Publications by authors named "Mohammad S Mubarak"

114 Publications

Health promoting benefits of pongamol: An overview.

Biomed Pharmacother 2021 Aug 27;142:112109. Epub 2021 Aug 27.

Department of Chemistry, The University of Jordan, Amman 11942, Jordan. Electronic address:

Plant-derived chemicals are a source of novel chemotherapeutic agents. Throughout the human civilization, these novel chemicals have led to the discovery of new pharmacological active agents. Research on herbal medicine is of great importance, as most of the active agents used for treating numerous diseases are from natural sources, while other agents are either semisynthetic or synthetic. Pongamol, a flavonoid, which is the main constituent of Pongamia pinnata, is one such active agents, which exhibits diverse pharmacological activities. Various in vivo and in vitro studies revealed that pongamol is a potentially active agent, as it exerts anticancer, anti-inflammatory, antioxidant, antimicrobial, and anti-diabetic activities. Accordingly, the aim of the present review was to give an up-to-date overview on the chemistry, isolation, bioavailability, pharmacological activity, and health benefits of pongamol. This review focuses on the medicinal and health promoting activities of pongamol, along with possible mechanisms of action. For this purpose, this review summarizes the most recent literature pertaining to pongamol as a therapeutic agent against several diseases. In addition, the review covers information related to the toxicological assessment and safety of this phytochemical, and highlights the medicinal and folk values of this compound against various diseases and ailments.
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http://dx.doi.org/10.1016/j.biopha.2021.112109DOI Listing
August 2021

Genistein: An Integrative Overview of Its Mode of Action, Pharmacological Properties, and Health Benefits.

Oxid Med Cell Longev 2021 19;2021:3268136. Epub 2021 Jul 19.

Department of Clinical Pharmacy, University of Medicine and Pharmacy of Craiova, 200349 Craiova, Romania.

Genistein is an isoflavone first isolated from the brooming plant Dyer's L. and is widely distributed in the Fabaceae family. As an isoflavone, mammalian genistein exerts estrogen-like functions. Several biological effects of genistein have been reported in preclinical studies, such as the antioxidant, anti-inflammatory, antibacterial, and antiviral activities, the effects of angiogenesis and estrogen, and the pharmacological activities on diabetes and lipid metabolism. The purpose of this review is to provide up-to-date evidence of preclinical pharmacological activities with mechanisms of action, bioavailability, and clinical evidence of genistein. The literature was researched using the most important keyword "genistein" from the PubMed, Science, and Google Scholar databases, and the taxonomy was validated using The Plant List. Data were also collected from specialized books and other online resources. The main positive effects of genistein refer to the protection against cardiovascular diseases and to the decrease of the incidence of some types of cancer, especially breast cancer. Although the mechanism of protection against cancer involves several aspects of genistein metabolism, the researchers attribute this effect to the similarity between the structure of soy genistein and that of estrogen. This structural similarity allows genistein to displace estrogen from cellular receptors, thus blocking their hormonal activity. The pharmacological activities resulting from the experimental studies of this review support the traditional uses of genistein, but in the future, further investigations are needed on the efficacy, safety, and use of nanotechnologies to increase bioavailability and therapeutic efficacy.
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http://dx.doi.org/10.1155/2021/3268136DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8315847PMC
July 2021

Role of L. Fruits Extract in Combatting the Hematological and Hepatic Toxic Effects of Carbofuran.

Chem Res Toxicol 2021 Aug 15;34(8):1890-1902. Epub 2021 Jul 15.

Department of Pharmacy, Jahangirnagar University, Savar, Dhaka 1342, Bangladesh.

L. is rich in numerous vital bioactive constituents, though it is an underutilized among the citrus genus. Therefore, the aim of the present investigation was to evaluate the protective role of the fruit (CMF) methanol extract against carbofuran (CF)-induced toxicity in experimental rats. In addition, this work aims at detecting and measuring polyphenolic compounds by means of high-performance liquid chromatography (HPLC) and evaluation of the antioxidant activity of this extract. For this, studies dealing with serum hematological and biochemical parameters, liver endogenous antioxidants, as well as hepatic histo-architectural features have been carried out to assess the protective ability of CMF against CF-induced toxicity. Additionally, total phenol, flavonoid, and antioxidant capability were measured and the antioxidant action was investigated using DPPH and nitric oxide radical scavenging assays as well as reducing power assessments. HPLC results revealed the presence of benzoic acid, cinnamic acid, gallic acid, quercetin, and salicylic acid in CMF extract. Furthermore, results showed that CMF has considerable total phenol, flavonoid, and antioxidant capability and exhibits significant free radical scavenging and reducing potentialities. On the other hand, CF intoxication of rats significantly altered the hematological and serum biochemical parameters with hepatocytes disruption. Carbofuran also caused an upsurge in malondialdehyde (MDA) level and a decline in hepatic cellular antioxidant enzymes levels in rats compared to the control group. Co-administration of CMF amended the anomalies and improved the histo-architectural arrangement of hepatocytes in treated groups. CMF also inhibited the alteration of endogenous antioxidant enzymes and MDA levels as compared to the carbofuran treated group and returned them to their normal state. Taken all together, results from this investigation highlight the protective role of CMF against CF-induced toxicity which might be attributed to the polyphenolic constituents of the extract.
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http://dx.doi.org/10.1021/acs.chemrestox.1c00166DOI Listing
August 2021

Role of Withaferin A and Its Derivatives in the Management of Alzheimer's Disease: Recent Trends and Future Perspectives.

Molecules 2021 Jun 17;26(12). Epub 2021 Jun 17.

Department of Chemistry, The University of Jordan, Amman 11942, Jordan.

Globally, Alzheimer's disease (AD) is one of the most prevalent age-related neurodegenerative disorders associated with cognitive decline and memory deficits due to beta-amyloid deposition (Aβ) and tau protein hyperphosphorylation. To date, approximately 47 million people worldwide have AD. This figure will rise to an estimated 75.6 million by 2030 and 135.5 million by 2050. According to the literature, the efficacy of conventional medications for AD is statistically substantial, but clinical relevance is restricted to disease slowing rather than reversal. Withaferin A (WA) is a steroidal lactone glycowithanolides, a secondary metabolite with comprehensive biological effects. Biosynthetically, it is derived from (Ashwagandha) and (Gallinero) through the mevalonate and non-mevalonate pathways. Mounting evidence shows that WA possesses inhibitory activities against developing a pathological marker of Alzheimer's diseases. Several cellular and animal models' particulates to AD have been conducted to assess the underlying protective effect of WA. In AD, the neuroprotective potential of WA is mediated by reduction of beta-amyloid plaque aggregation, tau protein accumulation, regulation of heat shock proteins, and inhibition of oxidative and inflammatory constituents. Despite the various preclinical studies on WA's therapeutic potentiality, less is known regarding its definite efficacy in humans for AD. Accordingly, the present study focuses on the biosynthesis of WA, the epidemiology and pathophysiology of AD, and finally the therapeutic potential of WA for the treatment and prevention of AD, highlighting the research and augmentation of new therapeutic approaches. Further clinical trials are necessary for evaluating the safety profile and confirming WA's neuroprotective potency against AD.
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http://dx.doi.org/10.3390/molecules26123696DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8234716PMC
June 2021

Isolation, Biological Evaluation, and Molecular Docking Studies of Compounds from (Royle) Graham Ex Baker.

ACS Omega 2021 Jun 10;6(24):15911-15919. Epub 2021 Jun 10.

Department of Chemistry, The University of Jordan, Amman 11942, Jordan.

The is one of the best anti-inflammatory, antioxidant, and anticancerous plant; therefore, the isolated chemical constituents, that is, scopoletin (), pinitol (), 2-propenoic acid, 3-(3,4-dihydroxyphenyl)-octacosyl ester (), betulin (), and β-sitosterol glucoside () were tested for these folklores. The structures of the isolated compounds were confirmed by H NMR, C NMR, 2D-NMR, and mass spectral data. The anti-inflammatory, anticancer, antiglycation, and antioxidant activities of compounds were evaluated using different assays. Compound exhibited significant anti-inflammatory effect as it reduced edema of the paw (83.98%), which is more potent than the standard drug (ibuprofen) (which showed an inhibition percentage of 73.22% a), followed by compound . Furthermore, compound showed significant free-radical scavenging activity using the 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) free-radical assay. Percentage inhibition of DPPH recorded was 95.646 ± 0.003, 94.766 ± 0.014, and 94.516 ± 0.011% at concentrations of 400, 200, and 100 μg/mL, respectively. Evaluation of anticancer activity of isolated compounds reveals weak effect against HeLa and 3T3 cell lines. Docking studies of the most active compound into the binding sites of cyclooxygenase isoforms showed a better antagonistic potential against COX-1 than the COX-2 isoform.
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http://dx.doi.org/10.1021/acsomega.1c01532DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8223426PMC
June 2021

and Studies of Flavonoids Isolated from as Potential Antidiarrheal Agents.

ACS Omega 2021 Jun 14;6(24):15617-15624. Epub 2021 Jun 14.

Department of Pharmacology, Faculty of Health Science, University of Free State, Bloemfontein 9300, South Africa.

Pistacia integerrima leaf galls are used in several traditional medicines to cure many diseases such as diarrhea, asthma, fever, cough, vomiting, and hepatitis. The main goal of the present investigation was to assess the antidiarrheal effect of the extracts/fractions and four isolated flavonoid compounds () on mice. An assay involving castor-oil-induced diarrhea was used to evaluate the antidiarrheal potential of extracts/fractions at 100, 200, and 400 mg/kg p.o., as well as isolated compounds at 5, 10, and 20 mg/kg p.o. Pretreatment of mice with extracts/fractions significantly attenuated castor-oil-induced diarrhea in a dose-dependent manner. Among all crude extracts and fractions, the ethyl acetate extract was the most effective with 100% protection against diarrhea followed by chloroform (75% protection) at 400 mg/kg p.o. Although all the isolated compounds exhibited strong antidiarrheal activity, isolated compounds and demonstrated 100% protection against diarrhea. Moreover, docking models were performed using the Molecular Operating Environment (MOE) and AutoDock software and suggested that the extracts and isolated compounds exert antidiarrheal activity by inhibiting mu-opioid and delta-opioid receptors. Therefore, our finding affords a strong pharmacological basis for the traditional use of galls in the treatment of diarrhea.
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http://dx.doi.org/10.1021/acsomega.1c00298DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8223227PMC
June 2021

Natural-Derived Molecules as a Potential Adjuvant in Chemotherapy: Normal Cell Protectors and Cancer Cell Sensitizers.

Anticancer Agents Med Chem 2021 Jun 22. Epub 2021 Jun 22.

Department of Biochemistry and Molecular Biology, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, Bangladesh.

Background: Cancer is a global threat to humans and a leading cause of death worldwide. Cancer treatment includes, among other things, the use of chemotherapeutic agents, compounds that are vital for treating and preventing cancer. However, chemotherapeutic agents produce oxidative stress along with other side effects that would affect the human body.

Objective: To reduce the oxidative stress of chemotherapeutic agents in cancer and normal cells by naturally derived compounds with anti-cancer properties, and protect normal cells from the oxidation process. Therefore, the need to develop more potent chemotherapeutics with fewer side effects has become increasingly important.

Method: Recent literature dealing with the antioxidant and anticancer activities of the naturally naturally-derived compounds: morin, myricetin, malvidin, naringin, eriodictyol, isovitexin, daidzein, naringenin, chrysin, and fisetin has been surveyed and examined in this review. For this, data were gathered from different search engines, including Google Scholar, ScienceDirect, PubMed, Scopus, Web of Science, Scopus, and Scifinder, among others. Additionally, several patient offices such as WIPO, CIPO, and USPTO were consulted to obtain published articles related to these compounds.

Result: Numerous plants contain flavonoids and polyphenolic compounds such as morin, myricetin, malvidin, naringin, eriodictyol, isovitexin, daidzein, naringenin, chrysin, and fisetin, which exhibit ‎antioxidant, anti-inflammatory, and anti-carcinogenic actions via several mechanisms. These compounds show sensitizers of cancer cells and protectors of healthy cells. Moreover, these compounds can reduce oxidative stress, which is accelerated by chemotherapeutics and exhibit a potent anticancer effect on cancer cells.

Conclusions: Based on these findings, more research is recommended to explore and evaluate such flavonoids and polyphenolic compounds.
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http://dx.doi.org/10.2174/1871520621666210623104227DOI Listing
June 2021

Therapeutic perspectives of the black cumin component thymoquinone: A review.

Food Funct 2021 Jul 4;12(14):6167-6213. Epub 2021 Jun 4.

Department of Pharmacy, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj-8100, Bangladesh.

The dietary phytochemical thymoquinone (TQ), belonging to the family of quinones, mainly obtained from the black and angular seeds of Nigella sativa, is one of the promising monoterpenoid hydrocarbons, which has been receiving massive attention for its therapeutic potential and pharmacological properties. It plays an important role as a chemopreventive and therapeutic agent in the treatment of various diseases and illnesses. The aim of this review is to present a summary of the most recent literature pertaining to the use of TQ for the prevention and treatment of various diseases along with possible mechanisms of action, and the potential use of this natural product as a complementary or alternative medicine. Research findings indicated that TQ exhibits numerous pharmacological activities including antioxidant, anti-inflammatory, cardioprotective, hepatoprotective, antidiabetic, neuroprotective, and anticancer, among others. Conclusions of this review on the therapeutic aspects of TQ highlight the medicinal and folk values of this compound against various diseases and ailments. In short, TQ could be a novel drug in clinical trials, as we hope.
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http://dx.doi.org/10.1039/d1fo00401hDOI Listing
July 2021

Corrigendum: Immunomodulatory Effects of Diterpenes and Their Derivatives Through NLRP3 Inflammasome Pathway: A Review.

Front Immunol 2021 22;12:692302. Epub 2021 Apr 22.

Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol, Iran.

[This corrects the article DOI: 10.3389/fimmu.2020.572136.].
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http://dx.doi.org/10.3389/fimmu.2021.692302DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8101406PMC
April 2021

Superoxide dismutase: an updated review on its health benefits and industrial applications.

Crit Rev Food Sci Nutr 2021 Apr 27:1-19. Epub 2021 Apr 27.

Department of Chemistry, The University of Jordan, Amman, Jordan.

Many short-lived and highly reactive oxygen species, such as superoxide anion (O) and hydrogen peroxide (HO), are toxic or can create oxidative stress in cells, a response involved in the pathogenesis of numerous diseases depending on their concentration, location, and cellular conditions. Superoxide dismutase (SOD) activities as an endogenous and exogenous cell defense mechanism include the potential use in treating various diseases, improving the potential use in treating various diseases, and improving food-stuffs preparation dietary supplements human nutrition. Published work indicates that SOD regulates oxidative stress, lipid metabolism, inflammation, and oxidation in cells. It can prevent lipid peroxidation, the oxidation of low-density lipoprotein in macrophages, lipid droplets' formation, and the adhesion of inflammatory cells into endothelial monolayers. It also expresses antioxidant effects in numerous cancer-related processes. Additionally, different forms of SOD may also augment food processing and pharmaceutical applications, exhibit anticancer, antioxidant, and anti-inflammatory effects, and prevent arterial problems by protecting the proliferation of vascular smooth muscle cells. Many investigations in this review have reported the therapeutic ability and physiological importance of SOD. Because of their antioxidative effects, SODs are of great potential in the medicinal, cosmetic, food, farming and chemical industries. This review discusses the findings of human and animal studies that support the advantages of SOD enzyme regulations to reduce the formation of oxidative stress in various ways.
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http://dx.doi.org/10.1080/10408398.2021.1913400DOI Listing
April 2021

Evaluation of the anti-diarrheal effects of the whole plant extracts of Roxb in pigeons.

Toxicol Rep 2021 23;8:395-404. Epub 2021 Feb 23.

Department of Chemistry, The University of Jordan, Amman, 11942, Jordan.

Background: (dodder) belonging to the family Convolvulaceae has many ethno-medicinal uses such as antidiarrheal and antiemetic. This plant has been employed to treat diarrhea, where the antidiarrheal use of this plant is well established in different communities around the world without scientific bases. In addition, the antibacterial, anthelmintic, anticholinergic, and antihistaminic effects of this parasitic vine are partly responsible for the folkloric antidiarrheal use of this plant. In the present study, the antidiarrheal activity was evaluated in pigeons () using the juice (JCR), aqueous (CRAE), and methanol (CRME) extracts.

Methods: The antidiarrheal effect of was evaluated using different reported research models, with few modifications. In pigeons, diarrhea was induced by administration of castor oil (6 mL/kg, PO), ampicillin (250 mg/kg, IP), magnesium sulfate (2 gm/kg, PO), and cisplatin (6 mg/kg, IV). In these experiments, loperamide (2 mg/kg, IM) was used as a positive control, whereas JCR (1 mL/kg (1%) and 1 mL/kg (2%), CRAE (50, 100 and 200 mg/kg) and CRME (50, 100 and 200 mg/kg) were administered intramuscularly at different doses into each pigeon in the test groups.

Results: In addition to cisplatin-induced diarrhea, all paradigms tested gave significant results ( < 0.01). The JCR, at different doses, exhibited a significant ( < 0.01) a dose-dependent antidiarrheal effect on both the frequency and the onset of diarrhea. Similarly, CRAE and CRME, at doses of 100 and 200 mg/kg, showed considerable ( < 0.001) inhibition against the onset and frequency of diarrhea. On the other hand, JCR, CRAE, and CRME exerted significant effects ( < 0.001) on the percentage inhibition (PI) of diarrhea and gastrointestinal charcoal transit in a dose-dependent manner. In this respect, the maximum PI ( < 0.01) of JCR, CRAE, and CRME in different experimental paradigms was 43.13, 49.14, and 55.99 %, respectively.

Conclusions: Taken all together, results from this study reveal that the juice, aqueous, and methanol extract of exhibit significant anti-motility and anti-secretory potential. These findings may explain the medicinal use of folk medicine as an antidiarrheal medicinal plant.
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http://dx.doi.org/10.1016/j.toxrep.2021.02.013DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7921875PMC
February 2021

Evaluation of the Binding Affinity of Anti-Viral Drugs against Main Protease of SARS-CoV-2 through a Molecular Docking Study.

Infect Disord Drug Targets 2020 Dec 7. Epub 2020 Dec 7.

Department of Chemistry, The University of Jordan, Amman 11942. Jordan.

Background: Coronavirus disease 2019 (COVID-19) is a life intimidating viral infection caused by a positive sense RNA virus belonging to the Coronaviridae family, named severe acute respiratory distress syndrome coronavirus 2 (SARA-CoV-2). Since its outbreak in December 2019, the pandemic has spread to more than 200 countries, infected more than 26 million, and claimed the lives of more than 800,000 people. As a disease, COVID-19 can lead to severe and occasionally fatal respiratory problems in humans. Infection with this virus is associated with fever, cough, dyspnea, and muscle aches, and it may progress to pneumonia, multiple organ failure, and death. To date, there is no specific antiviral treatment against this virus. However, the main viral protease has been recently discovered and it is regarded as an appropriate target for antiviral agents in the search for treatment of COVID-19, due to its pivotal role in polyproteins processing during viral replication.

Aim: Consequently, this study intends to evaluate the effectiveness of FDA-approved anti-viral drugs against SARA-CoV-2 through a molecular docking study.

Methods: AutoDock Vina in PyRx platform was used for docking analysis against the main viral protease (Mpro) (PDB ID 6LU7), and Computed Atlas of Surface Topography of proteins (CASTp 3.0) was applied for detecting and characterizing cavities, pockets, and channels of this protein structure.

Results: Results revealed that among the conventional antiviral drugs, the protease inhibitors, lopinavir, amprenavir, indinavir, maraviroc, saquinavir, and daclatasvir showed high binding affinity and interacted with amino acid residues of the binding site.

Conclusion: In conclusion, protease inhibitors may be effective potential antiviral agents against Mpro to combat SARSCoV-2.
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http://dx.doi.org/10.2174/1871526520666201207124408DOI Listing
December 2020

Immunomodulatory Effects of Diterpenes and Their Derivatives Through NLRP3 Inflammasome Pathway: A Review.

Front Immunol 2020 25;11:572136. Epub 2020 Sep 25.

Zabol Medicinal Plants Research Center, Zabol University of Medical Sciences, Zabol, Iran.

Nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing protein (NLRP) inflammasomes are involved in the molecular pathogenesis of many diseases and disorders. Among NLRPs, the NLRP3 (in humans encoded by the gene) is expressed predominantly in macrophages as a component of the inflammasome and is associated with many diseases, including gout, type 2 diabetes, multiple sclerosis, atherosclerosis, and neurological diseases and disorders. Diterpenes containing repeated isoprenoid units in their structure are a member of some essential oils that possess diverse biological activities and are becoming a landmark in the field of drug discovery and development. This review sketches a current scenario of diterpenes or their derivatives acting through NLRPs, especially NLRP3-associated pathways with anti-inflammatory effects. For this, a literature survey on the subject has been undertaken using a number of known databases with specific keywords. Findings from the aforementioned databases suggest that diterpenes and their derivatives can exert anti-inflammatory effects NLRPs-related pathways. Andrographolide, triptolide, kaurenoic acid, carnosic acid, oridonin, teuvincenone F, and some derivatives of tanshinone IIA and phorbol have been found to act through NLRP3 inflammasome pathways. In conclusion, diterpenes and their derivatives could be one of the promising compounds for the treatment of NLRP3-mediated inflammatory diseases and disorders.
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http://dx.doi.org/10.3389/fimmu.2020.572136DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7546345PMC
June 2021

Ethnomedicinal documentation and anti-inflammatory effects of n-butanol extract and of four compounds isolated from the stems of Pituranthos scoparius: An in vitro and in vivo investigation.

J Ethnopharmacol 2021 Mar 20;267:113488. Epub 2020 Oct 20.

Department of Chemistry, The University of Jordan, Amman, 11942, Jordan; Department of Chemistry, Indiana University, Bloomington, IN, 47405, United States. Electronic address:

Ethnopharmacological Relevance: Pituranthos scoparius is a medicinal plant belonging to the Apiaceae family. It thrives in North Africa, and is widely distributed in the high plateau of most parts of the Sahara in Algeria. This plant is widely used in the Algerian traditional medicine to treat numerous infectious diseases, dermatoses, nervous breakdowns, digestive disorders, and calm abdominal pain.

Aim Of The Study: The aim of the present work was to examine the ethnomedicinal uses of Pituranthos scoparius in Setif region, Algeria, isolate and identify the chemical constituents of the n-butanol stem extract of P. scoparius (BEPS), and to determine the toxicity and anti-inflammatory effects of these compounds in addition to the extract.

Materials And Methods: The anti-inflammatory effects of BEPS and the four compounds isolated from the extract were evaluated using the in vitro protein denaturation assay, whereas the topical anti-inflammatory activity was assessed using the croton oil-induced ear edema in mice. Toxicity was determined based on assessment of in vitro cytotoxicity using hemolytic activity against human red blood cells (RBCs).

Results: Four compounds, identified as the rare isorhamnetin-3-O-β-apiofuranosyl (1 → 2)-β glucopyranoside (2), in addition to three known compounds, namely isorhamnetin-3-O-β-glucoside (1), D-mannitol (3), and isorhamnetin-3-O-β-glucopyranosyl-(1 → 6)-β-glucopyranoside (4) were isolated from BEPS. These compounds were characterized by means of NMR and high-resolution mass spectral (HRMS) data. These four compounds were isolated for the first time from this traditional Algerian medicinal plant. Screening of the extract indicated the presence of alkaloids, polyphenols, flavonoids, free quinones, coumarins and tannins. Topical anti-inflammatory effect showed that the four isolated compounds, as well as BEPS, exhibit a significant (p < 0.05) dose-dependent (0.5 and 1 mg/ear) anti-inflammatory effect. At a dose of 1 mg/ear, compounds 1, 2, and 4, exhibited remarkable anti-inflammatory effect with a percentage inhibition of 85.50 ± 2.78, 79.78 ± 4.68, and 75.78 ± 2.98%, respectively. Results from in vitro cytotoxicity showed that the % lysis of the extract, along with isolated compounds was found to be virtually nontoxic.

Conclusions: These results suggest that BEPS and isolated compounds are safe, nontoxic, and exert remarkable anti-inflammatory effects, and can be new sources of natural anti-inflammatory agents.
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http://dx.doi.org/10.1016/j.jep.2020.113488DOI Listing
March 2021

Curcumin and its Multi-target Function Against Pain and Inflammation: An Update of Pre-clinical Data.

Curr Drug Targets 2021 ;22(6):656-671

Department of Chemistry, The University of Jordan, Amman 11942, Jordan.

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.
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http://dx.doi.org/10.2174/1389450121666200925150022DOI Listing
January 2021

Recent Advances in the Synthesis and Biological Activity of 8-Hydroxyquinolines.

Molecules 2020 Sep 21;25(18). Epub 2020 Sep 21.

Department of Chemistry, School of Science, The University of Jordan, Amman 11942, Jordan.

Compounds containing the 8-hydroxyquinoline (8-HQ) nucleus exhibit a wide range of biological activities, including antimicrobial, anticancer, and antifungal effects. The chemistry and biology of this group have attracted the attention of chemists, medicinal chemists, and professionals in health sciences. A number of prescribed drugs incorporate this group, and numerous 8-HQ- based molecules can be used to develop potent lead compounds with good efficacy and low toxicity. This review focusses on the recent advances in the synthesis of 8-HQ derivatives with different pharmacological properties, including anticancer, antiviral, and antibacterial activities. For this purpose, recent relevant references were searched in different known databases and search engines, such as MEDLINE (PubMed), Google Scholar, Science Direct, Scopus, Cochrane, Scientific Information Database (SID), SciFinder, and Institute for Scientific Information (ISI) Web of Knowledge. This review article provides a literature overview of the various synthetic strategies and biological activities of 8-HQ derivatives and covers the recent related literature. Taken together, compounds containing the 8-HQ moiety have huge therapeutic value and can act as potential building blocks for various pharmacologically active scaffolds. In addition, several described compounds in this review could act leads for the development of drugs against numerous diseases including cancer.
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http://dx.doi.org/10.3390/molecules25184321DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7571046PMC
September 2020

Piperine: A review of its biological effects.

Phytother Res 2021 Feb 14;35(2):680-700. Epub 2020 Sep 14.

Department of Chemistry, The University of Jordan, Amman, Jordan.

Medicinal plants have been used for years as a source of food, spices, and, in traditional medicine, as a remedy to numerous diseases. Piper nigrum, belonging to the family Piperaceae is one of the most widely used spices all over the world. It has a distinct sharp flavor attributed to the presence of the phytochemical, piperine. Apart from its use as a spice, P. nigrum is frequently used for medicinal, preservation, and perfumery purposes. Black pepper contains 2-7.4% of piperine, varying in content is associated with the pepper plant. Piperine displays numerous pharmacological effects such as antiproliferative, antitumor, antiangiogenesis, antioxidant, antidiabetic, anti-obesity, cardioprotective, antimicrobial, antiaging, and immunomodulatory effects in various in vitro and in vivo experimental trials. Furthermore, piperine has also been documented for its hepatoprotective, anti-allergic, anti-inflammatory, and neuroprotective properties. This review highlights and discusses the medicinal and health-promoting effects of piperine, along with possible mechanisms of its action in health promotion and disease prevention. In addition, the present review summarizes the recent literature related to piperine as a therapeutic agent against several diseases.
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http://dx.doi.org/10.1002/ptr.6855DOI Listing
February 2021

Anti-inflammatory and In Silico Docking Studies of Heterophragma adenophyllum Seem Stem Constituents.

Inflammation 2021 Feb 8;44(1):297-306. Epub 2020 Sep 8.

Laboratory of Biological Control and Antimicrobial Resistance, Orel State University named after I.S. Turgenev, Orel City, 302026, Russia.

Heterophragma adenophyllum is a traditional medicinal plant that has been used as anti-inflammatory and to relief muscular tension. In the current research, four isolated constitutes namely lapacho (1), peshawaraquinone (2), indanone derivatives (3), α-lapachone (4) of H. adenophyllum were tested for anti-inflammatory effect using the carrageenan- and histamine-induced paw edema paradigm. The tested compounds (1-4) were evaluated for anti-inflammatory effect during the early and late phase of edema induction. In the early phase, all tested compounds (0.5 2.5 mg/kg each i.p.) demonstrated less than 50% effect, while in the later phase, compounds (2 and 3) demonstrated 85.66 and 89.87% attenuation. In addition, compounds (1-4) were subjected to histamine-induced inflammation, where compounds 2 and 3 exhibited excellent effects 86.87 and 89.98%, respectively at 5 mg/kg after the 2nd hour of administration, whereas compounds 1 and 4 did not exhibit any significant effect as compared with the negative control. Molecular docking results revealed a very high potency of compound based on the protein-ligand interaction (PLI) profile, which was further evaluated through a molecular dynamic simulation study. Therefore, the anti-inflammatory effect of H. adenophyllum attributed to the presence of these bioactive compounds (1-4) strongly supports the traditional uses of H. adenophyllum for treatment of inflammation. However, compounds 2 and 3 which exerted anti-inflammatory effect must be subjected for further mechanistic studies.
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http://dx.doi.org/10.1007/s10753-020-01333-7DOI Listing
February 2021

Citrinin against breast cancer: A cytogenotoxicological study.

Phytother Res 2021 Jan 31;35(1):504-516. Epub 2020 Aug 31.

Northeast Biotechnology Network (RENORBIO), Postgraduate Program in Biotechnology, Federal University of Piauí - UFPI, Teresina, Piauí, Brazil.

Breast cancer is one of the most lethal types of cancer and a leading cause of mortality among Women worldwide. Citrinin (CIT), a polyketide extracted from the fungus Penicillium citrinum, exhibits a wide range of biological activities such as antibacterial, antifungal, and cytotoxic effects. The aim of the current study was to evaluate the antitumoral effects of CIT against 7,12-dimethylbenzanthracene (DMBA)-induced mammary carcinoma in Swiss mice For this, CIT, DMBA and the standard cyclophosphamide (CPA) induced behavioral changes in experimental animals, and these changes were screened by using the rota rod and open field tests. Additionally, hematological, biochemical, immuno-histochemical, and histopathological analyses were carried out. Results suggest that CIT did not alter behavioral, hematological, and biochemical parameters in mice. DMBA induced invasive mammary carcinoma and showed genotoxic effects in the breasts, bone marrow, lymphocytes, and hepatic cells. It also caused mutagenic effects in the formation of micronuclei, bridges, shoots, and binucleate cells in bone marrow and liver. CIT and CPA genotoxic effects were observed after 3 weeks of therapy, where CIT exhibited a repair capacity and induced significant apoptotic damage in mouse lymphocytes. In conclusion, CIT showed antitumoral effects in Swiss mice, possibly through induction of apoptosis.
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http://dx.doi.org/10.1002/ptr.6830DOI Listing
January 2021

Anti-Inflammatory, Antinociceptive, and Antioxidant Properties of Anacardic Acid in Experimental Models.

ACS Omega 2020 Aug 29;5(31):19506-19515. Epub 2020 Jul 29.

RENORBIO - Post-Graduation Program in Biotechnology, Federal University of Piauí, Teresina 64049-550, Piauí, Brazil.

Anacardic acid (AA), a compound extracted from cashew nut liquid, exhibits numerous pharmacological activities. The aim of the current investigation was to assess the anti-inflammatory, antinociceptive, and antioxidant activities of AA in mouse models. For this, Swiss albino mice were pretreated with AA (10, 25, 50 mg/kg, intraperitoneally, ip) 30 min prior to the administration of carrageenan, as well as 25 mg/kg of prostaglandin E2, dextran, histamine, and compound 48/80. The antinociceptive activity was evaluated by formalin, abdominal, and hot plate tests, using antagonist of opioid receptors (naloxene, 3 mg/kg, ip) to identify antinociceptive mechanisms. Results from this study revealed that AA at 25 mg/kg inhibits carrageenan-induced edema. In addition, AA at 25 mg/kg reduced edema and leukocyte and neutrophilic migration to the intraperitoneal cavity, diminished myeloperoxidase activity and malondialdehyde concentration, and increased the levels of reduced glutathione. In nociceptive tests, it also decreased licking, abdominal writhing, and latency to thermal stimulation, possibly via interaction with opioid receptors. Taken together, these results indicate that AA exhibits anti-inflammatory and antinociceptive actions and also reduces oxidative stress in acute experimental models, suggesting AA as a promising compound in the pharmaceutical arena.
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http://dx.doi.org/10.1021/acsomega.0c01775DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7424580PMC
August 2020

Biogenically Synthesized Polysaccharides-Capped Silver Nanoparticles: Immunomodulatory and Antibacterial Potentialities Against Resistant .

Front Bioeng Biotechnol 2020 21;8:643. Epub 2020 Jul 21.

Department of Chemistry, The University of Jordan, Amman, Jordan.

Bacterial infections are the key cause of death in patients suffering from burns and diabetic wounds while the use of traditional antibiotics has been growing steadily. Thus, in the present study, we are trying to introduce a paradigm shift strategy to improve chronic wound healing of bacterial infection. To that end, we have biologically synthesized silver nanoparticles (AgNPs) using polysaccharides, and evaluated their antibacterial efficacy with their safety pattern. Scanning electron micrographs showed spherical AgNPs coated with algal polysaccharides with an approximate size of 9.7 nm. Treatment of with the AgNPs (0.5-1 μg/mL) resulted in a significant disruption in outer membrane, reduction in biofilm formation, and a significant decrease of production of alginate and pyocyanin along with a concentration-dependent reduction in β-lactamase activity. In addition, at the level, AgNPs displayed substantial activity to control infections in rat skin wounds with significant reduction in in COX-2 enzyme in both rat skin homogenate and serum samples. Furthermore, AgNPs facilitated wound curative in the infected model by reducing the hemorrhagic areas number and the infiltrated inflammatory cells. Taken all together, these biogenic nanoparticles showed unique properties in controlling bacterial wound infections and improving the healing process of damaged tissues via its direct and indirect effects.
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http://dx.doi.org/10.3389/fbioe.2020.00643DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7391905PMC
July 2020

Density functional theory, molecular docking and muscle relaxant, sedative, and analgesic studies of indanone derivatives isolated from .

J Biomol Struct Dyn 2020 Aug 5:1-12. Epub 2020 Aug 5.

Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, China.

(HA) is an important medicinal plant which is used in traditional medicine for the treatment of muscular tension and pain. Herein, we report the isolation of methyl,1,2-dihydroxy-2-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-indene-1-carboxylate (), from the roots of The isolated compound was evaluated for muscle relaxant, sedative, and analgesic potential in Swiss albino mice. Results revealed that the isolated compound exhibited a dose- and time-dependent muscle coordination (51%) and a significant ( < 01) sedative effect. It also showed a considerable ( < 0.5) analgesia after 30 min of post treatment and was maintained for up-to 120 min of experimental duration. In acute toxicity studies, no mortality was observed which indicates a preliminary safety of compound . Furthermore, the experimental results were compared with the theoretical studies by using density functional theory (DFT). The stability of the compound as well as the flow of electrons was determined by the calculated Frontier orbital analysis. The calculated stretching frequencies, H-NMR/C-NMR chemical shift values and UV-visible spectra were found to be in agreement with experimental values. The results obtained from molecular docking studies were used to explore the mechanism of analgesic and muscle relaxant activity.Communicated by Ramaswamy H. Sarma.
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http://dx.doi.org/10.1080/07391102.2020.1802343DOI Listing
August 2020

A Perspective on Emerging Therapeutic Interventions for COVID-19.

Front Public Health 2020 3;8:281. Epub 2020 Jul 3.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Coronaviruses are enveloped positive-sense RNA viruses with an unusual large RNA genome and a unique replication mechanism, which are characterized by club-like spikes that protrude from their surface. An outbreak of a novel coronavirus 2019 infection has posed significant threat to the health and economies in the whole world. This article reviewed the viral replication, pathogenicity, prevention and treatment strategies. With a lack of approved treatment options for this virus, alternative approaches to control the spread of disease is in urgent need. This article also covers some management strategies which may be applied to this virus outbreak. Ongoing clinical studies related to possible treatments for COVID-19, potential vaccines, and alternative medication such as natural compounds are also discussed.
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http://dx.doi.org/10.3389/fpubh.2020.00281DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7362761PMC
January 2021

In vivo analgesic, anti-inflammatory, and sedative activity and a molecular docking study of dinaphthodiospyrol G isolated from Diospyros lotus.

BMC Complement Med Ther 2020 Jul 25;20(1):237. Epub 2020 Jul 25.

Department of Chemistry, The University of Jordan, Amman, 11942, Jordan.

Background: Analgesic, anti-inflammatory, and sedative drugs are available with potential side effects such as peptic ulcer and addiction among other things. In this regard, research is underway to find safe, effective, and economical drugs free of these side effects. In this study, an isolated natural product from Diospyros lotus, was tested for the aforementioned bioactivities.

Objectives: To evaluate analgesic, anti-inflammatory, and sedative potential of D. lotus extracts in animal paradigms using BALB/c mice as experimental model.

Methods: Analgesic, anti-inflammatory and sedative activities of dinaphthodiospyrol G (1) isolated from the chloroform fraction of D. lotus were evaluated using different experimental procedures. Anti-inflammatory effect was evaluated using the carrageenan and histamine-induced paw edema, whereas the antinociceptive effect was quantified by means of the hot plate analgesiometer. On the other hand, the sedative effect was determined using animal assay for screening the locomotors effects of compound 1. Compound 1 was also subjected to molecular modeling studies against cyclooxygenase enzymes.

Results: Results from this investigation showed that the extract is devoid of anti-inflammatory and antinociceptive potentials but has a significant sedative effect, whereas the tested compound exhibited 55.23 and 78.34% attenuation in paw edema by carrageenan and histamine assays, respectively. A significant (p < 0.001) and dose-dependent antinociceptive and sedative effects were demonstrated by the isolated compound. Molecular docking and dynamics simulation studies of the isolated compound against cyclooxygenase enzyme indicated that compound 1 forms specific interactions with key residues in the active site of the target receptor, which validates the potential use of the isolated compound as cyclooxygenase inhibitor.

Conclusions: Compound 1 exhibited remarkable analgesic, anti-inflammatory, and sedative activities. These findings strongly justify the traditional use of D. lotus in the treatment of inflammation, pain, and insomnia.
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http://dx.doi.org/10.1186/s12906-020-03030-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7382863PMC
July 2020

Electrosynthesis of a Biaurone by Controlled Dimerization of Flavone: Mechanistic Insight and Large-Scale Application.

J Org Chem 2020 08 2;85(16):10658-10669. Epub 2020 Aug 2.

Department of Chemistry, Indiana University, Bloomington, Indiana 47405, United States.

The electrochemistry of flavone () has been carefully investigated at glassy carbon cathodes in dimethylformamide containing 0.10 M tetra--butylammonium tetrafluoroborate as supporting electrolyte. In this medium, a cyclic voltammogram for a reduction of exhibits a reversible cathodic process ( = -1.58 V and = -1.47 V vs SHE) that is followed by an irreversible cathodic peak ( = -2.17 V vs SHE). When water (5.0 M) is introduced into the medium, the first peak for becomes irreversible ( = -1.56 V vs SHE), and the second (irreversible) peak shifts to -2.07 V vs SHE. Bulk electrolyses of at -1.60 V vs SHE afford flavanone, 2'-hydroxychalcone, 2'-hydroxy-3-phenylpropionate, and two new compounds, namely ()-1,6-bis(2-hydroxyphenyl)-3,4-diphenylhex-3-ene-1,6-dione () and ()-2,2'-(1,2-diphenylethene-1,2-bis(benzofuran-3(2))-one) (), obtained in significant amounts, that were characterized by means of H and C NMR spectrometry as well as single-crystal X-ray diffraction. Along with the above findings, we have proposed a mechanism for the electroreduction of , which has been further corroborated by our quantum mechanical study.
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http://dx.doi.org/10.1021/acs.joc.0c01220DOI Listing
August 2020

Phytol anti-inflammatory activity: Pre-clinical assessment and possible mechanism of action elucidation.

Cell Mol Biol (Noisy-le-grand) 2020 Jun 25;66(4):264-269. Epub 2020 Jun 25.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Phytol (PHY) is an acyclic natural diterpene alcohol and a chlorophyll constituent that exhibits several pharmacological effects, such as anticancer, antioxidant, and antimicrobial. Here, we aimed to assess the PHY anti-inflammatory effect in vitro and in vivo, and to deepen knowledge on the possible mechanism of action. For this purpose, egg albumin (in vitro) test was performed by using acetyl salicylic acid (ASA) as a standard nonsteroidal anti-inflammatory drugs (NSAID). For in vivo test, male Wistar albino rats were treated (intraperitoneally) with 100 mg/kg of PHY and/or standard NSAIDs ASA (100 mg/kg) and diclofenac sodium (Diclo-Na, 10 mg/kg) to evaluate the combined effect of PHY in formalin-induced paw edema model. Furthermore, an in silico (CADD) study was accomplished to assess the effect of PHY against cyclooxygenase (COX)-1 and 2 enzymes, nuclear factor kappa B (NF-κB), and interleukin-1β (IL-1β). Results revealed that PHY exhibits dose-dependent anti-inflammatory effect using the egg albumin method. PHY (100 mg/kg) co-treated with ASA and/or Diclo-Na reduced paw edema better than PHY alone or NSAIDs individual groups. Computational study showed that PHY efficiently interacts with COX-1 and 2, NF-κB, and IL-1β. In conclusion, PHY exhibits anti-inflammatory activity, possibly via COX-1 and 2, NF-κB, and IL-1β dependent pathways.
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June 2020

Anti-diarrheal activities of phytol along with its possible mechanism of action through in-vivo and in-silico models.

Cell Mol Biol (Noisy-le-grand) 2020 Jun 25;66(4):243-249. Epub 2020 Jun 25.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Phytol (PHY), a chlorophyll-derived diterpenoid, exhibits numerous pharmacological properties, including antioxidant, antimicrobial, and anticancer activities. This study evaluates the anti-diarrheal effect of phytol (PHY) along with its possible mechanism of action through in-vivo and in-silico models. The effect of PHY was investigated on castor oil-induced diarrhea in Swiss mice by using prazosin, propranolol, loperamide, and nifedipine as standards with or without PHY. PHY at 50 mg/kg (p.o.) and all other standards exhibit significant (p < 0.05) anti-diarrheal effect in mice. The effect was prominent in the loperamide and propranolol groups. PHY co-treated with prazosin and propranolol was found to increase in latent periods along with a significant reduction in diarrheal section during the observation period than other individual or combined groups. Furthermore, molecular docking studies also suggested that PHY showed better interactions with the α- and β-adrenergic receptors, especially with α-ADR1a and β-ADR1. In the former case, PHY showed interaction with hydroxyl group of Ser192 at a distance of 2.91Å, while in the latter it showed hydrogen bond interactions with Thr170 and Lys297 with a distance of 2.65 and 2.72Å, respectively. PHY exerted significant anti-diarrheal effect in Swiss mice, possibly through blocking α- and β-adrenergic receptors.
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June 2020

Ascorbic acid antagonizes the sedative effect of diazepam possibly through inhibition of GABA(Aρ₁) and GABA(B1) receptors.

Cell Mol Biol (Noisy-le-grand) 2020 Jun 25;66(4):15-19. Epub 2020 Jun 25.

Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.

Gamma-aminobutyric acid (GABA) receptors belong to a ligand-gated ion channels family and are markedly expressed at the axon terminals of retinal bipolar cells. Ascorbic acid (AA), a known and vital antioxidant in the brain can modulate GABA receptors. We postulate that AA would antagonize benzodiazepines' effect via GABA receptor(s) interacting pathway. Here, we evaluated the modulatory sedative effect of AA on diazepam (DZP)'s anxiolytic effects in Swiss albino mice. The anxiolytic study was accomplished by using open-field, hole-board, and by swing and light-dark tests taking DZP as a standard anxiolytic drug. To understand the possible modulatory effects of AA, animals were co-administered with AA and DZP and/or its antagonist flumazenil (FLU). Additionally, an in-silico study was undertaken against GABA(A1), GABA(B1), and GABA(Aρ₁) receptors. Data suggest that AA at 25 mg/kg (i.p.) increased (p<0.05) the number of field cross, rearing, number of hole cross, and swing and residence, while decreased grooming and dark residence parameters as compared to the control and DZP groups. In addition, AA and/or FLU combined with DZP (2 mg/kg, i.p.) reversed DZP-mediated sedative effects in mice. Results from in silico study suggest that AA has good interactions with GABA(Aρ₁) and GABA(B1) receptors. In conclusion, DZP is a GABA receptor agonist and AA may reverse DZP-mediated sedative effects in a non-competitive binding fashion in mice through inhibition of GABA(Aρ₁) and GABA(B1) receptors.
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June 2020

Anticancer Perspectives on the Fungal-Derived Polyphenolic Hispolon.

Anticancer Agents Med Chem 2020 ;20(14):1636-1647

Department of Chemistry, The University of Jordan, Amman 11942, Jordan

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.
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http://dx.doi.org/10.2174/1871520620666200619164947DOI Listing
June 2021

Chemical profile and therapeutic potentials of Xylocarpus moluccensis (Lam.) M. Roem.: A literature-based review.

J Ethnopharmacol 2020 Sep 16;259:112958. Epub 2020 May 16.

Department of Chemistry, The University of Jordan, Amman, 11942, Jordan. Electronic address:

Ethnopharmacological Relevance: Historically, mangrove plants are among the potential sources of foods and remedies for humans living in the forests and nearby communities. Xylocarpus moluccensis (Lam.) M. Roem., an important mangrove medicinal plant, has been traditionally used for many purposes such as treatment of fever, dysentery, diarrhea, swelling, and abdominal disorders. The aim of the present work was to summarize the chemical reports and biological activities of the mangrove medicinal plant X. moluccensis based on information collected from different databases.

Materials And Methods: An up-to-date search (till Aug 2019) was carried out in databases such as PubMed, Science Direct, Google Scholar, and various patient offices (e.g., WIPO, CIPO, USPTO) using the keywords: 'Xylocarpus moluccensis', and/or paired with 'ethnobotanical use', and 'phytochemical'. In vitro, ex vivo, or in vivo studies were included.

Results: Findings suggest that X. moluccensis contains various important minerals and phytochemicals, where flavonoids, terpenes and terpenoids are the most prominent isolated phyto-constituents of X. moluccensis. Extracts/fractions or isolated compounds from this plant possess diverse biological activities, including anti-inflammatory, anti-microbial, antineoplastic, anti-diarrheal, insecticidal, anti-feedant, neuropharmacological (e.g., central nervous system depressant), anti-atherosclerotic, and lipid-lowering activity. Only one report suggests that the methanol and aqueous extracts of this plant did not exert cytotoxic effects on normal mouse fibroblast cells. However, no clinical studies were reported.

Conclusions: Taken all together, X. moluccensis may be one of the best sources of pharmacologically active lead compounds. More research, however, is necessary to establish the safety and efficacy, and its toxicogenetic effects in animal models.
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http://dx.doi.org/10.1016/j.jep.2020.112958DOI Listing
September 2020
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