Farid Abd Elreheem Badria

Mansoura University · Department of Pharmacology

We synthesized a novel compound library featuring a spirooxindole core structure combined with various heterocycles, including benzofuran, benzothiophene, and thiophene scaffolds. Evaluation using MTT assays against HepG2, 4T1, and MDA‐MB‐231 cells revealed the most potent candidate, spirooxindole hybrid 5c, with an IC50 of 5 ± 0.6 µM against HepG2...

Pharmacovigilance involves detecting, assessing, understanding, and preventing adverse drug effects. The field aims to systematically monitor medicines and promote their safe, effective use. However, pharmacovigilance faces challenges such as fragmented systems and passive reporting. As the discipline advances, priorities now include centralizing d...

Background Obstructive sleep apnea (OSA) is one of the foremost potential severe disorders, with frequent episodes of complete or partial obstructions of the upper airway during sleep. Therefore, several attempts to find an effective pharmacotherapy by repurposing several drugs such as serotonin reuptake inhibitors (SRIs) and norepinephrine and dop...

This study intended to improve the quality and medicinal value of edible plants. Our interest is to focus on utilizing various plant extracts (Bio-modulators) in the modulation of medicinal plants’ secondary metabolites. This study aimed to modulate the contents of potato (Solanum tuberosum L.) peel to comply with food safety regulations and also o...

The utilization of elicitation techniques presents a novel and inventive approach in the realm of functional food and nutraceutical production. The interconnection between plant elicitation, functional food, and nutraceutical production can be approached from various perspectives. Plant elicitation refers to the process of stimulating plants to pro...

A spirooxindole nanoformulation includes a proniosome loaded with a spirooxindole derivative. In an embodiment, the spirooxindole derivative comprises (Compound 4d)

This research investigates repurposing potato glycoalkaloids as lifesaving anticancer drugs. There is integration of network pharmacology with multiomics. Solanine, chaconine, and their hydrolysis products’ pharmacokinetics were tested using SwissADME. Solanine and chaconine targets were identified via reverse pharmacophore mapping. Through databas...

Potato peel may play a mixed blessing role via providing useful and economic compounds, in contrast, it contains very toxic glycoalkaloids. However, massive amounts of potato peel waste are generated from industrial and personal uses. The evaluation of the four used bio-modulator responses on potato peel was estimated by monitoring the chemical con...

In the postmoderenizaton era, limitation of resources is one of the main obstacles that face scientific research, specially drug discovery. This requires new prespective that would allow the reuse of available resources and extend their spercta of applications. Natural products (NPs) have been studied thoroughly in the last century which lead to ac...

In an effort to develop new compounds for managing drug-induced liver injury, we prepared 23 novel hybrids based on 3-acetyl-11-keto-β-boswellic acid (AKBA) using various biocompatible linkers. A bioguided approach was employed to identify the most promising hybrid. Eight compounds exhibited superior anti-inflammatory activity compared to the paren...

In this study, we investigated the conjugation of theophylline with different compounds of natural origin hoping to construct new hybrids with dual activity against cholinergic and inflammatory pathways as potential agents for the treatment of Alzheimer's disease (AD). Out of 28 tested hybrids, two hybrids, acefylline-eugenol 6d and acefylline-isat...

Background liver cancer is one of the most common cancers in the world. So far, there is no gold standard treatment for hepatocellular carcinoma. We conducted this in vitro study to assess the effect of three natural products: Boswellic acids, curcumin and naringin versus corresponding nanoparticles (NPs) on Hep G2 cells proliferation. Methods Bos...

SARS-CoV-2 pandemic in the end of 2019 led to profound consequences on global health and economy. Till producing successful vaccination strategies, the healthcare sectors suffered from the lack of effective therapeutic agents that could control the spread of infection. Thus, academia and the pharmaceutical sector prioritise SARS-CoV-2 antiviral dru...

The biotransformation of vulgarin (1), an eudesmanolides-type sesquiterpene lactone obtained from Artemisia judaica, by the microorganism, Aspergillus niger, was carried out to give three more polar metabolites; 1-epi-tetrahydrovulgarin (1α,4α-dihydroxy-5αH,6,11βH-eudesman-6,12-olide (2), 20% yield, 1α,4α-dihydroxyeudesm-2-en-5αH,6,11βH-6,12-olide...

The low amount of metabolites isolated from natural products is one of the challenges preventing their biological evaluation. The modulation of biosynthetic pathways by stimulating stress-induced responses in plants, was proven to be a valuable tool for diversification of already known natural products. Recently, we reported the dramatic effect of...

Metformin is one of the most prescribed agents in the treatment of type 2 diabetes. Its history goes back to the use of goat’s rue (Galega officinalis Linn., Fabaceae). G. officinalis is rich in galegine, a guanidine derivative with a blood glucose-lowering effect. Research based on the effects of guanidine rich on this traditional herbal medicine...

Background. The aim of this study was the clinical and laboratory evaluation of using polycaprolactone (PCL) nanofibers loaded with oxytetracycline hydrochloride (OTC) and zinc oxide (ZnO) as an adjunct to mechanical therapy in managing stage II grade A periodontitis patients concerning GCF lipocalin2- levels. Methods. Fifty stage II grade A period...

Chemical transformation study is considered as an important tool for new drugs discovery. It was conducted on the natural compound eugenol for semi‐synthesizing new structural scaffolds. Three new eugenol 1,2,3‐triazole derivatives as well as a known one were synthesized via click chemistry using the Cu(I)‐catalyzed azide–alkyne 1,3‐dipolar cycload...

Vanillin (1), the main constituent of vanilla species, was used as a starting natural scaffold for the synthesis of five new (2–6) and one known (7) triazole derivatives via click chemistry using the copper (I)-catalyzed azide–alkyne cycloaddition method. Vanillin and its new derivatives; 4-{1-[2-Hydroxymethyl-5-(5 methyl-2,4-dioxo-3,4-dihydro-2H-p...

Ovarian cancer (OC) is the 7th most common cancer in women world-wide and the 3rd most common female cancer. For the treatment of OC, there is no successful therapeutic. The medications that are currently available have significant side effects and a low therapeutic index. This work aimed to evaluate the anticancer activity of organoselenium pseudo...

The present work provided in vitro anticancer investigation of novel spirooxindole based benzimidazole scaffold SP1 and its nanoformulation with in vivo evaluation of anticancer and antimetastatic activity as potential drug for breast adenocarcinoma. The synthesized compound SP1 exhibited potent growth inhibitory efficacy against four types of huma...

The poor solubility and stability of 6-gingerol (6-G) could hamper its clinical applications. The aim of the current study was to develop a novel ultra-deformable cyclodextrin-functionalized transethoniosomes (CD-TENs) as a promising delivery system for 6-G. Transethoniosomes (TENs) are flexible niosomes (NVs) due to their content of ethanol and ed...

World Health Organization (WHO) declared on March 11, 2020, coronavirus disease, which erupted in December 19th, 2019 in Wuhan, China (COVID-19) as worldwide pandemic disease. Researchers worldwide were successful to provide a prophylactic approach via developing several vaccines, which were swiftly approved by WHO under Emergency Use Listing (EUL)...

Use of Gingerols in pulp treatment may lead to successful pulp treatment by reducing the body's exposure to chemicals and their potential toxicity. This experimental study was performed to compare the effectiveness of Gingerols versus Metapex as obturating material in the treatment of infected pulp in primary premolar teeth of puppies. Gingerols we...

Phenolic compounds represent one of the secondary metabolites of plants with pharmaceutical and therapeutic applications. Flavonoids, quinones, bioflavonoids, neo-lignans, xanthones, curcuminoids, tannins, and coumarins are some examples of the major groups of commonly available phenolic compounds in our daily foods, beverages, and spices. From thi...

Background:Netrin was believed to have a regulating role on the inflammatory reaction via its receptor UNC5B. Thus it takes apart in bone destructive diseases. Periodontitis represent a localized inflammatory bone destructive disease, so Netrin-1could be involved in anti-inflammatory regulation of periodontitis. However, to the best of our knowledg...

A new series of spirooxindole analogs tethered pyrazole scaffold constructed via [3+2] cycloaddition (32CA) reaction starting from the new chalcone named (E)‐3‐(5‐chloro‐3‐methyl‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐1‐(5‐methyl‐1‐phenyl‐1H‐pyrazol‐4‐yl)prop‐2‐en‐1‐one which confirmed by single crystal X‐ray diffraction analysis. Synthesized spirooxindole anal...

In this work, the natural piperine moiety was utilised to develop two sets of piperine-based amides (5a–i) and ureas (8a–y) as potential anticancer agents. The anticancer action was assessed against triple negative breast cancer (TNBC) MDA-MB-231, ovarian A2780CP and hepatocellular HepG2 cancer cell lines. In particular, 8q stood out as the most po...

Twenty-five new hits of spirooxindole analogs 8a–y engrafted with indole and pyrazole scaffolds were designed and constructed via a [3+2]cycloaddition (32CA) reaction starting from three components: new chalcone-based indole and pyrazole scaffolds 5a–d, substituted isatins 6a–c, and secondary amines 7a–d. The potency of the compounds were assessed...

Purpose: To biosynthesize silver nanoparticles (AgNPs) using Psidium guajava L. and Lawsonia inermis L. leaf extracts, and investigate their antioxidant and cytotoxic activities. Methods: The aqueous extracts were prepared by maceration in distilled H2O followed by partitioning with EtOAc. AgNPs were prepared by treating the extracts with 1 mM AgNO...

Plant-derived natural products represent a significant source of green chemical compounds. The fruit extract of Emblica officinalis Gaertn., a traditionally used medicinal plant, was exploited in green synthesis of silver nanoparticles (AgNPs) using AgNO3 reduction method. Characterization of the synthesized AgNPs was achieved using UV–Vis, FTIR sp...

Radiopharmaceutical material is a pharmaceutical product or drug that may exert spontaneous degradation of unstable nuclei with nuclear particles or photons emission. Radiopharmaceuticals may be used in research, diagnosis, therapy, and environmental purposes. Moreover, radiopharmaceuticals act as radioactive tracers among patients via gamma-ray em...

The natural product piperine, the major bioactive alkaloid present in black pepper fruits, has the ability to modulate the functional activity of several biological targets. In this study, we have utilized the natural piperine as a tail moiety to develop new SLC-0111 analogues (6a-d, 8 and 9) as potential carbonic anhydrase inhibitors. Thereafter,...

Triple negative breast cancer (TNBC) is the most aggressive subtype of the breast cancer commonly occurring in females. It was estimated that around 17%–25% of people with breast cancer are triple negative. Despite the availability of various therapeutics and approaches for breast cancer treatment, there is still an increasing need to develop safe...

After decades of restriction of use of Cannabis and cannabinoid, there's increased realization of their importance as potential therapeutic agents. The extensive pharmacological studies revealed their ability to interact with several molecular targets which widen their application in treatment of different diseases, especially immunity related cond...

Seven alkaloids of indole nucleus were isolated from Rhazya stricta (Apocynaceae). Two of which are new epi-rhazyaminine (1) and 20-epi-sitsirikine (2), while the rest are known; eburenine (3), strictamine (4), (16 R)-E-isositsirikine (5), antirhine (6), and strictanol (7). The chemical structures of the isolated compounds were elucidated by interp...

Background Hepatocellular carcinoma (HCC) is the second most common cancer-related death in the world. No effective curative option exists for the treatment of HCC. The available drugs exhibit severe toxic effects and low therapeutic index. Aim This work aimed to examine different monocationic arylthiophene derivatives for possible use as chemothe...

A new lupane caffeoyl ester, lup-20(29)-ene 3β-caffeate-30-al (7), and a new oleanane-type triterpene, 3β-hydroxyolean-13(18)-en-12-one (17), were isolated from the aerial parts of Dobera glabra (Forssk), along with ten known triterpenes, including seven lupane-type lupeol (1), 30-nor-lup-3β-ol-20-one (2), ∆1-lupenone (3), lup-20(29)-en-3β,30-diol...

Background: Chronic periodontitis is a common public health concern characterized by progressive gingival inflammation. Objective: This study assessed the clinical and laboratory effect of diacerein as adjunctive therapy to scaling and root planing (SRP) in the therapeutic management of moderate chronic periodontitis. Methods: This double-blind ran...

Through bio-guided isolation, two natural iron chelators were isolated from Mangifera indica L. leaves, identified as mangiferin (1) and iriflophenone-3-C-β-D-glucoside (2). Their iron-chelating activity was compared to that of Desferal ® using bipyridyl assay and EDTA as a standard. Mangiferin showed the highest activity with IC 50 value of 0.385...

Olea Europaea is an evergreen tree used for centuries to produce oil, diet and medicines. The Olive leaves extract was investigated thoroughly to identify its phytochemical components and its bioactivities, since it showed remarkable pharmacological effect for prevention and treatment experimentally induced metabolic diseases such as cataract , we...

Curcumin is a natural compound that has many medical applications. However, its low solubility and poor stability could impede its clinical applications. The present study aimed to formulate dry proniosomes to overcome these pitfalls and improve the therapeutic efficacy of Curcumin. Curcumin-loaded proniosomes were fabricated by the slurry method a...

[This corrects the article DOI: 10.1371/journal.pone.0134156.].

Purpose The current study aimed to discuss the potential of nanospanlastics as a surfactant-based vesicular system for improving the topical delivery of 3-acetyl-11-keto-β-boswellic acid (AKBA). AKBA is a potent anti-inflammatory drug, but it has poor oral bioavailability due to its poor aqueous solubility. Moreover, the topical delivery of AKBA is...

Sodium valproate (SV) is an antiepileptic drug that is widely used in the treatment of different seizure disorders. The topical SV has a hair regenerative potential through activating the Wnt/β-catenin pathway and anagen phase induction. The aim of the current investigation was to fabricate nanospanlastics of SV for improving its dermal delivery by...

The withdrawal of several blockbuster drugs due to severe adverse effects and the failure of several developed drugs in clinical trials raised questions about the efficacy of current approaches of drug discovery. Moreover, the limitation of resources and the long and costive process of drug discovery made a lot of pharmaceutical companies to employ...

The ability of quinoline alkaloids (cinchonine, cinchonidine, quinine and quinidine) to sensitize different human cancer cell lines to doxorubicin (DOX)‐induced cell death was evaluated. Cell viability was analyzed using MTT assay and the alkaloids ability to enhance DOX‐induced apoptosis was explored using Western Blotting analysis. Also, flow cyt...

Enzyme activity modulation by synthetic compounds provide strategies combining the inhibitory and therapeutic mode of action of the confirmed inhibitors. However, natural modulators could offer a valuable alternative for synthetic ones for the treatment of different chronic diseases (diabetes, hypertension, cancer); due to the numerous side effects...

Hyaluronidase enzyme (HAase) has a role in the dissolution or disintegration of hyaluronic acid (HA) and in maintaining the heathy state of skin. Bioassay-guided fractionation of Ravenala madagascariensis (Sonn.) organ extracts (leaf, flower, stem, and root) testing for hyaluronidase inhibition was performed followed by metabolic profiling using LC...

A one-pot, single-step, and an atom-economical process towards the synthesis of highly functionalized spirooxindoles analogues was efficiently conducted to produce a satisfactory chemical yields (70-93%) with excellent relative diastereo-, and regio-selectivity. An in vitro antiproliferative assay was carried out on different cancer cell lines to e...

Enzyme activity modulation by synthetic compounds provide strategies combining the inhibitory and therapeutic mode of action of the confirmed inhibitors. However, natural modulators could offer a valuable alternative for synthetic ones for the treatment of different chronic diseases (diabetes, hypertension, cancer); due to the numerous side effects...

Considerable attention has been focused on the [1,3] dipolar cycloaddition reaction approach of olefin with amino acid (sarcosine), and isatin which underwent smoothly, and afforded a highly functionalized complex molecule. The target spiroindolone analogue 4 was synthesized in excellent yield. The desired compound was elucidated based on X-ray sin...

The Michael addition reaction of barbituric acid with chalcones incorporating the indole scaffold was achieved by using a highly efficient bimetallic Iron–palladium catalyst in the presence of acetylacetone (acac). This catalytic approach produced the desired products in a simple operation and low catalyst loading with acceptable yield of the new h...

The crystal structures of five new chalcones derived from N-ethyl-3-acetylindole with different substituents were investigated: (E)-3-(4-bromophenyl)-1-(1-ethyl-1H-indol-3-yl)prop-2-en-1-one (3a); (E)-3-(3-bromophenyl)-1-(1-ethyl-1H-indol-3-yl)prop-2-en-1-one (3b); (E)-1-(1-ethyl-1H-indol-3-yl)-3-(4-methoxyphenyl)prop-2-en-1-one (3c); (E)-1-(1-ethy...

Rhazya stricta is a rich indole alkaloid medicinal plant species, that is used in traditional medicine particularly in Middle East countries to treat inflammations, diabetes, rheumatism, and skin disorders. The alkaloid plant extract of R. stricta was fractionated on aluminum oxide column and further purified by different chromatographic methods. T...

Sixteen new analogues were synthesized from ricinine and tested alongside with seven known analogues for their cytotoxic activity against oral cancer (SAS cells) and normal epithelial cells (L132 cells). In contrast to 5-FU, the synthesized ricinine analogues did not show toxicity to normal cells. However, some of them inhibited the proliferation o...

Liver injury is a common problem in numerous common diseases. Caffeine, which is metabolized mainly in the liver, is a widely consumed stimulant that exists in many commonly consumed beverages. Glycyrrhizin (GZ) and boswellic acids (BA) are naturally occurring compounds, isolated from licorice and Olibanumgum, respectively. They have both hepatopro...

Multi-label classification has a great importance in medical data analysis. It means that each sample can associate with more than one class label. Therefore, it represents complex objects by labeling some basic and hidden patterns. The patient may have multiple diseases at one organ, such as the retina, at the same time. The ophthalmological disea...

A new series of pyrazole derivatives was prepared in this work, including pyrazolopyrimidines, pyrazolotriazines, pyrazolylthienopyridines, and 2-(pyrazolylamino)thiazol-4-ones, utilizing 3-amino-5-methyl-1H-pyrazole as a synthetic precursor. Their in vitro anticancer activity was tested on hepatocellular carcinoma cell line, HepG2. The results rev...

An efficient and practical method for the synthesis of 2,6-diaryl-4-oxo-N,N-di(pyridin-2-yl)cyclohexane-1,1-dicarboxamide is described in this present study, which occurs through a double Michael addition reaction between diamide and various dibenzalacetones. The reaction was carried out in dichloromethane (DCM) in the presence of 1,8-diazabicyclo[...

Two isosteric series of 1,2,4‐triazole and 1,3,4‐thiadiazole derivatives were designed and synthesized in this work to be evaluated for their antiviral activity. Compounds 2–9 and 11–19 were synthesized and their antiviral activity was tested against herpes simplex virus type 1, HSV‐1, using acyclovir, ACV, as a reference drug. In addition, molecul...

The designed compounds, 4a–p, were synthesized using a simple and smooth method with an asymmetric 1,3-dipolar reaction as the key step. The chemical structures for all synthesized compounds were elucidated and confirmed by spectral analysis. The molecular complexity and the absolute stereochemistry of 4b and 4e designed analogs were determined by...

We herein report a new small library of Schiff-base compounds that encompasses s-triazine and (2 or 4)-hydroxylbenzylidene derivatives. These compounds were synthesized through a hydrazone linkage connecting both the s-triazine and hydroxybenzylidene derivatives. The synthetic strategy adopted allowed the synthesis of the target compounds with exce...

Background Liver cancer is a life threating disease as it occupies the fifth most common cancers from incidences and the third cause of death worldwide and with no available safe, efficient, economic drug for treatment. Method Therefore, this study intended to investigate different glycyrrhizin and their derivatives for possible use as a cytotoxic...