different methods including total flavonoid content, phenolic content, tannin content, total antioxidant activity, hydroxyl radical scavenging activity, DPPH assay and reducing power capacity. Results The results demonstrated that investigated mushrooms were found rich in proteins (20–45 g/100 g), carbohydrate (11–61 g/100 g in dry sample) and fibre (5–40 g/100 g). The ash content was found 6–10 g/100 g and glucose content 54–160 mg/100 g. However, all the mushrooms showed a lower content of lipid (1–4%). Results also revealed that the total antioxidant capacity of the extracts were found in the concentration range of 0.08–0.21 mg/mL, whereas the hydroxyl radical and DPPH radical scavenging activity were 0.88–1.40 and 0.05–0.63 mg/mL. Conclusion The findings of the current investigation proved that the studied Bangladeshi mushrooms are good source of nutritional and antioxidant components. Therefore, this study can help spreading awareness among Bangladeshi people regarding consumption of mushrooms as functional foods.

Background Cestrum diurnum L. (Solanaceae) is used in various traditional medicine for pain and related disorders. The Malayali tribe of Tamil Nadu in India use the leaf in joint pain. In the Chinese traditional medicine it is used for the treatment of burns and swellings. Present study was designed to evaluate its traditional use in pain and inflammation. Methods Methanol extract of the aerial parts of C. diurnum was tested by carrageenan induced paw oedema and formalin induced paw licking test in mice at the oral doses of 150 and 300 mg/kg body weight. NF-κB inhibitory activity was evaluated by TNF-α induced NF-κB activation assay in RAW 264.7 macrophage cells at the concentration of 100 µg/ml. Results The extract, at the doses of 150 and 300 mg/kg, showed significant inhibition (p

Pain is one of the most prevalent medical conditions but with limited therapeutic options. Morphine and salicin are not only the first analgesics but also played an important role in modern day medicinal chemistry, pharmacology and therapeutics. Despite the search for better agents for the management of pain, most of the newly introduced agents are either analogues of these old drugs or work in the same way. Ziconotide, capsaicin and botulinum toxin type A are the natural products that received FDA approval as analgesics. Each of them represents novel mechanisms of their analgesic action. Some other Conus venom peptides (MrIA, Contulakin G, Vc1.1, conantokin G), capsaicinoids, capsinoids and their synthetic analogues are also under investigations for the development of new analgesics. Natural products including nonpeptide toxins, mitragynine, salvinorin A, and flavonoids represent important scaffolds for the development of analgesics with novel mechanism of actions.

Phytol (PYT) is a diterpene member of the long-chain unsaturated acyclic alcohols. PYT and some of its derivatives, including phytanic acid (PA), exert a wide range of biological effects. PYT is a valuable essential oil (EO) used as a fragrance and a potential candidate for a broad range of applications in the pharmaceutical and biotechnological industry. There is ample evidence that PA may play a crucial role in the development of pathophysiological states. Focusing on PYT and some of its most relevant derivatives, here we present a systematic review of reported biological activities, along with their underlying mechanism of action. Recent investigations with PYT demonstrated anxiolytic, metabolism-modulating, cytotoxic, antioxidant, autophagy- and apoptosis-inducing, antinociceptive, anti-inflammatory, immune-modulating, and antimicrobial effects. PPARs- and NF-κB-mediated activities are also discussed as mechanisms responsible for some of the bioactivities of PYT. The overall goal of this review is to discuss recent findings pertaining to PYT biological activities and its possible applications.

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, 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 root-bark of the medicinally important plant Zanthoxylum budrunga (ZBRB) brooks a variety of uses in ethnobotanical and ethnomedicinal practice in Bangladesh and thus demands biological investigation to reveal its therapeutic potentiality. So, the present study was perpetrated to explore antioxidant, analgesic, antidiarrhoeal, and a cytotoxic activity of ethanolic root-bark extract of Zanthoxylum budrunga and was also to quantify the major bioactive polyphenolic constituents by HPLC analysis. Methods Total phenolic content was measured spectrophotometrically by using Folin Chiocalteu’s reagent while in vitro antioxidant activity was determined by means of 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and reducing power assay. HPLC analysis was performed to identify and quantify the major bioactive polyphenolic constituents present in the extract. Acetic acid induced writhing test and hot-plate test were conducted to evaluate the analgesic activity of the crude extract. On the other hand, in vivo antidiarrheal potentiality was investigated by using experimentally castor oil induced diarrhoea in mice and brine shrimp lethality bio-assay was implemented to check the cytotoxic potentiality of the crude extract. Results Zanthoxylum budrunga showed DPPH scavenging activity (IC50 54.27 μg/mL), while the total phenolic content was 647.91 mg GAE/100 g of extract. ZBRB also showed concentration dependent ferric reducing power activity. At the doses of 250 and 500 mg/kg, ZBRB exhibited statistically significant (P

Human tuberculosis (TB), caused by Mycobacterium tuberculosis, is the leading bacterial killer disease worldwide and new anti-TB drugs are urgently needed. Natural remedies have long played an important role in medicine and continue to provide some inspiring templates for drug design. Propolis, a substance naturally-produced by bees upon collection of plant resins, is used in folk medicine for its beneficial anti-TB activity. In this study, we used a molecular docking approach to investigate the interactions between selected propolis constituents and four ‘druggable’ proteins involved in vital physiological functions in M. tuberculosis, namely MtPanK, MtDprE1, MtPknB and MtKasA. The docking score for ligands towards each protein was calculated to estimate the binding free energy, with the best docking score (lowest energy value) indicating the highest predicted ligand/protein affinity. Specific interactions were also explored to understand the nature of intermolecular bonds between the most active ligands and the protein binding site residues. The lignan (+)-sesamin displayed the best docking score towards MtDprE1 (−10.7 kcal/mol) while the prenylated flavonoid isonymphaeol D docked strongly with MtKasA (−9.7 kcal/mol). Both compounds showed docking scores superior to the control inhibitors and represent potentially interesting scaffolds for further in vitro biological evaluation and anti-TB drug design.

Present investigation was aimed to evaluate the traditional use of edible part of soft shoots of Trichosanthes dioica Roxb. (Cucurbitaceae) as an antidiabetic in mice model. In addition, antioxidant activity and chemical profiling of this plant part were also performed to support its observed activity. The extract was subjected to oral glucose tolerance test in normal and alloxan induced diabetic mice to explore its antihyperglycemic activity. Antioxidant capacity was analyzed by a number of in vitro assays. Quantification of bioactive polyphenols was done by HPLC. Liquid Chromatography coupled with Mass Spectrometry (LCMS) was used to identify chemical constituents present in the extract. Total polyphenol and flavonoids content were found in significant quantity. In DPPH radical scavenging assay the IC50 value of the extract was found to be 148.62 µg/mL. Reducing power of the extract was comparable with that of butylatedhydroxytoluene (BHT). HPLC analysis indicated that quercetin, rutin, p-coumaric acid and kaempferol were the major bioactive polyphenols present in the extract. Further chemical profiling using LCMS analysis was identified a total of nine compounds with different chemical classes. In OGTT, extract (400 mg/kg BW) showed a 31.13% decrease (p

Antianxiety drugs currently in use are associated with a number of serious side effects. Present study was designed to evaluate the efficacy of anacardic acids (AAs) isolated from cashew nut (Anacardium occidentale L.) shell liquid (CNSL) to treat anxiety as well as its role in oxidative stress in mice model. Anxiolytic effect of AA was evaluated using rota-rod and a set of behavioral tests in male Swiss albino mice at the doses of 10, 25, and 50 mg/kg. Flumazenil was used to evaluate the possible involvement of GABAergic system in the mechanism of action of AA. The effect of AA on oxidative stress in mice was evaluated by determining the concentration of malondialdehyde (MDA), reduced glutathione, and catalase (CAT) activity. The detection of DNA damage of the treated animals was performed using alkaline comet test in the hippocampus and frontal cortex of the animals. The results demonstrated that AA did not produce myorelaxant and sedative effects, nor did it cause a decrease in locomotor activity. The anxiolytic effect of AA was well-evident in all tests, especially at higher dose levels (25 and 50 mg/mg). Flumazenil reversed the anxiolytic effect of AA at all doses. In addition, AA reduced oxidative stress by decreasing the concentration of MDA and increasing the levels of reduced glutathione (GSH) and CAT activity. Statistical analysis by Pearson's correlation indicated a positive correlation between anxiolytic effect of AA to its antioxidant and lipid peroxidation inhibitory activity. Furthermore, increased CAT activity and GSH concentrations in the hippocampus and frontal cortex of mice was also complementary to the reduced genotoxic damage observed in the study. In comet assay, AA did not increase in DNA damage. In conclusion, the results supported that AA possesses GABAA receptor mediated anxiolytic activity with the lack of myorelaxation and genotoxicity. © 2018 IUBMB Life, 70(5):420-431, 2018.

Consumable herbs play a basic part in sustenance and human health. Traditionally, Colocasia gigantea Hook (Araceae) is used to treat fever, infection, wounds healing, drowsiness, tuberculosis, stomach problems etc. AIM OF THE STUDY: The study aspired to identify bioactive compounds, to evaluate anti-inflammatory and analgesic potentials of edible herb C. gigantea, and to molecular docking study against anti-inflammatory enzyme Cyclooxygenase-2 (COX-2).Chemical components of C. gigantea were discerned by HPLC and GCMS assays. In vitro anti-inflammatory activity was appraised by heat-induced, hypotonicity, and hydrogen peroxide-induced hemolysis assays and in vivo by formalin-induced paw edema assay. In vivo analgesic activity was evaluated by acetic acid-induced pain modulation assay. Also, molecular docking of the identified compounds was explored against the anti-inflammatory enzyme cyclooxygenase-2.HPLC-DAD analysis divulged the presence of trans-cinnamic acid along with (-)-epicatechin as a prime component. Also, 9, 12-Octadecadienoic acid (37.86%) and n-Hexadecanoic acid (25.89%) as the major as well as 24 other compounds were confirmed through GCMS in the extract. In in vitro anti-inflammatory study, C. gigantea extract indicated prominent erythrocyte membrane stabilization activity with good percentage aegis in all experimental assays. In addition to, formalin-induced in vivo anti-inflammatory assay revealed the maximum (42.37% and 48.72%) suppression of edema at the fourth hour at 250 and 500 mg/kg body weight, respectively. Moreover, an in-vivo pain modulation assay exposed significant (p 0.05) activity at experimental doses. Furthermore, in the docking study, (-)-epicatechin was more active rather than other identified compounds with strong binding affinity to COX-2 protein.The extract evinced remarkable anti-inflammatory and analgesic activities. Identified bioactive components along with other components of the extract might play a pivotal role in the observed bioactivity and the results vindicate the use of edible herb C. gigantea in ancestral medicine.

Background: Cancer is a dreadful disease causing thousands of deaths per year worldwide, which requires precision diagnostics and therapy. Although the selection of therapeutic regimens depends on the cancer type, chemotherapy remains a sustainable treatment strategy despite some of its known side-effects. To date, a number of natural products and their derivatives or analogues have been investigated as potent anticancer drugs. These drug discoveries have aimed for targeted therapy and reduced side-effects, including natural therapeutic regimens. Objective: This review introduces a prospective fungal-derived polyphenol, Hispolon (HIS), as an anticancer agent. Accordingly, this review focuses on exploring the anticancer effect of hispolon based on information extracted from databases such as PubMed, ScienceDirect, MedLine, Web of Science, and Google Scholar. Methods: A literature search in PubMed, ScienceDirect, MedLine, Web of Science, and Google Scholar was accomplished, using the keyword ‘Hispolon’, pairing with ‘cancer’, ‘cytotoxicity’, ‘cell cycle arrest’, ‘apoptosis’, ‘metastasis’, ‘migration’, ‘invasion’, ‘proliferation’, ‘genotoxicity’, ‘mutagenicity’, ‘drug-resistant cancer’, ‘autophagy’, and ‘estrogen receptor. Results: Database-dependent findings from reported research works suggest that HIS can exert anticancer effects by modulating multiple molecular and biochemical pathways, including cell cycle arrest, apoptosis, autophagy, inhibition of proliferation, metastasis, migration, and invasion. Moreover, HIS inhibits the estrogenic activity and exhibits chemoprevention prospects, possibly due to its protective effects such as anticancer and anti-inflammatory mechanisms. To date, a number of HIS derivatives and analogues have been introduced for their anticancer effects in numerous cancer cell lines. Conclusion: Data obtained from this review suggest that hispolon and some of its derivatives can be promising anticancer agents, and may become plant-based cancer chemotherapeutic leads for the development of potent anticancer drugs, alone or in combination with other chemotherapeutic agents.

Southern coastal people of Bangladesh are highly vulnerable to food insecurity and malnutrition due to coastal flooding, deforestation and increased soil salinity. A number of green leafy vegetables are found in the southern coastal belt being traditionally eaten as daily basis by local people. But they are unaware of nutritional and medicinal use of these vegetables. To contribute to their wider utilization, five common vegetables namely Hibiscus sabdariffa, Trianthema portulacastrum, Diplazium esculentum, Heliotropium indicum L. and Hygrophila auriculata were selected for analysis of nutritional proximate, micronutrients and antioxidant potential. Nutritional properties were analyzed in terms of moisture, pH, protein, lipid, ash, fibre, minerals and carbohydrate. Total flavonoid, tannin and antioxidant capacity were evaluated using established protocols. The results demonstrated that collected plants are rich in carbohydrate, fibre, proteins, moisture and ash content but low in lipid content. The mineral elements were high with remarkable amount of Na (19.9–21.5 mg/gm), K (7.9–13.5 mg/gm) and P (1.0–1.8 mg/gm). All the samples were found to have considerable amount of flavonoid (90.6–144.5 mg QE/gm) and tannin content (26.8–57.2 mg GAE/gm). The IC50 value of DPPH and superoxide radical scavenging was the lowest for H. indicum (37.1 and 83.4 μg/ml, respectively) whereas T. portulacastrum possessed high reducing power (IC50 53.7 μg/ml). Among the five investigated species, T. portulacastrum and H. indicum were found to have good nutritional and antioxidant properties, thus can be promoted as a significant source of nutritional and antioxidant food supplements., Natural product chemistry; Food analysis; Food composition; Food chemistry; Nutrition; Nutrient availability; Coastal vegetables; Nutritional and antioxidant potential; Micronutrient; Free radical.

Date palm (P. dactylifera) plays a vital role in ethnomedicinal practices in several parts of the world. There are over 2000 cultivars of date palm that differ in chemical composition and extent of bioactivity. The present study was undertaken to comparatively evaluate the antioxidant potential of three cultivars of date palm (Ajwah, Safawy and Sukkari) from Saudi Arabia and analyze their phenolic constituents in order to draw a rationale for their activity. Antioxidant activities of the date cultivars were evaluated by different quantitative methods including 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydroxyl radical scavenging assay, total antioxidant capacity, reducing power, total phenolic (TPC), flavonoid (TFC) and tannin content (TTC), while qualitative phenolic composition was determined using ultra performance liquid chromatography coupled to quadropole time of flight mass spectrometry (UPLC-QTOF-MS). All the three date extracts showed good DPPH radical scavenging (IC50 103–177 μg/mL) and hydroxyl radical scavenging (IC50 1.1–1.55 mg/mL) activity and total antioxidant capacity (IC50 87–192 μg/mL). The reducing power was also comparable to that of ascorbic acid, used as standard in above experiments. All the three samples contain significant amount of major antioxidant components (phenolic, flavonoid and tannin) that successfully correlates with the results of radical scavenging assays. UPLC-QTOF-MS revealed a total of 22 compounds in these date cultivars classified into common phenolics, flavonoids, sterols and phytoestrogens. Significant variation in the degree of antioxidant activity of these three date cultivars can be attributed to the difference in the content and composition of phenolic compounds., Highlights • Ajwah, Safawy and Sukkari date palm possess significant amount of natural antioxidant components. • Dietary intake of Ajwah, Safawy and Sukkari date palm can prevent a number of oxidative damage mediated diseases. • The common phenolics, flavonoids, sterols and phytoestrogens of date palm might contributed in the prevention of diseases.

In addition to the rich nutritional value, date palm is also used in various ethnobotanical practices for the treatment of various disease conditions. Present investigation was undertaken to examine the neuropharmacological and antinociceptive effect of the ethanol extract of three date cultivars growing in Saudi Arabia, namely Ajwah, Safawy and Sukkari. Neuropharmacological effect was observed by pentobarbitone induced sleeping time, open field, and hole board test. Antinociceptive activity was tested by acetic acid induced writhing and hot plate test. The date extracts were also subjected to HPLC analysis to detect the presence of common bioactive polyphenols. All the three date extracts extended the pentobarbitone induced sleeping time, reduced locomotor activity in open field test and reduced exploratory behaviour in hole board test in mice. The extracts also reduced acetic acid induced writhing and delayed response time in hot plate test. The activities were stronger for Ajwah than the other two date cultivars. HPLC analysis indicated the presence of trans-ferulic acid in all three cultivars, while (+)-catechin and (-)-epicatechin only in Ajwah and Safawy. The observed neuropharmacological and analgesic activity could be partly due to the presence of (+)-catechin, (-)-epicatechin and trans-ferulic acid, three important plant polyphenols well known for their neuroprotective activity and their ability to exert antioxidant activity on brain cells. Present investigation also supports the ethnobotanical use of date palm to provide ameliorating effects in pain and CNS disorders.

Chisocheton is one of the genera of the family Meliaceae and consists of ca. 53 species; the distribution of most of those are confined to the Indo-Malay region. Species of broader geographic distribution have undergone extensive phytochemical investigations. Previous phytochemical investigations of this genus resulted in the isolation of mainly limonoids, apotirucallane, tirucallane, and dammarane triterpenes. Reported bioactivities of the isolated compounds include cytotoxic, anti-inflammatory, antifungal, antimalarial, antimycobacterial, antifeedant, and lipid droplet inhibitory activities. Aside from chemistry and biological activities, this review also deals briefly with botany, distribution, and uses of various species of this genus.

The ethanol extract of tuber part of Colocasia fallax Schott (Araceae) was tested for its potential analgesic and antioxidant activities. Acetic acid induced writhing method was used to evaluate the analgesic activity at the concentration of 250 and 500 mg/kg body weight. In order to investigate the antioxidant activity, four complementary test systems, namely, 2,2-diphenyl-1-picryl-hydrazil (DPPH) free radical scavenging, ferric reducing power assay, total phenolic and flavonoid contents were used. Polyphenolic compounds were also detected by HPLC analysis. The extract showed significant (P

Purpose: Inflammation and oxidative stress can lead to different chronic diseases including cancer and atherosclerosis. Many medicinal plants have the potential to show as anti-inflammatory activity. Present investigation was performed to investigate anti-inflammatory, antioxidant activity, and quantification of selected bioactive plant polyphenols of the ethanol (EAH) and aqueous (AAH) extracts of Acalypha hispida (Euphorbiaceae) leaves. Methods: Anti-inflammatory activity was evaluated by carragenan and histamine induced rat paw edema models while antioxidant capacity was evaluated by DPPH free radical scavenging, Fe+2 chelating ability, reducing power, NO scavenging, total phenolic and total flavonoid content assay. Identification and quantification of bioactive polyphenols was done by HPLC. Results: At the doses of 200 and 400 mg/kg, both EAH and AAH showed statistically significant inhibition of paw volume in the anti-inflammatory activity test. Both the extracts showed DPPH scavenging (IC50: 14 and 17 µg/ml, respectively), Fe+2 ion chelating (IC50: 40 and 46 µg/ml, respectively), NO scavenging activity (65.49 and 60.66% inhibition at 100 µg/ml), and concentration dependent reducing power ability. For EAH and AAH, flavonoid content was 126.30 and 149.72 mg QE/g dry extract, while phenolic content was 130.51 and 173.80 mg GAE/g dry extract, respectively. HPLC analysis of EAH and AAH indicated the presence of high content of ellagic acid along with other phenolic constituents. Conclusion: High content of ellagic acid along with other phenolic constituents might have played an important role in the observed anti-inflammatory and antioxidant activity.

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.

Present study was undertaken to evaluate the analgesic activity of the ethanol extract of Chrysopogon aciculatus. In addition to bioassays in mice, chemical profiling was done by LC-MS and GC-MS to identify phytochemicals, which were further docked on the catalytic site of COX-2 enzymes with a view to suggest the possible role of such phytoconstituents in the observed analgesic activity. Analgesic activity of C. aciculatus was evaluated by acetic acid induced writhing reflex method and hot plate technique. Phytochemical profiling was conducted using liquid chromatography mass spectrometry (LC-MS) and gas chromatography mass spectrometry (GC-MS). In docking studies, homology model of human COX-2 enzyme was prepared using Easy Modeler 4.0 and the identified phytoconstituents were docked using Autodock Vina. Preliminary acute toxicity test of the ethanol extract of C. aciculatus showed no sign of mortality at the highest dose of 4,000 mg/kg. The whole plant extract significantly (p < 0.05) inhibited acetic acid induced writhing in mice at the doses of 500 and 750 mg/kg. The extract delayed the response time in hot plate test in a dose dependent manner. LC-MS analysis of the plant extract revealed the presence of aciculatin, nudaphantin and 5α,8α-epidioxyergosta-6,22-diene-3β-ol. Three compounds namely citronellylisobutyrate; 2,4-dihydroxy-7-methoxy-(2H)-1,4-benzoxazin-3(4H)-one and nudaphantin were identified in the n-hexane fraction by GC-MS. Among these compounds, six were found to be interacting with the binding site for arachidonic acid in COX-2 enzyme. Present study strongly supports the traditional use of C. aciculatus in the management of pain. In conclusion, compounds (tricin, campesterol, gamma oryzanol, and citronellyl isobutyrate) showing promising binding affinity in docking studies, along with previously known anti-inflammatory compound aciculatin can be held responsible for the observed activity.

Purpose Free radicals are considered as the causative agents of a variety of acute and chronic pathologies. Natural antioxidants have drawn attention of the researchers in recent years for their ability to scavenge free radicals with minimal or even no side effects. This study evaluates the antioxidant capacity of agathisflavone, a naturally occurring biflavonoid by a number of in vitro methods. Methods Agathisflavone was subjected to DPPH, ABTS, OH and NO radical scavenging assay, reducing potential and inhibition of lipid peroxidation (TBARS) test using trolox as a standard. Results Agathisflavone showed concentration-dependent antioxidant activity against all types of free radicals used in this study. The antioxidant capacity, reducing potential and inhibition of lipid peroxidation showed by agathisflavone were comparable to that of trolox. Conclusion Agathisflavone exhibited antioxidant capacity, which suggests considering this biflavonoid for the use in the prevention and/or treatment of diseases precipitated by oxidative stress.

© 2018 Elsevier Ltd. This manuscript version is made available under the CC-BY-NC-ND 4.0 license: http://creativecommons.org/licenses/by-nc-nd/4.0/ This author accepted manuscript is made available following 12 month embargo from date of publication (May 2018) in accordance with the publisher’s archiving policy, Omeprazole (OME) is a proton pump inhibitor used for the treatment of various gastric and intestinal disease; however, studies on its effects on the genetic materials are still restricted. The present study aimed to evaluate possible toxicogenic effects of OME in Allium cepa meristems with the application of cytogenetic biomarkers for DNA damage, mutagenic, toxic and cytotoxic effects. Additionally, retinol palmitate (RP) and ascorbic acid (AA) were also co-treated with OME to evaluate possible modulatory effects of OME-induced cytogenetic damages. OME was tested at 10, 20 and 40 μg/mL, while RP and AA at 55 μg/mL and 352.2 μg/mL, respectively. Copper sulphate (0.6 μg/mL) and dechlorinated water were used as positive control and negative control, respectively. The results suggest that OME induced genotoxicity and mutagenicity in A. cepa at all tested concentrations. It was noted that cotreatment of OME with the antioxidant vitamins RP and/or AA significantly (p

A total of seven compounds were isolated from the methanol extract of leaves of Murraya koenigii (Linn.) Spreng. The isolated compounds were characterized as arborinine ( 1 ), ferulic acid ( 2 ), umbelliferone ( 3 ), mahanimbine ( 4 ), koenimbine ( 5 ), koenidine ( 6 ) and O -demethyl murrayanine ( 7 ) by extensive spectroscopic studies, including high field NMR analysis as well as co-TLC with authentic samples, whenever possible. This is the first report of occurrence of arborinine ( 1 ) and ferulic acid ( 2 ) from Murraya species. Dhaka Univ. J. Pharm. Sci. 14(1): 29-33, 2015 (June)

A series of 21 compounds isolated from Curcuma zedoaria was subjected to cytotoxicity test against MCF7, Ca Ski, PC3 and HT-29 cancer cell lines, and a normal HUVEC cell line. To rationalize the structure–activity relationships of the isolated compounds, a set of electronic, steric and hydrophobic descriptors were calculated using density functional theory (DFT) method. Statistical analyses were carried out using simple and multiple linear regressions (SLR, MLR), principal component analysis (PCA), and hierarchical cluster analysis (HCA). SLR analyses showed that the cytotoxicity of the isolated compounds against a given cell line depend on certain descriptors, and the corresponding correlation coefficients (R2) vary from 0%–55%. MLR results revealed that the best models can be achieved with a limited number of specific descriptors applicable for compounds having a similar basic skeleton. Based on PCA, HCA and MLR analyses, active compounds were classified into subgroups, which was in agreement with the cell based cytotoxicity assay.

Ceriops decandra is a mangrove tree species, reputed for its folkloric uses in the treatment of gastrointestinal disorders, infection, snakebites, inflammation, and cancer. Different parts of the plant are rich with various phytoconstituents which include diterpenoids (ceriopsin A-G), triterpenoids (lupeol, α-amyrin, oleanolic acid, ursolic acid), and phenolics (catechin, procyanidins).These phytoconstituents and their derivatives could form a new basis for developing new drugs against various diseases. The objective of the present study is to compile the phytochemical, ethnobotanical, biological, and pharmacological significance of the plant to provide directions for future research to find out therapeutically active lead compounds for developing new drugs against diseases of current interest including diabetes, inflammation, and cancer.

The diterpene lactone andrographolide, isolated from Andrographis paniculata, has been proven to possess several important protective biological activities, including antioxidant, anti-inflammatory, immunomodulatory, antiseptic, antimicrobial, cytotoxic, hypolipidemic, cardioprotective, hepatoprotective, and neuroprotective effects. In addition, it has been reported to play a therapeutic role in the treatment of major human diseases, such as Parkinson's disease, rheumatoid arthritis, and colitis. This systematic review aims to highlight andrographolide as a promising agent in cancer treatment. To this purpose, a number of databases were used to search for the cytotoxic/anticancer effects of andrographolide in pre-clinical and clinical studies. Among 1703 identified literature articles, 139 were included in this review; 109 were investigated as non-clinical, whereas 24, 3, and 3 were pre-clinical, clinical, and non-pre-clinical trials, respectively. Among the model systems, cultured cell lines appeared as the most frequently (79.14%) used, followed by in vivo models using rodents, among others. Furthermore, andrographolide was found to exert cytotoxic/anticancer effects on almost all types of cell lines with the underlying mechanisms involving oxidative stress, cell cycle arrest, anti-inflammatory and immune system mediated effects, apoptosis, necrosis, autophagy, inhibition of cell adhesion, proliferation, migration, invasion, anti-angiogenic activity, and other miscellaneous actions. After careful consideration of the relevant evidence, we suggest that andrographolide can be one of the potential agents in the treatment of cancer in the near future.

The present study was designed to investigate the inflammatory and antioxidant activities of ethanolic leaf extract of Brownlowia tersa (L.) Kosterm. The anti-inflammatory activity of leaf extract was studied using carrageenan and histamine-induced rat paw edema test at different doses (200 and 400 mg/kg body weight). DPPH free radical scavenging, nitric oxide scavenging, reducing power, Fe++ ion chelating ability and total phenolic content were used for determining antioxidant activities. The extract, at the dose of 400 mg/kg, showed a significant anti-inflammatory activity (P

Chisocheton is one of the genera of the family Meliaceae and consists of ca. 53 species; the distribution of most of those are confined to the Indo-Malay region. Species of broader geographic distribution have undergone extensive phytochemical investigations. Previous phytochemical investigations of this genus resulted in the isolation of mainly limonoids, apotirucallane, tirucallane, and dammarane triterpenes. Reported bioactivities of the isolated compounds include cytotoxic, anti-inflammatory, antifungal, antimalarial, antimycobacterial, antifeedant, and lipid droplet inhibitory activities. Aside from chemistry and biological activities, this review also deals briefly with botany, distribution, and uses of various species of this genus.

Air-dried powdered L. adscendens (931 g) was Soxhlet extracted, successively with n-hexane, EtOAc and MeOH. Vacuum liquid chromatography of the hexane extract (14 g), using a hexane-CHCl3 gradient (100:0-0:100) yielded 11 fractions.

The methanol extract of Xylocarpus granatum bark was studied for its antidiarrhoeal properties in experimental diarrhoea, induced by castor oil and magnesium sulphate in mice. At the doses of 250 and 500 mg/kg per oral, the methanol extract showed significant and dose-dependent antidiarrhoeal activity in both models. The extracts also significantly reduced the intestinal transit in charcoal meal test when compared to atropine sulphate (5 mg/kg; i.m.). The results showed that the extracts of Xylocarpus granatum bark have a significant antidiarrhoeal activity and supports its traditional uses in herbal medicine.

Purpose There is an urgent need to discover and develop new drugs to combat Mycobacterium tuberculosis, the causative agent of tuberculosis (TB) in humans. In recent years, there has been a renewed interest in the discovery of new anti-TB agents from natural sources. In the present investigation, molecular docking studies were carried out on two ellagic acid derivatives, namely pteleoellagic acid (1) isolated from Ludwigia adscendens, and 3,3′-di-O-methyl ellagic acid 4-O-α-rhamnopyranoside (2) isolated from Trewia nudiflora, to investigate their binding to two enzymes involved in M. tuberculosis cell wall biogenesis, namely 2-trans-enoyl-ACP reductase (InhA) and β-ketoacyl-ACP reductase (MabA), and to pantothenate kinase (PanK type I) involved in the biosynthesis of coenzyme A, essential for the growth of M. tuberculosis. Methods Molecular docking experiments were performed using AutoDock Vina. The crystal structures of InhA, MabA and PanK were retrieved from the RCSB Protein Data Bank (PDB). Isonicotinic-acyl-NADH for InhA and MabA, and triazole inhibitory compound for PanK, were used as references. Results Pteleoellagic acid showed a high docking score, estimated binding free energy of −9.4 kcal/mol, for the MabA enzyme comparable to the reference compound isonicotinic-acyl-NADH. Conclusions Knowledge on the molecular interactions of ellagic acid derivatives with essential M. tuberculosis targets could prove a useful tool for the design and development of future anti-TB drugs.

Curcumenol and curcumenone are two major constituents of the plants of medicinally important genus of Curcuma, and often govern the pharmacological effect of these plant extracts. These two compounds, isolated from C. zedoaria rhizomes were studied for their binding to human serum albumin (HSA) using the fluorescence quench titration method. Molecular docking was also performed to get a more detailed insight into their interaction with HSA at the binding site. Additions of these sesquiterpenes to HSA produced significant fluorescence quenching and blue shifts in the emission spectra of HSA. Analysis of the fluorescence data pointed toward moderate binding affinity between the ligands and HSA, with curcumenone showing a relatively higher binding constant (2.46 × 105 M−1) in comparison to curcumenol (1.97 × 104 M−1). Cluster analyses revealed that site I is the preferred binding site for both molecules with a minimum binding energy of −6.77 kcal·mol−1. However, binding of these two molecules to site II cannot be ruled out as the binding energies were found to be −5.72 and −5.74 kcal·mol−1 for curcumenol and curcumenone, respectively. The interactions of both ligands with HSA involved hydrophobic interactions as well as hydrogen bonding.

The crude ethanolic extract of the leaves of Clerodendrum viscosum (Family: Verbenaceae) was evaluated for its antioxidant and analgesic activities to investigate the scientific basis of the traditional uses. The antioxidant property of the extract was assessed by 1, 1-diphenyl -2- picryl hydrazyl (DPPH) free radical scavenging assay. The extract showed prominent antioxidant activity () which was comparable to standard drug ascorbic acid ().The extract produced significant (P

Preliminary pharmacological studies were performed on the methanol extract of Bixa orellana L. (Bixaceae) leaves to investigate neuropharmacological, anticonvulsant, analgesic, antidiarrhoeal activity and effect on gastrointestinal motility. All studies were conducted in mice using doses of 125, 250 and 500 mg/kg of body weight. In the pentobarbitone-induced hypnosis test, the extract statistically reduced the time for the onset of sleep at 500 mg/kg dose and (dose-dependently) increased the total sleeping time at 250 and 500 mg/kg dose. A statistically significant decrease in locomotor activity was observed at all doses in the open-field and hole-cross tests. In the strychnine-induced anticonvulsant test, the extract increased the average survival time of the test animals (statistically significant at 250 and 500 mg/kg). The extract significantly and dose-dependently reduced the writhing reflex in the acetic acid-induced writhing test. Antidiarrhoeal activity was supported by a statistically significant decrease in the total number of stools (including wet stools) in castor oil-induced diarrhoea model. A statistically significant delay in the passage of charcoal meal was observed at 500 mg/kg in the gastrointestinal motility test. The extract was further evaluated in vitro for antioxidant and antibacterial activity. It revealed radical scavenging properties in the DPPH assay (IC(50)=22.36 microg/ml) and antibacterial activity against selected causative agents of diarrhoea and dysentery, including Shigella dysenteriae.

The extracts of some Bangladeshi medicinal plants, Possur (Xylocarpus mekongensis), Dhundul (Xylocarpus granatum), Gab (Diospyros peregrina), Kadom (Anthocephalus chinensis) and Sundari (Heritiera fomes), were assessed for their possible antinociceptive activity using acetic acid induced writhing model in mice. Most of these plants have been used in traditional medicine in Bangladesh as well as in other countries for the treatment of various ailments ranging from common cold to cancer. All these extracts significantly inhibited the acetic acid induced writhing in mice at the oral dose of 500 mg/kg body weight. The extract of Anthocephalus chinensis bark showed the most potent writhing inhibition (69.47%, P

Piper chaba Hunter (Piperaceae) is a common pepper in the southern part of Bangladesh. Various parts of this plant have been extensively used in different traditional formulations including ayurveda. In order to rationalize the ethnomedical uses of this plant in a number of ailments, the methanol extract of the stem bark was subjected to preliminary evaluation for analgesic, anti-inflammatory, diuretic, anti-diarrhoeal, effect on gastrointestinal motility and CNS depressant activity in mice and rat at 125, 250 and 500 mg/kg body weight doses. The extract at given doses significantly and dose dependently reduced the frequency of acetic acid induced writhing in mice, prolonged the tail flicking latency in mice, reduced Carrageenan-induced paw edema volume in rat, delayed the onset as well as reduced the frequency of castor oil induced diarrhoeal episodes in mice, decreased gastrointestinal motility as assessed by the charcoal motility test in mice and prolonged pentobarbitone induced sleeping time in mice. However at the same doses, the extract exhibited moderate diuretic activity only at the highest dose.

The crude methanolic extract of the leaves of Amoora cucullata Roxb. was investigated for its possible anti-inflammatory activity using carrageenin induced rat paw edema model and cotton pellet implantation method in rat. The extract was also studied for its antinociceptive activity using acetic acid induced writhing model in mice. At the doses of 200 and 400 mg/kg body weight, the extract showed significant anti-inflammatory activity in both models. At the same doses, the extract also significantly reduced the number of acetic acid-induced abdominal constriction (writhing) in mice. The crude extract also showed significant diuretic activity in albino mice.

The methanol extract of Diospyros peregrina bark was studied for its effect on the central nervous system (CNS) using the pentobarbitone induced sleeping time test, the open field test and the hole cross test in Swiss albino mice. The present investigation revealed that the extract, at the doses of 250 and 500 mg/kg, significantly prolonged the pentobarbitone induced sleeping time in mice though the onset of sleep was delayed as compared to the control. In open field test, the depressing effect was prominent from the second observation period (30 min) and persisted throughout the entire experimental period (240 min). In the hole cross test, the depressing effect was observed from the second observation period (30 min) and persisted up to fifth observation period (120 min) for 250 mg dose group and up to sixth observation period (180 min) for 500 mg dose group. These results support the finding that D. peregrina bark extract at the above doses has CNS depressing effects and indicate that D. peregrina bark may contain biologically active constituent(s) having CNS depressant activity.

A number of plants from different geographical origins have been shown to possess antioxidant activity. Some of them have been developed as natural antioxidant formulations for food, cosmetic and other applications. Bangladeshi flora is a rich source of a range of plant species, many of which are medicinal plants, and have been used in the preparations of the Unani and Ayurvedic traditional medicines. There are no, or just a few, reports on any systematic screening of the extracts of Bangladeshi plants for free radical scavenging activity using DPPH assay available to date. As part of our on-going search for biological activity in Bangladeshi plants, Kadam (Anthocephalus chinensis), Goran (Ceriaps decandra), Swarnalata (Cuscuta reflexa), Gab (Diospyros peregrina), Sundari (Heritiera fomes), Dhundul (Xylocarpus granatum) and Possur (Xylocarpus mekongensis) have been selected for the assessment of their free radical scavenging activity, and studies on the contents of alkaloids, anthraqunones, flavonoids and tannins in these extracts. Most of these species have been used in traditional medicine in Bangladesh and other countries for the treatment of various illnesses ranging from common cold to cancer. All extracts, except the methanol extract of Cuscuta reflexa, displayed significant free radical scavenging activity in the DPPH assay values within the range of . Among these extracts, the methanol extract of Xylocarpus granatum exhibited the most potent activity and that of Cuscuta reflexa had the least activity . While none of these plants showed positive tests with Dragendorff's reagent, presence of low to moderate amounts of phenolic compounds, e.g. anthraquinones, flavonoids and tannins was evident in all of these plants, except for the methanolic extracts of C. reflexa and the barks of D. peregrina, which did not display any evidence for the presence of flavonoids and anthraquinones, respectively.