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Nelumbo nucifera (sacred lotus), locally known as Poddo, has been used as food and traditional remedy in Ayurvedic system in India and Traditional Chinese Medicine for a wide range of diseases. During past two decades, there are numerous scientific studies and general reviews have been published on its phytochemistry and pharmacology. However, in this paper, we aim to make a survey on neuropharmacological effects, as well as psychoactivities, of N. nucifera, identifying the active constituents and their proposed mechanism of actions which has not been systematically documented in the literature. Several online databases, including Google Scholar, PubMed, Web of Science, Science Direct, and Scopus were employed to conduct this survey. Previous studies have demonstrated that N. nucifera has potential neuropharmacological effects in various test systems, including in vivo animal models and in vitro cultured cells or enzymes through various mechanistic pathways, including 5-HT2A receptor blockade, GABAergic system, regulating the NCAM and GAP-43 expression levels, regulating for skolinstimulated cAMP production, and many more. Our survey showed that many alkaloids isolated from N. nucifera demonstrated antidepressant, sedative-hypnotic, anxiolytic, analgesia-potentiating action, anticonvulsant, antipsychotic, and memory enhancer activities. Although many studies have showed potential neurotherapeutic benefits of this plant and many of its constituents, but the focus of research towards clinical trial in human is rather very limited. Dhaka Univ. J. Pharm. Sci. 20(3): 347-358, 2022 (June) Centennial Special Issue

The demand for medicinal plants and their derived substances is increasing day by day due to their relevance in the context of drug discovery and development. The goal of this investigation is to assess the pharmacological and phytochemical potentials of the grossly underexplored Antidesma montanum Blume (Family: Phyllanthaceae). The methanolic extract of the leave of this plant was fractionated and then followed by initial screening of phytochemical. The investigation of the pharmacological potential, which includes antioxidant, antidiarrheal, anti-inflammatory, analgesic, anti-pyretic, and anxiolytic evaluations, was accomplished using an in vitro free radical scavenging assay with 2,2-diphenyl-1-picrylhydrazyl (DPPH), castor oil-induced diarrheal test, egg albumin test, acetic acid-induced writhing model, brewer’s yeast induced fever test, swing test, open field, and light-dark test, respectively. The investigation o phytochemicals proposes that the methanol extract of A. montanum possesses flavonoids, tannins, terpenoids, saponins, amino acids, fixed oils, and sterols. Pharmacological evaluation suggests that A. montanum possesses significant antioxidant, anti-diarrheal, anti-inflammatory, and analgesic effects. The methanol and chloroform fractions exhibited better DPPH radical scavenging activities with an IC50: 103 ± 0.05 and 108.7 ± 0.05 µg/ml, respectively. The methanol and chloroform fractions also showed anti-inflammatory capacities in the egg albumin (IC50 values: 89.10 ± 0.07 and 92.85 ± 0.07 µg/ml, respectively) model. The plant also showed anti-pyretic and anxiolytic activities in a dose-dependent manner. One of the possible sources of phytotherapeutic lead compounds is A. montanum. To extract and analyze the key bioactive components of this essential therapeutic plant, more research is required.

Lectins are capable of cell agglutination by interacting with the cell surface exposed glycans. Lectins that agglutinate erythrocytes are called hemagglutinin. These compounds occur in various organisms including plants. In this study, twenty edible vegetables were subjected to screen for haemagglutination and lectin activity. Lectin activity was assessed by measuring the inhibition ability of haemagglutination by different sugars. PBS (Phosphate Buffer Saline) treated homogenate was tested for haemagglutination against erythrocytes suspension, and inhibition of agglutination was determined by serially diluted sugar solution. The results of this study demonstrated that one homogenate among the homogenates of 20 vegetables was found to be capable of human erythrocyte agglutination. The Ipomoea aquatica homogenate shown positive haemagglutination reaction against red blood cells (RBCs) with HA titer value of 4 HA-U/25uL, and four out of seven sugars were able to inhibit RBCs agglutination. Among the four sugars, two are potent inhibitors of agglutination. The neutralization of haemagglutination by four monosaccharides provides a suggestion that the lectin present in I. aquatica may be multivalent carbohydrate binding hemagglutinin. This is the first report to identify that Ipomoea aquatica contains lectin protein which is a polyvalent sugar binding lectin and specific for glucose, galactose, mannose and N-Acetyl-D-Glucosamine.

Callicarpa arborea Roxb. is widely used as traditional medicine especially by the tribal people of Bangladesh in the management of wide range of ailments. In addition to Bangladesh, the leaves of this plant is utilized as a remedy to various painful and inflammatory conditions including rheumatism, toothache and stomachache in other countries of Indian subcontinent.Depending on the ethnomedicinal uses, we undertook this study to investigate the in-vivo analgesic and anti-inflammatory activities of the methanolic extract of C. arborea Roxb. leaves in Swiss albino mice as well as its chemical composition.We evaluated the analgesic activity of Callicarpa arborea Roxb. leaves by the acetic acid induced writhing test, the hot plate test, and the formalin test. We undertook the egg albumin induced paw edema test to determine the anti-inflammatory activity of the plant. Furthermore, we conducted the phytochemical profiling by gas chromatography-mass spectrometry (GC-MS).In acute toxicity test, no mortality was observed at the highest dose of 2000 mg/kg b.w. Significant (p 0.005) inhibition of acetic acid induced writhing was observed at both doses of the extract. A dose dependent increase in the response time was seen in the hot-plate test. In the formalin test, the extract significantly inhibited pain response in both early and late phase. We observed marked anti-inflammatory activity manifested by a significant (p 0.005) reduction in egg albumin induced paw edema. We identified a total of twenty one compounds in the extract of by GC-MS analysis.Taken all into consideration we conclude that the leaves of C. arborea Roxb. possesses potent analgesic and anti-inflammatory activity, thus justifying its's ethnomedicinal use against painful and inflammatory pathological conditions.

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.

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.

This study aimed to determine the activity of PYT and its derivatives against COX-2, including 5IKR protein induced inflammation by using the computational tools. PYT and its derivatives have been designed by utilizing density functional theory (DFT) and the performance of the drugs was also evaluated by molecular docking study. Results suggest that the NH2 derivative of PYT (D-NH2) showed binding energy -6.4 (Kcal/mol) with protein 5IKR of COX-2 compared to the main drug (D) that showed binding energy -5.1 (Kcal/mol) with the same protein. HOMO and LUMO energy values were also calculated to determine the chemical reactivity of all the modified drugs. Non-covalent interactions of PYT and its derivatives were essential in improving the performance. In conclusion, D-NH2 showed better preference in inhibiting to the protein 5IKR of COX-2 compared to other modified drugs and it can be claimed that D-NH2 will be the best conformer for COX-2 induced inflammation.

Liver diseases are quite prevalant in many densely populated countries, including Bangladesh. The liver and its hepatocytes are targeted by virus and microbes, as well as by chemical environmental toxicants, causing wide-spread disruption of metabolic fuctions of the human body, leading to death from end-stage liver diseases. The aim of this review is to systematically explore and record the potential of Bangladeshi ethnopharmacological plants to treat liver diseases with focus on their sources, constituents, and therapeutic uses, including mechanisms of actions (MoA). A literature survey was carried out using Pubmed, Google Scholar, ScienceDirect, and Scopus databases with articles reported until July, 2020. A total of 88 Bangladeshi hepatoprotective plants (BHPs) belonging to 47 families were listed in this review, including Euphorbiaceae, Cucurbitaceae, and Compositae families contained 20% of plants, while herbs were the most cited (51%) and leaves were the most consumed parts (23%) as surveyed. The effect of BHPs against different hepatotoxins was observed via upregulation of antioxidant systems and inhibition of lipid peroxidation which subsequently reduced the elevated liver biomarkers. Different active constituents, including phenolics, curcuminoids, cucurbitanes, terpenoids, fatty acids, carotenoids, and polysaccharides, have been reported from these plants. The hepatoameliorative effect of these constituents was mainly involved in the reduction of hepatic oxidative stress and inflammation through activation of Nrf2/HO-1 and inhibition of NF-κB signaling pathways. In summary, BHPs represent a valuable resource for hepatoprotective lead therapeutics which may offer new alternatives to treat liver diseases.

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.

This study aimed at phytochemical analysis and evaluation of toxic and protective effects of the crude aqueous extract of Typhonium trilobatum. Toxicity analysis was done in Allium cepa, while anti-inflammatory, and membrane stabilizing and clotlysis capacity were tested by using egg albumin and human erythrocytes, respectively. The results suggest that T. trilobatum aqueous extract contains alkaloids, glycosides, tannins, saponins, flavonoids and reducing sugars. The crude extract exhibited toxicity in A. cepa in a time and concentration dependent manner. The highest root growth inhibition was observed at exposure time 72 h in 20% (v/v) concentration extract of the herb. The extract at low concentration (2.5 and 5%) reduced the root growth inhibition capacity at 48 h in comparison to 24 and 72 h, possibly by adaptation of DNA damage profile in the eukaryotic test system (A. cepa), which was further confirmed in anti-inflammatory and membrane stabilizing, and anti-atherothrombosis test. In the latter cases, the extract at 0.02–0.08% (v/v) significantly (p

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.

Heliotropium indicum Linn is a leafy vegetable that has been used in Bangladeshi ethnomedicinal practices. The attenuation effect of H. indicum supplementation was evaluated in high carbohydrate high-fat (HCHF) diet-induced obesity and associated disorders in 8-weeks-old female Wister rats. H. indicum significantly (p < .05) prevented weight gain and improved glucose intolerance in obese rats. It also significantly (p < .05) ameliorated lipid parameters in HCHF diet fed rats preventing hypercholesterolemia and hypertriglyceridemia, resulting in improved the artherogenic index (AI). Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (ALP) activities were brought to normal by H. indicum. It significantly elevated superoxide dismutase (SOD) and catalase (CAT) activities as well as increased reduced glutathione (GSH) concentration in liver. The intense liver fat deposition was seen in HCHF fed rats which were relatively low in H. indicum fed rats. Therefore, H. indicum has the ability to prevent obesity and associated metabolic disorders. PRACTICAL APPLICATIONS: Obesity and associated metabolic disorders are the most common threats to public health. Modern lifestyle and food habits are the main causes behind this malice, and the introduction of functional foods in daily diet is proved to be highly beneficial. Results of this study demonstrated that H. indicum can effectively attenuate obesity and its associated metabolic complications. Therefore, the current study has the merits to promote scientific knowledge of the dietary application of H. indicum as a functional food among the community.

Background Garlic (Allium sativum L.) is a common herb consumed worldwide as functional food and traditional remedy for the prevention of infectious diseases since ancient time. Garlic and its active organosulfur compounds (OSCs) have been reported to alleviate a number of viral infections in pre-clinical and clinical investigations. However, so far no systematic review on its anti-viral effects and the underlying molecular mechanisms exists. Scope and approach The aim of this review is to systematically summarize pre-clinical and clinical investigations on antiviral effects of garlic and its OSCs as well as to further analyse recent findings on the mechanisms that underpin these antiviral actions. PubMed, Cochrane library, Google Scholar and Science Direct databases were searched and articles up to June 2020 were included in this review. Key findings and conclusions Pre-clinical data demonstrated that garlic and its OSCs have potential antiviral activity against different human, animal and plant pathogenic viruses through blocking viral entry into host cells, inhibiting viral RNA polymerase, reverse transcriptase, DNA synthesis and immediate-early gene 1(IEG1) transcription, as well as through downregulating the extracellular-signal-regulated kinase (ERK)/mitogen activated protein kinase (MAPK) signaling pathway. The alleviation of viral infection was also shown to link with immunomodulatory effects of garlic and its OSCs. Clinical studies further demonstrated a prophylactic effect of garlic in the prevention of widespread viral infections in humans through enhancing the immune response. This review highlights that garlic possesses significant antiviral activity and can be used prophylactically in the prevention of viral infections., Highlights • Garlic have anti-viral and immune boosting properties. • Dietary intake of garlic and garlic products is suggested as a source of anti-viral agents that can prevent viral infections as a prophylactic intervention. • The organosulfur constituents of garlic contribute in prevention of viral infections.

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.

Beta (β)-caryophyllene (BCAR) is a major sesquiterpene of various plant essential oils reported for several important pharmacological activities, including antioxidant, anti-inflammatory, anticancer, cardioprotective, hepatoprotective, gastroprotective, nephroprotective, antimicrobial, and immune-modulatory activity. Recent studies suggest that it also possesses neuroprotective effect. This study reviews published reports pertaining to the neuropharmacological activities of BCAR. Databases such as PubMed, Scopus, MedLine Plus, and Google Scholar with keywords "beta (β)-caryophyllene" and other neurological keywords were searched. Data were extracted by referring to articles with information about the dose or concentration/route of administration, test system, results and discussion, and proposed mechanism of action. A total of 545 research articles were recorded, and 41 experimental studies were included in this review, after application of exclusion criterion. Search results suggest that BCAR exhibits a protective role in a number of nervous system-related disorders including pain, anxiety, spasm, convulsion, depression, alcoholism, and Alzheimer's disease. Additionally, BCAR has local anesthetic-like activity, which could protect the nervous system from oxidative stress and inflammation and can act as an immunomodulatory agent. Most neurological activities of this natural product have been linked with the cannabinoid receptors (CBRs), especially the CB2R. This review suggests a possible application of BCAR as a neuroprotective agent.

Mitochondria are the powerhouse of cells, which upon dysfunctions may lead to several diseases. Mycotoxins are the toxic secondary metabolites from fungi which are capable of causing diseases and death in humans and animals. They have a versatile mechanism of action in biological systems and can be used as lead compounds to treat some diseases including cancer. The present work encompasses analysis on the effects of mycotoxins on mitochondrial dysfunction. Electronic databases such as PubMed, ScienceDirect, Scopus, Web of Science, and Google Scholar were thoroughly searched for up-to-date published information associated with those mycotoxins and their effect on mitochondrial dysfunction. Findings suggest that mycotoxins such as citrinin, aflatoxin, and T-2 toxin exert multi-edged sword-like effects in test systems causing mitochondrial dysfunction. Mycotoxins can induce oxidative stress even at low concentration/dose that may be one of the major causes of mitochondrial dysfunction. On the other hand, activation of apoptotic caspases and other proteins by mycotoxins may lead to apoptotic cell death. Thus, mycotoxins-mediated mitochondrial dysfunction may be related to several chronic diseases which also makes these mycotoxins considerable as lead compounds for inducing toxic effects in cells. Their cytotoxic effects on cancer cells suggest their possible application as chemotherapeutic tools. © 2018 IUBMB Life, 70(11):1084-1092, 2018.

A lectin with strong cytotoxic effect on human colon cancer HT29 and monkey kidney VERO cells was recently identified from the Australian indigenous mushroom Psathyrella asperospora and named PAL. We herein present its biochemical and structural analysis using a multidisciplinary approach. Glycan arrays revealed binding preference towards N-acetylglucosamine (GlcNAc) and, to a lesser extent, towards sialic acid (Neu5Ac). Submicromolar and millimolar affinity was measured by surface plasmon resonance for GlcNAc and NeuAc, respectively. The structure of PAL was resolved by X-ray crystallography, elucidating both the protein's amino acid sequence as well as the molecular basis rationalizing its binding specificity. Proteins 2017; 85:969-975. © 2016 Wiley Periodicals, Inc.

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.

In this article, we have summarized the biological sources and pharmacological activities of agathisflavone along with molecular docking studies to correlate the interaction of this biflavonoid and biomacromolecules involving in its biological effects observed in database-oriented scientific reports. For this, an up-to-date (from 1991 to October 2018) search was done on the databases such as PubMed, Science Direct, Web of Science, Scopus, The American Chemical Society, Clinicaltrials.gov, and Google Scholar databases. The findings suggest that agathisflavone possesses antioxidant, anti-inflammatory, antiviral, antiparasitic, cytotoxic, neuroprotective, and hepatoprotective activities. An in silico study of agathisflavone against 17 essential proteins/enzymes revealed that inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 are the most efficient enzymes for the interaction and binding of this biflavonoid for its anti-inflammatory activity. In conclusion, agathisflavone may be one of the promising plant-derived lead compounds in the treatment of oxidative stress, inflammatory diseases, microbial infection, hepatic and neurological diseases and disorders, and cancer. © 2019 IUBMB Life, 71(9):1192-1200, 2019.

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.

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.

© 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

Beta (β)-caryophyllene (BCAR) is a major sesquiterpene of various plant essential oils reported for several important pharmacological activities, including antioxidant, anti-inflammatory, anticancer, cardioprotective, hepatoprotective, gastroprotective, nephroprotective, antimicrobial, and immune-modulatory activity. Recent studies suggest that it also possesses neuroprotective effect. This study reviews published reports pertaining to the neuropharmacological activities of BCAR. Databases such as PubMed, Scopus, MedLine Plus, and Google Scholar with keywords "beta (β)-caryophyllene" and other neurological keywords were searched. Data were extracted by referring to articles with information about the dose or concentration/route of administration, test system, results and discussion, and proposed mechanism of action. A total of 545 research articles were recorded, and 41 experimental studies were included in this review, after application of exclusion criterion. Search results suggest that BCAR exhibits a protective role in a number of nervous system-related disorders including pain, anxiety, spasm, convulsion, depression, alcoholism, and Alzheimer's disease. Additionally, BCAR has local anesthetic-like activity, which could protect the nervous system from oxidative stress and inflammation and can act as an immunomodulatory agent. Most neurological activities of this natural product have been linked with the cannabinoid receptors (CBRs), especially the CB2R. This review suggests a possible application of BCAR as a neuroprotective agent.

Lectins are non-immunoglobulin proteins that bind diverse sugar structures with a high degree of selectivity. Lectins play crucial role in various biological processes such as cellular signaling, scavenging of glycoproteins from the circulatory system, cell–cell interactions in the immune system, differentiation and protein targeting to cellular compartments, as well as in host defence mechanisms, inflammation, and cancer. Among all the sources of lectins, plants have been most extensively studied. However, more recently fungal lectins have attracted considerable attention due to their antitumor, antiproliferative and immunomodulatory activities. Given that only 10% of mushroom species are known and have been taxonomically classified, mushrooms represent an enormous unexplored source of potentially useful and novel lectins. In this review we provide an up-to-date summary on the biochemical, molecular and structural properties of mushroom lectins, as well as their versatile applications specifically focusing on mushroom lectin bioactivity.

A lectin with strong cytotoxic effect on human colon cancer HT29 and monkey kidney VERO cells was recently identified from the Australian indigenous mushroom Psathyrella asperospora and named PAL. We herein present its biochemical and structural analysis using a multidisciplinary approach. Glycan arrays revealed binding preference towards N-acetylglucosamine (GlcNAc) and, to a lesser extent, towards sialic acid (Neu5Ac). Submicromolar and millimolar affinity was measured by surface plasmon resonance for GlcNAc and NeuAc, respectively. The structure of PAL was resolved by X-ray crystallography, elucidating both the protein's amino acid sequence as well as the molecular basis rationalizing its binding specificity. Proteins 2017; 85:969-975. © 2016 Wiley Periodicals, Inc.

A new N-acetyl-D-glucosamine (GlcNAc) specific lectin was identified and purified from the fruiting body of the Australian indigenous mushroom Psathyrella asperospora. The functional lectin, named PAL, showed hemagglutination activity against neuraminidase treated rabbit and human blood types A, B and O, and exhibited high binding specificity towards GlcNAc, as well as mucin and fetuin, but not against asialofetuin. PAL purified to homogeneity by a combination of ammonium sulfate precipitation, chitin affinity chromatography and size exclusion chromatography, was monomeric with a molecular mass of 41.8 kDa, was stable at temperatures up to 55 °C and between pH 6–10, and did not require divalent cations for optimal activity. De novo sequencing of PAL using LC-MS/MS, identified 10 tryptic peptides that revealed substantial sequence similarity to the GlcNAc recognizing lectins from Psathyrella velutina (PVL) and Agrocybe aegerita (AAL-II) in both the carbohydrate binding and calcium binding sites. Significantly, PAL was also found to exert a potent anti-proliferative effect on HT29 cells (IC50 0.48 μM) that was approximately 3-fold greater than that observed on VERO cells; a difference found to be due to the differential expression of cell surface GlcNAc on HT29 and VERO cells. Further characterization of this activity using propidium iodine staining revealed that PAL induced cell cycle arrest at G2/M phase in a manner dependent on its ability to bind GlcNAc.

Cyclotides are considered promising scaffolds for drug development owing to their inherent host defence activities and highly stable structure, defined by the cyclic cystine knot. These proteins are expressed as complex mixtures in plants. Although several methods have been developed for their isolation and analysis, purification of cyclotides is still a lengthy process. Here, we describe the use of affinity chromatography for the purification of cyclotides using polyclonal IgG antibodies raised in rabbits against cycloviolacin O2 and immobilized on NHS-activated Sepharose columns. Cycloviolacin O2 was used as a model substance to evaluate the chromatographic principle, first as a pure compound and then in combination with other cyclotides, that is, bracelet cyclotide cycloviolacin O19 and Möbius cyclotide kalata B1, and in a plant extract. We demonstrate that single-step purification of cyclotides by affinity chromatography is possible but cross reactivity may occur between homologue cyclotides of the bracelet subfamily.

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. Electronic supplementary material The online version of this article (doi:10.1007/s13596-016-0239-5) contains supplementary material, which is available to authorized users.

The methanolic extracts of the barks and pneumatophores of Xylocarpus moluccensis were assessed for their effects on the central nervous system (CNS) using a series of established pharmacological tests including pentobarbitone-induced sleeping time, open field, hole cross, hole-board and evasions tests in mice model. These extracts produced a dose-dependent reduction of the onset and duration of pentobarbitone-induced hypnosis, reduction of locomotor and exploratory activities in the open field, hole cross, head-dip and evasion tests. These results suggest that both the bark and pneumatophore extracts possess CNS depressant activity, the pneumatophore extract being more potent than the bark extract.

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.

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

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.

Cyclotides are considered promising scaffolds for drug development owing to their inherent host defence activities and highly stable structure, defined by the cyclic cystine knot. These proteins are expressed as complex mixtures in plants. Although several methods have been developed for their isolation and analysis, purification of cyclotides is still a lengthy process. Here, we describe the use of affinity chromatography for the purification of cyclotides using polyclonal IgG antibodies raised in rabbits against cycloviolacin O2 and immobilized on NHS-activated Sepharose columns. Cycloviolacin O2 was used as a model substance to evaluate the chromatographic principle, first as a pure compound and then in combination with other cyclotides, that is, bracelet cyclotide cycloviolacin O19 and Mobius cyclotide kalata B1, and in a plant extract. We demonstrate that single-step purification of cyclotides by affinity chromatography is possible but cross reactivity may occur between homologue cyclotides of the bracelet subfamily.

Ethanolic extract of Aphanamixis polystachya bark was used to investigate its analgesic activity by acetic acid induced writhing in mice. The bark extract exhibited statistically significant and dose dependent analgesic activity in mice. The bark extract at the doses of 250 and 500 mg/kg body weight showed 40.69% and 62.07% writhing inhibition respectively in mice whereas diclofenac-Na produced 75.17% writhing inhibition as a positive control.

A new N-acetyl-D-glucosamine (GlcNAc) specific lectin was identified and purified from the fruiting body of the Australian indigenous mushroom Psathyrella asperospora. The functional lectin, named PAL, showed hemagglutination activity against neuraminidase treated rabbit and human blood types A, B and O, and exhibited high binding specificity towards GlcNAc, as well as mucin and fetuin, but not against asialofetuin. PAL purified to homogeneity by a combination of ammonium sulfate precipitation, chitin affinity chromatography and size exclusion chromatography, was monomeric with a molecular mass of 41.8 kDa, was stable at temperatures up to 55 °C and between pH 6-10, and did not require divalent cations for optimal activity. De novo sequencing of PAL using LC-MS/MS, identified 10 tryptic peptides that revealed substantial sequence similarity to the GlcNAc recognizing lectins from Psathyrella velutina (PVL) and Agrocybe aegerita (AAL-II) in both the carbohydrate binding and calcium binding sites. Significantly, PAL was also found to exert a potent anti-proliferative effect on HT29 cells (IC50 0.48 μM) that was approximately 3-fold greater than that observed on VERO cells; a difference found to be due to the differential expression of cell surface GlcNAc on HT29 and VERO cells. Further characterization of this activity using propidium iodine staining revealed that PAL induced cell cycle arrest at G2/M phase in a manner dependent on its ability to bind GlcNAc.

In this study, ethyl acetate and aqueous fractions from 117 collections of Australian macrofungi belonging to the mushroom genus Cortinarius were screened for antimicrobial activity against Staphylococcus aureus and Pseudomonas aeruginosa. Overall, the lipophilic fractions were more active than the aqueous fractions. The ethyl acetate fractions of most or all collections of 13 species, namely Cortinarius ardesiacus, C. archeri, C. austrosaginus, C. austrovenetus, C. austroviolaceus, C. coelopus, C. [Dermocybe canaria](2), C. clelandii, C. [D. kula], C. memoria-annae, C. persplendidus, C. sinapicolor, C. vinosipes and forty seven collections of un-described Cortinarius species exhibited IC(50) values of 0.09 mg/mL against S. aureus. In contrast, most or all collections of only four species, namely C. abnormis, C. austroalbidus, C. [D. kula], C. persplendidus, and eleven un-described Cortinarius collections exhibited similar effects against P. aeruginosa (IC(50)or= 0.09 mg/mL). Anthraquinonoid pigments isolated from C. basirubescens together with emodin physcion and erythrogluacin were assessed for their antimicrobial activity. The fungal octaketides austrocortilutein, austrocortirubin, torosachrysone, physcion and emodin were found to strongly inhibit the growth of S. aureus (IC(50) 0.7-12 microg/mL) whereas only physcion and emodin exhibited potency against P. aeruginosa (IC(50) 1.5 and 2.0 microg/mL, respectively).