Publications by authors named "Raffaele Capasso"

137 Publications

Isolation, Characterization and Neuroprotective Activity of Folecitin: An In Vivo Study.

Life (Basel) 2021 Aug 12;11(8). Epub 2021 Aug 12.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

Neurodegenerative diseases (NDs) extend the global health burden. Consumption of alcohol as well as maternal exposure to ethanol can damage several neuronal functions and cause cognition and behavioral abnormalities. Ethanol induces oxidative stress that is linked to the development of NDs. Treatment options for NDs are yet scarce, and natural product-based treatments could facilitate ND management since plants possess plenty of bioactive metabolites, including flavonoids, which typically demonstrate antioxidant and anti-inflammatory properties. is an important traditional medicinal plant used for hepatitis, gastric ulcer, external wounds, and other gastrointestinal disorders. However, it also possesses multiple bioactive compounds and antioxidant properties, but the evaluation of isolated pure compounds for neuroprotective efficacy has not been done yet. Therefore, in the current study, we aim to isolate and characterize the bioactive flavonoid folecitin and evaluate its neuroprotective activity against ethanol-induced oxidative-stress-mediated neurodegeneration in the hippocampus of postnatal day 7 (PND-7) rat pups. A single dose of ethanol (5 g/kg body weight) was intraperitoneally administered after the birth of rat pups on PND-7. This caused oxidative stress accompanied by the activation of phosphorylated-c-Jun N-terminal kinase (p-JNK), nod-like receptor family pyrin domain containing 3 (NLRP3), apoptosis-associated speck-like protein (ASC), and cysteine-aspartic acid protease-1 (caspase-1) proteins to form a complex called the NLRP3-inflammasome, which converts pro-interleukin 1 beta (IL-1B) to activate IL-1B and induce widespread neuroinflammation and neurodegeneration. In contrast, co-administration of folecitin (30 mg/kg body weight) reduced ethanol-induced oxidative stress, inhibited p-JNK, and deactivated the NLRP3-inflammasome complex. Furthermore, folecitin administration reduced neuroinflammatory and neurodegenerative protein markers, including decreased caspase-3, BCL-2-associated X protein (BAX), B cell CLL/lymphoma 2 (BCL-2), and poly (ADP-ribose) polymerase-1 (PARP-1) expression in the immature rat brain. These findings conclude that folecitin is a flavone compound, and it might be a novel, natural and safe agent to curb oxidative stress and its downstream harmful effects, including inflammasome activation, neuroinflammation, and neurodegeneration. Further evaluation in a dose-dependent manner would be worth it in order to find a suitable dose regimen for NDs.
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http://dx.doi.org/10.3390/life11080825DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8400650PMC
August 2021

Peripheral Artery Disease and Abdominal Aortic Aneurysm: The Forgotten Diseases in COVID-19 Pandemic. Results from an Observational Study on Real-World Management.

Medicina (Kaunas) 2021 Jun 29;57(7). Epub 2021 Jun 29.

Department of Translational Medical Sciences, Section of Cardiology, University of Campania "Luigi Vanvitelli", 80131 Naples, Italy.

: It is well established that patients with peripheral artery disease (PAD) as well abdominal aortic aneurysm (AAA) have an increased cardiovascular (CV) mortality. Despite this higher risk, PAD and AAA patients are often suboptimality treated. This study assessed the CV profile of PAD and AAA patients, quantifying the survival benefits of target-based risk-factors modification even in light of the COVID-19 pandemic. : PAD and AAA patients admitted for any reason to the Vascular Unit from January 2019 to February 2020 were retrospectively analyzed. Biochemical and CV profiles as well as ongoing medical therapies were recorded. Benefits of CV risk-factors control were estimated using the SMART-REACH model. A follow-up visit during the year 2020 was scheduled. : A total of 669 patients were included. Of these, 190 showed AAA and 479 PAD at any stage. Only 54% of PAD and 41% of AAA patients were on lipid-lowering drugs with non-optimal low-density lipoprotein (LDL) levels for most of them. A better control of all modifiable CV risk-factors based on the current guidelines would offer an absolute risk reduction of the mean 10-year CV risk by 9% in PAD and 14% in AAA. Unfortunately, the follow-up visit was lost because of COVID-19 limitations. : Lipid profiles of PAD and AAA patients were far from guideline-based targets, and medical management was suboptimal. In our center, the COVID-19 pandemic impacted on the strict surveillance required in these very high-risk patients. The achievement of guideline-based therapeutic targets would definitively confer additional significant benefits in reducing the CV risk in these patients.
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http://dx.doi.org/10.3390/medicina57070672DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8307785PMC
June 2021

Computational and Pharmacological Studies on the Antioxidant, Thrombolytic, Anti-Inflammatory, and Analgesic Activity of .

Curr Issues Mol Biol 2021 Jun 22;43(2):434-456. Epub 2021 Jun 22.

Nutrition and Bromatology Group, Department of Analytical and Food Chemistry, Faculty of Food Science and Technology, University of Vigo-Ourense Campus, E32004 Ourense, Spain.

is an ornamental plant that has traditionally been used to treat several chronic diseases. The present study was designed to examine the antioxidant, cytotoxic, thrombolytic, anti-inflammatory, and analgesic activities of a methanolic extract of leaves (MEMC) using both experimental and computational models. Previously established protocols were used to perform qualitative and quantitative phytochemical screening in MEMC. A computational study, including molecular docking and ADME/T analyses, was performed. The quantitative phytochemical analysis revealed the total phenolic and flavonoid contents as 148.67 and 24 mg/g, respectively. Antioxidant activity was assessed by examining the reducing power of MEMC, resulting in absorbance of 1.87 at 400 µg/mL, demonstrating a strong reduction capacity. The extract exhibited significant protection against blood clotting and showed the highest protein denaturation inhibition at 500 µg/mL. In both the acetic acid-induced writhing and formalin-induced paw-licking models, MEMC resulted in significant potential pain inhibition in mice. In the computational analysis, 4-hydroxybenzaldehyde, orcinol glucoside, curcapital, crassifogenin C, and 2,6-dimethoxy-benzoic acid displayed a strong predictive binding affinity against the respective receptors. These findings indicated that possesses significant pharmacological activities to an extent supported by computational studies.
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http://dx.doi.org/10.3390/cimb43020035DOI Listing
June 2021

Unfolding the apoptotic mechanism of antioxidant enriched-leaves of Tabebuia pallida (lindl.) miers in EAC cells and mouse model.

J Ethnopharmacol 2021 Oct 10;278:114297. Epub 2021 Jun 10.

Department of Pharmacy, University of Rajshahi, Rajshahi, 6205, Bangladesh. Electronic address:

Ethnopharmacological Relevance: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. The leaves and barks of T. pallida are used as traditional medicine in the form of herbal or medicinal tea to manage cancer, fever, and pain. Moreover, extracts from the leaves of T. pallida showed anticancer activity. However, the chemical profile and mechanism of anticancer activity of T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) remain unexplored.

Aim Of The Study: The present study was designed to explore the regulation of apoptosis by T. pallida using Ehrlich Ascites Carcinoma (EAC) cultured cells and an EAC mouse model. LC-ESI-MS/MS was used for compositional analysis of T. pallida extracts.

Materials And Methods: Dried and powdered TPL, TPSB, TPRB and TPF were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from active extracts. Computer aided analyses was undertaken to sort out the best-fit phytoconstituent of total ten isolated compounds of this plant for antioxidant and anticancer activity.

Results: In EAC mice compared with untreated controls, the TPL extract exhibited the highest cancer cell toxicity with significant tumor cell growth inhibition (p < 0.001), reduced ascites by body weight (p < 0.01), increased the life span (p < 0.001), normalized blood parameters (RBC/WBC counts), and increased the levels of superoxide dismutase and catalase. TPL-treated EAC cells showed increased apoptotic characteristics of membrane blebbing, chromatin condensation and nuclear fragmentation, and caspase-3 activation, compared with untreated EAC cells. Moreover, annexin V-FITC and propidium iodide signals were greatly enhanced in response to TPL treatment, indicating apoptosis induction. Pro- and anti-apoptotic signaling after TPL treatment demonstrated up-regulated p53, Bax and PARP-1, and down-regulated NFκ-B, Bcl-2 and Bcl-xL expression, suggesting that TPL shifts the balance of pro- and anti-apoptotic genes towards cell death. LC-ESI-MS data of TPL showed a mixture of glycosides, lapachol, and quercetin antioxidant and its derivatives that were significantly linked to cancer cell targets. The compound, pelargonidin-3-O-glucoside was found to be most effective in computer aided models.

Conclusions: In conclusion, the TPL extract of T. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.
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http://dx.doi.org/10.1016/j.jep.2021.114297DOI Listing
October 2021

Is Emodin with Anticancer Effects Completely Innocent? Two Sides of the Coin.

Cancers (Basel) 2021 May 31;13(11). Epub 2021 May 31.

Department of Agricultural Sciences, University of Naples Federico II, Via Università 100, 80055 Portici, Italy.

Many anticancer active compounds are known to have the capacity to destroy pathologically proliferating cancer cells in the body, as well as to destroy rapidly proliferating normal cells. Despite remarkable advances in cancer research over the past few decades, the inclusion of natural compounds in researches as potential drug candidates is becoming increasingly important. However, the perception that the natural is reliable is an issue that needs to be clarified. Among the various chemical classes of natural products, anthraquinones have many biological activities and have also been proven to exhibit a unique anticancer activity. Emodin, an anthraquinone derivative, is a natural compound found in the roots and rhizomes of many plants. The anticancer property of emodin, a broad-spectrum inhibitory agent of cancer cells, has been detailed in many biological pathways. In cancer cells, these molecular mechanisms consist of suppressing cell growth and proliferation through the attenuation of oncogenic growth signaling, such as protein kinase B (AKT), mitogen-activated protein kinase (MAPK), HER-2 tyrosine kinase, Wnt/-catenin, and phosphatidylinositol 3-kinase (PI3K). However, it is known that emodin, which shows toxicity to cancer cells, may cause kidney toxicity, hepatotoxicity, and reproductive toxicity especially at high doses and long-term use. At the same time, studies of emodin, which has poor oral bioavailability, to transform this disadvantage into an advantage with nano-carrier systems reveal that natural compounds are not always directly usable compounds. Consequently, this review aimed to shed light on the anti-proliferative and anti-carcinogenic properties of emodin, as well as its potential toxicities and the advantages of drug delivery systems on bioavailability.
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http://dx.doi.org/10.3390/cancers13112733DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8198870PMC
May 2021

Emergent Drug and Nutrition Interactions in COVID-19: A Comprehensive Narrative Review.

Nutrients 2021 May 4;13(5). Epub 2021 May 4.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Naples, Italy.

Coronaviruses are a large family of viruses that are known to cause respiratory tract infections ranging from colds to more severe diseases, such as Middle East Respiratory Syndrome (MERS) and the Severe Acute Respiratory Syndrome (SARS). New Coronavirus Disease 2019 (COVID-19), which led to deaths as well as social and economic disruptions, is an ongoing worldwide pandemic caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Currently, there is no approved treatment for COVID-19. Hence, only supportive care has been approved by the World Health Organization (WHO) for now. Pharmacological agents used for the adjunctive treatment of COVID-19 following the current literature and clinical experiences include antiviral, anti-inflammatory, and anti-malaria drugs, and other traditional or untraditional treatments. However, it has been reported that the use of these drugs may have some negative effects and comorbidities. Moreover, the current data have indicated that the risk of drug-drug interactions may also be high in polypharmacy cases, especially in elderly people, some comorbidity situations, and intensive care unit (ICU) patients. It is highly possible that these situations can not only increase the risk of drug-drug interactions but also increase the risk of food/nutrition-drug interactions and affect the nutritional status. However, this issue has not yet been entirely discussed in the literature. In this review, current information on the possible mechanisms as well as pharmacokinetic and pharmacodynamic effects of some pharmacological agents used in the treatment of COVID-19 and/or their secondary interactions with nutrition were evaluated and some future directions were given.
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http://dx.doi.org/10.3390/nu13051550DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8147951PMC
May 2021

Natural Compounds as Medical Strategies in the Prevention and Treatment of Psychiatric Disorders Seen in Neurological Diseases.

Front Pharmacol 2021 13;12:669638. Epub 2021 May 13.

Department of Agricultural Sciences, University of Naples Federico II, Potici, Italy.

Psychiatric disorders are frequently encountered in many neurological disorders, such as Alzheimer's and Parkinson diseases along with epilepsy, migraine, essential tremors, and stroke. The most common comorbid diagnoses in neurological diseases are depression and anxiety disorders along with cognitive impairment. Whether the underlying reason is due to common neurochemical mechanisms or loss of previous functioning level, comorbidities are often overlooked. Various treatment options are available, such as pharmacological treatments, cognitive-behavioral therapy, somatic interventions, or electroconvulsive therapy. However oral antidepressant therapy may have some disadvantages, such as interaction with other medications, low tolerability due to side effects, and low efficiency. Natural compounds of plant origin are extensively researched to find a better and safer alternative treatment. Experimental studies have shown that phytochemicals such as alkaloids, terpenes, flavonoids, phenolic acids as well as lipids have significant potential in and models of psychiatric disorders. In this review, various efficacy of natural products in and studies on neuroprotective and their roles in psychiatric disorders are examined and their neuro-therapeutic potentials are shed light.
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http://dx.doi.org/10.3389/fphar.2021.669638DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8155682PMC
May 2021

Central and peripheral pain intervention by Ophiorrhizarugosa leaves: Potential underlying mechanisms and insight into the role of pain modulators.

J Ethnopharmacol 2021 Aug 5;276:114182. Epub 2021 May 5.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy. Electronic address:

Ethnopharmacological Relevance: Ophiorrhiza rugosa var. prostrata is a traditional medicinal plant used by the indigenous and local tribes (Chakma, Marma and Tanchangya) of Bangladesh for the management of chest pain, body ache, and earache. However, the knowledge of anti-nociceptive and anti-inflammatory potentials of this plant is scarce.

Aim Of The Study: Therefore, we scrutinized the anti-nociceptive and anti-inflammatory properties of O. rugosa leaves along with its possible mechanism(s) of action using chemical and heat-induced pain models.

Methods And Materials: O. rugosa was extracted using 100% ethanol (EEOR) followed by exploring phytochemicals and assessing acute toxicity. To determine anti-nociceptive potentials, chemical-induced (acetic acid and formalin) and heat-induced (hot plate and tail immersion) nociceptive models were followed. To investigate the possible involvement of opioid receptors during formalin, hot plate, and tail immersion tests, naltrexone was administered whereas methylene blue and glibenclamide were used to explore cGMP involvement and ATP-sensitive K channel pathways, respectively. Moreover, the anti-inflammatory potential was assessed using the carrageenan-induced paw edema test model. Motor behaviours of EEOR were assessed by the open-field test. Finally, bioactive constituents (identified by GC-MS) from O. rugosa were subjected to molecular docking and ADME/t analysis to evaluate its potency and safety.

Results: During chemical-induced and heat-induced pain models, EEOR exhibited significant and effective nociception suppression at all experimental doses (200 and 400 mg/kg). Also, the administration of naltrexone corroborated the association of opioid receptors with the anti-nociceptive activity by EEOR. Similarly, cGMP and ATP-sensitive K channel pathways were also found to be involved in the anti-nociceptive mechanism. Furthermore, significant and dose-dependent inhibition of inflammation induced by carrageenan was recorded for EEOR. Both doses of EEOR did not affect the animal's locomotor capacity in the open-field test. Besides, in silico test identified the key compounds (loliolide, harman, squalene, vitamin E, and gamma-sitosterol) that inhibited some particular receptors regarding pain and inflammation.

Conclusion: This research exposes central and peripheral pain intervention as well as anti-inflammatory activity of O. rugosa. Also, the identified compounds from this plant support its activities by effectively inhibiting anti-nociceptive and anti-inflammatory receptors. Overall, these outcomes valorize the ethnomedicinal efficacy of O. rugosa in managing various painful conditions.
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http://dx.doi.org/10.1016/j.jep.2021.114182DOI Listing
August 2021

An Effective Phytoconstituent Aconitine: A Realistic Approach for the Treatment of Trigeminal Neuralgia.

Mediators Inflamm 2021 14;2021:6676063. Epub 2021 Apr 14.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici Naples, Italy.

Trigeminal neuralgia pain remains a challenge to treat. Natural compounds may be promising options for relieving pain. This study was aimed at investigating the effects of aconitine in a rat model of trigeminal neuralgia pain. Infraorbital nerve chronic constriction injury was performed in adult Wistar Albino rats. After the neuropathic pain developed, the rats were assigned to one of the treatment groups: carbamazepine 40 or 80 mg/kg; aconitine 0.25, 0.50, or 0.75 mg/kg; or saline injection (control group). Behavioral testing with von Frey filaments and the rotarod test were carried out before the surgical procedure and on the 24th to 29th postoperative days. Following the completion of tests, ipsilateral and contralateral spinal cords were harvested for Western blot analyses to assess NR-1 protein expression. ANOVA followed by Mann-Whitney test was performed for the statistical analyses. values of <0.05 were considered significant. Aconitine significantly reduced mechanical sensitivity in a dose-dependent manner. A significant reduction in motor coordination was noted for the higher doses of aconitine which was similar with the 40 and 80 mg/kg doses of carbamazepine. NR-1 expression was reduced in the ipsilateral spinal cord, whereas no significant difference was noted between the groups in the expression of NR-1 in the contralateral spinal cord. Aconitine had a significant pain relieving effect, which was similar to carbamazepine, in a dose-dependent manner. Aconitine may be an alternative pharmacological agent for the control of trigeminal neuralgia pain.
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http://dx.doi.org/10.1155/2021/6676063DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8062177PMC
April 2021

(Burm. f.) Wall. ex Nees: An Updated Review of Phytochemistry, Antimicrobial Pharmacology, and Clinical Safety and Efficacy.

Life (Basel) 2021 Apr 16;11(4). Epub 2021 Apr 16.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

Infectious disease (ID) is one of the top-most serious threats to human health globally, further aggravated by antimicrobial resistance and lack of novel immunization options. (Burm. f.) Wall. ex Nees and its metabolites have been long used to treat IDs. Andrographolide, derived from can inhibit invasive microbes virulence factors and regulate the host immunity. Controlled clinical trials revealed that treatment is safe and efficacious for acute respiratory tract infections like common cold and sinusitis. Hence, , mainly andrographolide, could be considered as an excellent candidate for antimicrobial drug development. Considering the importance, medicinal values, and significant role as antimicrobial agents, this study critically evaluated the antimicrobial therapeutic potency of and its metabolites, focusing on the mechanism of action in inhibiting invasive microbes and biofilm formation. A critical evaluation of the secondary metabolites with the aim of identifying pure compounds that possess antimicrobial functions has further added significant values to this study. Notwithstanding that is a promising source of antimicrobial agents and safe treatment for IDs, further empirical research is warranted.
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http://dx.doi.org/10.3390/life11040348DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8072717PMC
April 2021

Palmitoylethanolamide Reduces Colon Cancer Cell Proliferation and Migration, Influences Tumor Cell Cycle and Exerts In Vivo Chemopreventive Effects.

Cancers (Basel) 2021 Apr 16;13(8). Epub 2021 Apr 16.

Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, 80131 Naples, Italy.

Palmitoylethanolamide (PEA) is an endogenous fatty acid amide related to the endocannabinoid anandamide. PEA exerts intestinal anti-inflammatory effects, but knowledge of its role in colon carcinogenesis is still largely fragmentary. We deepened this aspect by studying the effects of PEA (ultramicronized PEA, um-PEA) on colon cancer cell proliferation, migration and cell cycle as well as its effects in a murine model of colon cancer. Results showed that um-PEA inhibited tumor cell proliferation via peroxisome proliferator-activated receptor α and G protein-coupled receptor 55, induced cell cycle arrest in the G2/M phase, possibly through cyclin B1/CDK1 upregulation, and induced DNA fragmentation. Furthermore, um-PEA reduced tumor cell migration by reducing MMP2 and TIMP1 expression. In vivo administration of um-PEA exerted beneficial effects in the azoxymethane model of colonic tumors, by reducing the number of preneoplastic lesions and tumors. Collectively, our findings provide novel proofs on the effects of um-PEA in colon carcinogenesis.
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http://dx.doi.org/10.3390/cancers13081923DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8073478PMC
April 2021

Efficacy of Phytochemicals Derived from for the Management of COVID-19: A Combined In Silico and Biochemical Study.

Molecules 2021 Apr 12;26(8). Epub 2021 Apr 12.

Nutrition and Bromatology Group, Department of Analytical and Food Chemistry, Faculty of Food Science and Technology, Ourense Campus, University of Vigo, E32004 Ourense, Spain.

The recent coronavirus disease 2019 (COVID-19) pandemic is a global threat for healthcare management and the economic system, and effective treatments against the pathogenic severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus responsible for this disease have not yet progressed beyond the developmental phases. As drug refinement and vaccine progression require enormously broad investments of time, alternative strategies are urgently needed. In this study, we examined phytochemicals extracted from and evaluated their potential effects against the main protease of SARS-CoV-2. The antioxidant activities of leaf and fruit extracts at 150 µg/mL were 95.97% and 92.48%, respectively. Furthermore, both extracts displayed low cytotoxicity levels against . The gas chromatography-mass spectroscopy analysis confirmed the identifies of 75 phytochemicals from both extracts, and four potent compounds, triacontane, hexacosane, methyl linoleate, and methyl palminoleate, had binding free energy values of -6.75, -6.7, -6.3, and -6.3 Kcal/mol, respectively, in complexes with the SARS-CoV-2 main protease. The active residues Cys145, Met165, Glu166, Gln189, and Arg188 in the main protease formed non-bonded interactions with the screened compounds. The root-mean-square difference (RMSD), root-mean-square fluctuations (RMSF), radius of gyration (Rg), solvent-accessible surface area (SASA), and hydrogen bond data from a molecular dynamics simulation study confirmed the docked complexes' binding rigidity in the atomistic simulated environment. However, this study's findings require in vitro and in vivo validation to ensure the possible inhibitory effects and pharmacological efficacy of the identified compounds.
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http://dx.doi.org/10.3390/molecules26082210DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070553PMC
April 2021

Involvement of Opioid System and TRPM8/TRPA1 Channels in the Antinociceptive Effect of .

Biomolecules 2021 04 17;11(4). Epub 2021 Apr 17.

Laboratory of Autoimmunity and Immunopharmacology (LAIF), Department of Health Sciences, Campus Araranguá, Universidade Federal de Santa Catarina, Araranguá 88906-072, Brazil.

is a "super-food" and has attracted researchers' attention due to its anti-inflammatory, antioxidant, and analgesic properties. Herein, we investigated the antinociceptive effects of in different rodent behavior models of inflammatory pain. Male Swiss mice were treated with (3-300 mg/kg, p.o.), indomethacin (10 mg/kg, p.o.), or vehicle (0.9% NaCl 10 mL/kg). Behavioral tests were performed with administration of acetic acid (0.6%, i.p.), formalin 2.7% (formaldehyde 1%, i.pl.), menthol (1.2 µmol/paw, i.pl.), cinnamaldehyde (10 nmol/paw, i.pl.), capsaicin (1.6 µg/paw, i.pl.), glutamate (20 µmol/paw, i.pl.), or naloxone (1 mg/kg, i.p.). The animals were also exposed to the rotarod and open field test to determine possible effects of on locomotion and motor coordination. The quantitative phytochemical assays exhibited that contains significant concentrations of total phenols and flavonoid contents, as well as it showed a powerful antioxidant effect with the highest scavenging activity. Oral administration of completely inhibited the abdominal contortions induced by acetic acid (ED = 20.51 mg/kg). treatment showed significant inhibition of formalin-induced nociceptive behavior during the inflammatory phase, and the opioid-selective antagonist markedly blocked this effect. Furthermore, our data indicate that the mechanisms underlying analgesia appear to be related to its ability to modulate TRMP8 and TRPA1, but not by TRPV1 or glutamatergic system. represents an orally active and safe natural analgesic that exhibits great therapeutic potential for managing inflammatory pain disorders.
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http://dx.doi.org/10.3390/biom11040592DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8074039PMC
April 2021

Bromelain a Potential Bioactive Compound: A Comprehensive Overview from a Pharmacological Perspective.

Life (Basel) 2021 Apr 6;11(4). Epub 2021 Apr 6.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

Bromelain is an effective chemoresponsive proteolytic enzyme derived from pineapple stems. It contains several thiol endopeptidases and is extracted and purified via several methods. It is most commonly used as an anti-inflammatory agent, though scientists have also discovered its potential as an anticancer and antimicrobial agent. It has been reported as having positive effects on the respiratory, digestive, and circulatory systems, and potentially on the immune system. It is a natural remedy for easing arthritis symptoms, including joint pain and stiffness. This review details bromelain's varied uses in healthcare, its low toxicity, and its relationship to nanoparticles. The door of infinite possibilities will be opened up if further extensive research is carried out on this pineapple-derived enzyme.
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http://dx.doi.org/10.3390/life11040317DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8067380PMC
April 2021

Diterpenes from Euphorbia myrsinites and Their Anti-inflammatory Property.

Planta Med 2021 Apr 27. Epub 2021 Apr 27.

Dipartimento di Agraria, Università degli Studi di Napoli Federico II, Portici, Naples, Italy.

is one of the oldest spurges described and used in folk medicine. It is characterized by blue-grey stems similar to myrtle, and it is spread in the Mediterranean region, Asia, and the USA. Chemical analysis of collected in Turkey afforded the isolation of 4 diterpenes based on the so-called myrsinane skeleton being tetraesters of the tetracyclic diterpene alcohol myrsinol. In this study, the phytochemical analysis of this species collected in Italy has been undertaken to afford the isolation of a new atisane diterpene, named myrsatisane, 3 ingenol derivatives, along with the 4 tetraester derivatives previously found. A triterpene compound based on the euphane skeleton has also been isolated. Structural elucidation of the new myrsatisane was based on spectroscopic techniques, including HR-MS and 1- and 2-dimensional NMR experiments. Its relative configuration was determined by NOE correlations, while absolute stereochemistry was obtained by quantum-mechanical DFT studies. While diterpenes with the atisane skeleton are relatively common in species, this is the first report of an atisane diterpene from . All the isolated terpenes were tested for anti-inflammatory activity on J774A.1 macrophages stimulated with lipopolysaccharide by evaluation of nitrite and pro-inflammatory cytokine Il-1 levels. Among tested compounds, the 3 ingenol diterpenes exhibited a dose-dependent (0.001 - 3 µM) significant activity, thus showing their potential as anti-inflammatory drug candidates.
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http://dx.doi.org/10.1055/a-1479-2866DOI Listing
April 2021

Pharmacological Studies on Traditional Plant-Based Remedies.

Biomedicines 2021 Mar 19;9(3). Epub 2021 Mar 19.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

For years, plant-based remedies have been used as a traditional practice to treat and prevent a broad range of diseases [...].
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http://dx.doi.org/10.3390/biomedicines9030315DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003496PMC
March 2021

Therapeutic Potentials of Fruit (Seed) Reflected into an Array of Pharmacological Assays and Prospective Receptors-Mediated Pathways.

Life (Basel) 2021 Feb 17;11(2). Epub 2021 Feb 17.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

(SF), a valuable Bangladeshi fruit, is considered an alternative therapeutic agent. Mainly, seeds are used as nutritional phytotherapy to ease physical and mental status by preventing chronic diseases. Here, we scrutinized the seed's fundamental importance in traditional medicine by following an integrated approach combining in vivo, in vitro, and in silico studies. The SF was fractionated with different solvents, and the ethyl acetate fraction of SF (EaF-SF) was further studied. Mice treated with EaF-SF (200 and 400 mg/kg) manifested anxiolysis evidenced by higher exploration in elevated plus maze and hole board tests. Similarly, a dose-dependent drop of immobility time in a forced swimming test ensured significant anti-depressant activity. Moreover, higher dose treatment exposed reduced exploratory behaviour resembling decreased movement and prolonged sleeping latency with a quick onset of sleep during the open field and thiopental-induced sleeping tests, respectively. In parallel, EaF-SF significantly ( < 0.001) and dose-dependently suppressed acetic acid and formalin-induced pain in mice. Also, a noteworthy anti-inflammatory activity and a substantial ( < 0.01) clot lysis activity (thrombolytic) was observed. Gas chromatography-mass spectrometry (GC-MS) analysis resulted in 49 bioactive compounds. Among them, 12 bioactive compounds with Lipinski's rule and safety confirmation showed strong binding affinity (molecular docking) against the receptors of each model used. To conclude, the seed is a prospective source of health-promoting effects that can be an excellent candidate for preventing degenerative diseases.
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http://dx.doi.org/10.3390/life11020155DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7921944PMC
February 2021

Investigation of the Pharmacological Properties of Nees through Experimental Approaches.

Life (Basel) 2021 Feb 25;11(3). Epub 2021 Feb 25.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

Nees is used locally in Ayurvedic medicine to treat coughs and cardiovascular diseases. This study explored its pharmacological potential through in vivo and in vitro approaches for the metabolites extracted (methanolic) from the stems of . A qualitative phytochemical analysis revealed the presence of numerous secondary metabolites. The methanol extract of stems (MELHS) showed a strong antioxidative activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and reducing power assays, and in the quantitative (phenolic and flavonoid) assay. Clot lysis and brine shrimp lethality bioassays were applied to investigate the thrombolytic and cytotoxic activities, respectively. MELHS exhibited an expressive percentage of clot lysis (33.98%) with a moderately toxic (115.11 μg/mL) effect. The in vivo anxiolytic activity was studied by an elevated plus maze test, whereas the antidepressant activity was examined by a tail suspension test and forced swimming test. During the anxiolytic evaluation, MELHS exhibited a significant dose-dependent reduction of anxiety, in which the 400 mg/kg dose of the extract showed 78.77 ± 4.42% time spent in the open arm in the elevated plus maze test. In addition, MELHS demonstrated dose-dependent and significant activities in the tail suspension test and forced swimming test, whereas the 400 mg/kg dose of the extract showed 87.67 ± 6.40% and 83.33 ± 6.39% inhibition of immobile time, respectively. Therefore, the current study suggests that could be a potential source of anti-oxidative, cytotoxic, thrombolytic, anxiolytic, and antidepressant agents. Further study is needed to determine the mechanism behind the bioactivities.
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http://dx.doi.org/10.3390/life11030180DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7996513PMC
February 2021

Synthesis, docking studies, and pharmacological evaluation of 2-hydroxypropyl-4-arylpiperazine derivatives as serotoninergic ligands.

Arch Pharm (Weinheim) 2021 May 5;354(5):e2000414. Epub 2021 Feb 5.

Dipartimento di Farmacia,  Università degli Studi di Napoli "Federico II", Napoli, Italy.

A new series of norbornene and exo-N-hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide derivatives was prepared, and their affinities to the 5-HT , 5-HT , and 5-HT receptors were evaluated and compared with a previously synthesized series of derivatives characterized by the same nuclei, to identify selective ligands for the subtype receptors. Arylpiperazines represent one of the most important classes of 5-HT R ligands, and the research of new derivatives has been focused on the modification of one or more portions of this pharmacophore. The combination of structural elements (heterocyclic nucleus, hydroxyalkyl chain, and 4-substituted piperazine), known to be critical for the affinity to 5-HT receptors, and the proper selection of substituents resulted in compounds with high specificity and affinity toward serotoninergic receptors. The most active compounds were selected for further in vivo assays to determine their functional activity. Finally, to rationalize the obtained results, molecular docking studies were performed. The results of the pharmacological studies showed that 3e, 4j, and 4n were the most active and promising derivatives for the serotonin receptor considered in this study.
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http://dx.doi.org/10.1002/ardp.202000414DOI Listing
May 2021

Phytosterols: From Preclinical Evidence to Potential Clinical Applications.

Front Pharmacol 2020 14;11:599959. Epub 2021 Jan 14.

Chair and Department of Food and Nutrition, Medical University of Lublin, Lublin, Poland.

Phytosterols (PSs) are plant-originated steroids. Over 250 PSs have been isolated, and each plant species contains a characteristic phytosterol composition. A wide number of studies have reported remarkable pharmacological effects of PSs, acting as chemopreventive, anti-inflammatory, antioxidant, antidiabetic, and antiatherosclerotic agents. However, PS bioavailability is a key issue, as it can be influenced by several factors (type, source, processing, preparation, delivery method, food matrix, dose, time of administration into the body, and genetic factors), and the existence of a close relationship between their chemical structures (e.g., saturation degree and side-chain length) and low absorption rates has been stated. In this sense, the present review intends to provide in-depth data on PS therapeutic potential for human health, also emphasizing their preclinical effects and bioavailability-related issues.
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http://dx.doi.org/10.3389/fphar.2020.599959DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7841260PMC
January 2021

Gut-Brain-Microbiota Axis: Antibiotics and Functional Gastrointestinal Disorders.

Nutrients 2021 Jan 27;13(2). Epub 2021 Jan 27.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Naples, Italy.

Gut microbiota composition and function are major areas of research for functional gastrointestinal disorders. There is a connection between gastrointestinal tract and central nervous system and this is mediated by neurotransmitters, inflammatory cytokines, the vagus nerve and the hypothalamic-pituitary-adrenal axis. Functional gastrointestinal disorders are prevalent diseases affecting more than one third of the population. The etiology of these disorders is not clarified. Visceral hyperalgesia is the main hypothesis for explaining clinical symptoms, however gut-brain axis disorder is a new terminology for functional disorders. In this review, microbiota-gut-brain axis connection pathways and related disorders are discussed. Antibiotics are widely used in developed countries and recent evidence indicates antibiotic-induced dysbiosis as an important factor for functional disorders. Antibiotics exert negative effects on gut microbiota composition and functions. Antibiotic-induced dysbiosis is a major factor for occurrence of post-infectious irritable bowel syndrome. Cognitive and mood disorders are also frequent in functional gastrointestinal disorders. Animal and human trials show strong evidence for the causal relationship between gut microbiota and brain functions. Therapeutic implications of these newly defined pathogenic pathways are also discussed.
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http://dx.doi.org/10.3390/nu13020389DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7910879PMC
January 2021

Topical Collection "Pharmacology of Medicinal Plants".

Biomolecules 2021 01 14;11(1). Epub 2021 Jan 14.

Department of Agricultural Science, University of Naples Federico II, 80138 Naples, Italy.

The use of remedies based on medicinal plants continues to expand rapidly around the world, with many people now resorting to this type of product for the treatment and prevention of several pathologies [...].
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http://dx.doi.org/10.3390/biom11010101DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7828774PMC
January 2021

Ethnomedicinal uses, phytochemistry, and biological activities of plants of the genus Gynura.

J Ethnopharmacol 2021 May 16;271:113834. Epub 2021 Jan 16.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka 1000, Bangladesh. Electronic address:

Ethnopharmacological Relevance: The genus Gynura (Compositae) includes around 46 species and is native to the tropical regions of Southeast Asia, Africa and Australia. Many species within this genus are used in ethnomedicine to treat various disorders including skin diseases, injuries, ulcers, wounds, burns, sores, scalds, as well as for the management of diabetes, hypertension, hyperlipidemia, constipation, rheumatism, bronchitis and inflammation.

Aim Of The Review: This review is an attempt to provide scientific information regarding the ethnopharmacology, phytochemistry, pharmacological and toxicological profiles of Gynura species along with the nomenclature, distribution, taxonomy and botanical features of the genus. A critical analysis has been undertaken to understand the current and future pharmaceutical prospects of the genus.

Materials & Methods: Several electronic databases, including Google scholar, PubMed, Web of Science, Scopus, ScienceDirect, SpringerLink, Semantic Scholar, MEDLINE and CNKI Scholar, were explored as information sources. The Plant List Index was used for taxonomical authentications. SciFinder and PubChem assisted in the verification of chemical structures.

Results: A large number of phytochemical analyses on Gynura have revealed the presence of around 342 phytoconstituents including pyrrolizidine alkaloids, phenolic compounds, chromanones, phenylpropanoid glycosides, flavonoids, flavonoid glycosides, steroids, steroidal glycosides, cerebrosides, carotenoids, triterpenes, mono- and sesquiterpenes, norisoprenoids, oligosaccharides, polysaccharides and proteins. Several in vitro and in vivo studies have demonstrated the pharmacological potential of Gynura species, including antidiabetic, anti-oxidant, anti-inflammatory, antimicrobial, antihypertensive and anticancer activities. Although the presence of pyrrolizidine alkaloids within a few species has been associated with possible hepatotoxicity, most of the common species have a good safety profile.

Conclusions: The importance of the genus Gynura both as a prominent contributor in ethnomedicinal systems as well as a source of promising bioactive molecules is evident. Only about one fourth of Gynura species have been studied so far. This review aims to provide some scientific basis for future endeavors, including in-depth biological and chemical investigations into already studied species as well as other lesser known species of Gynura.
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http://dx.doi.org/10.1016/j.jep.2021.113834DOI Listing
May 2021

Pharmacological insights on the antidepressant, anxiolytic and aphrodisiac potentials of Aglaonema hookerianum Schott.

J Ethnopharmacol 2021 Mar 3;268:113664. Epub 2020 Dec 3.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy. Electronic address:

Ethnopharmacological Relevance: Aglaonema hookerianum Schott is an ethnomedicinally important plant used to treat a variety of diseases, including sexual and depression-like disorders. However, the scientific basis underlying the aforesaid properties have not been well justified.

Aim Of The Study: The present investigation aimed to investigate the anxiolytic, antidepressant and aphrodisiac potentials of methanol leaves extract of A. hookerianum (MEAH) in Swiss albino mice.

Materials & Methods: Swiss albino mice (20-30 g) were orally administrated with MEAH at the doses ranging from 100 to 400 mg/kg, b.w. The elevated plus maze (EPM) and hole board test (HBT) were performed to determine the anxiolytic activity and the forced swimming test (FST) and tail suspension test (TST) were performed to determine the antidepressant activity of MEAH. Besides, the aphrodisiac activity of MEAH was conducted through the mounting behaviour and orientation behaviour analysis. Diazepam (1 mg/kg, b.w., i.p.) for EPM and HBT; fluoxetine HCl (20 mg/kg, b.w., p.o.) for FST and TST, and sildenafil (5 mg/kg, b.w., p.o.) for the mounting behaviour analysis and orientation behaviour analysis were used as reference drugs.

Results: The administration of the MEAH produced a strong (p < 0.001) dose-dependent anxiolytic effects in both HBT and EPM tests. Likewise, the extract revealed a significant (p < 0.001) reduction in the immobility time in both FST and TST as compared to the control group. Besides, the MEAH also found to possess marked aphrodisiac activity complying several facets such as an increase in the sexual performance at the highest dose (400 mg/kg, p.o.) as well as the orientation toward female mice (p < 0.001) at all tested doses.

Conclusion: Taken together, MEAH can be recommended as a potent source of neuroprotective and a libido-boosting drug candidate for the management of neurological and sexual disorders.
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http://dx.doi.org/10.1016/j.jep.2020.113664DOI Listing
March 2021

Special Issue "Plant Extracts: Biological and Pharmacological Activity".

Molecules 2020 11 4;25(21). Epub 2020 Nov 4.

Department of Neuroscience, Psychology, Drug Research and Child Health-Neurofarba-Section of Pharmacology and Toxicology, University of Florence, 50139 Florence, Italy.

The use of plant extracts for therapeutic purposes knows a wide diffusion [...].
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http://dx.doi.org/10.3390/molecules25215131DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7662983PMC
November 2020

Pharmacological insights and prediction of lead bioactive isolates of Dita bark through experimental and computer-aided mechanism.

Biomed Pharmacother 2020 Nov 5;131:110774. Epub 2020 Oct 5.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy. Electronic address:

Dita bark (Alstonia scholaris (L.) R. Br.) is an ethnomedicine used for the management of various ailments. This study aimed to investigate the biological properties of methanol extract of A. scholaris bark (MEAS), through in vivo, in vitro and in silico approaches alongside its phytochemical profiling. Identification and nature of the bioactive secondary metabolites were studied by the established qualitative tests and GC-MS analysis. The antidepressant activity was determined by forced swimming test (FST) and tail suspension test (TST) in mice. The anti-inflammatory and thrombolytic effect was evaluated using inhibition of protein denaturation technique and clot lysis technique, respectively. Besides, computational studies of the isolated compounds and ADME/T analysis were performed by Schrödinger-Maestro (v11.1) software, and PASS prediction was conducted through PASS online tools. The GC-MS analysis revealed the presence of several secondary metabolites in MEAS. Treatment with MEAS revealed a significant reduction of immobility time in a dose-dependent manner in FST and TST. Besides, MEAS showed substantial anti-inflammatory effects at the higher dose (400 μg/mL) as well as revealed notable clot lysis effect as compared to control. In the case of computer-aided investigation, all compounds meet the condition of Lipinski's rule of five. PASS study also predicted for all compounds, and among these safe compound furazan-3-amine showed the most spontaneous binding energy for both antidepressant and thrombolytic activities, as well as 5-dimethylamino-6 azauracil, found promising for anti-inflammatory activity. Taken together, the investigation concludes that MEAS can be a potent source of antidepressant, anti-inflammatory, and thrombolytic agents.
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http://dx.doi.org/10.1016/j.biopha.2020.110774DOI Listing
November 2020

Biological Evaluation, DFT Calculations and Molecular Docking Studies on the Antidepressant and Cytotoxicity Activities of Buch.-Ham. Compounds.

Pharmaceuticals (Basel) 2020 Sep 3;13(9). Epub 2020 Sep 3.

Nutrition and Bromatology Group, Department of Analytical and Food Chemistry, Faculty of Food Science and Technology, University of Vigo-Ourense Campus, E32004 Ourense, Spain.

Buch.-Ham. is commonly used in folk medicine against various disorders. The present study investigated the antidepressant and cytotoxicity activity of methanol extract of (MECP) along with quantitative phytochemical analysis by GC-MS method. Here, the GC-MS study of MECP presented 41 compounds, among which most were fatty acids, esters, terpenoids and oximes. The antidepressant activity was assessed by the forced swimming test (FST) and tail suspension test (TST) models. In contrast, MECP (200 and 400 mg/kg) exhibited a significant and dose-dependent manner reduction in immobility comparable with fluoxetine (10 mg/kg) and phenelzine (20 mg/kg). MECP showed a weak toxicity level in the brine shrimp lethality bioassay (ED: 358.65 µg/mL) comparable to the standard drug vincristine sulfate (ED: 2.39 µg/mL). Three compounds from the GC-MS study were subjected to density functional theory (DFT) calculations, where only cyclopentadecanone oxime showed positive and negative active binding sites. Cyclopentadecanone oxime also showed a good binding interaction in suppressing depression disorders by blocking monoamine oxidase and serotonin receptors with better pharmacokinetic and toxicological properties. Overall, the MECP exhibited a significant antidepressant activity with moderate toxicity, which required further advance studies to identify the mechanism.
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http://dx.doi.org/10.3390/ph13090232DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7557754PMC
September 2020

(Fabaceae) Phytochemistry, Ethnobotany, and Bioactivities: A Review.

Molecules 2020 Aug 23;25(17). Epub 2020 Aug 23.

Graduate Program in Biological Sciences-PPGCB; Federal University of Pernambuco-UFPE, Recife 50670-901, PE, Brazil.

, popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of . The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of .
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http://dx.doi.org/10.3390/molecules25173831DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7503918PMC
August 2020

Deciphering the Pharmacological Properties of Methanol Extract of Leaves by In Vivo, In Vitro and In Silico Approaches.

Pharmaceuticals (Basel) 2020 Aug 6;13(8). Epub 2020 Aug 6.

Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici, Italy.

The present study explores the neuropharmacological, antinociceptive, antidiarrheal, antioxidant, thrombolytic and cytotoxic activity of methanol extract of leaves (MEPC). In anxiolytic activity testing of MEPC by elevated plus maze test, hole-board test and light-dark test, the extract exhibited a dose-dependent reduction of anxiety while the open field test observed a decreased locomotion. The administration of MEPC revealed a significant dose-dependent reduction of depressant behavior in forced swimming and tail suspension test. Additionally, the antinociceptive and antidiarrheal activity exposed a significant reduction of nociception and diarrheal behavior at the highest dose. In addition, a strong antioxidant activity was observed in DPPH-free radical-scavenging assay (IC = 461.05 μg/mL), total phenol content (118.31 ± 1.12 mg) and total flavonoid content (100.85 ± 0.97 mg). The significant clot-lysis activity was also observed with moderate toxicity (LC = 247.92 μg/mL) level in the lethality assay of brine shrimp. Moreover, in silico molecular docking study showed that the compound Psychotriasine could offer promising active site interactions for binding proteins. Furthermore, ADME/T and toxicological properties of the compound satisfied the Lipinski's rule of five and Veber rules for drug-like potential and toxicity level. Overall, MEPC had a potential neuropharmacological, antinociceptive, antidiarrheal and antioxidant activity that warranted further investigation.
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http://dx.doi.org/10.3390/ph13080183DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7463710PMC
August 2020

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects.

Int J Mol Sci 2020 Aug 6;21(16). Epub 2020 Aug 6.

Department of Agricultural Sciences, University of Naples Federico II, Via Università 100, 80055 Portici, Italy.

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins' defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventive and chemotherapeutic synergistic potential when used in combination with other anticancer drugs. Here, we address different pathways which are activated by furanocoumarins and their therapeutic efficacy in various tumors. Ideally, this review will trigger interest in furanocoumarins and their potential efficacy and safety as a cancer lessening agents.
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http://dx.doi.org/10.3390/ijms21165622DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7460698PMC
August 2020
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