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Background: Cyclophosphamide (CYP) is a chemotherapy drug widely used in the treatment of several types of cancers and autoimmune disorders. Unfortunately, it causes severe side effects on many organs due to its oxidative stress effect. Objective: The present study aims to tentatively identify the phytochemical constituents of orange fruit (Citrus sinensis) peel extract (OFPE) and elucidate the chemopreventive effects of OFPE on CYP drug induced organ toxicity. Methods: The high performance liquid chromatography coupled with mass spectroscopy (HPLC-MS/MS) technique was used to identify the compounds. Thirty-five male rats were divided into five groups (GP; n = 7): GP1: normal control, GP2: OFPE 0.5 only, GP3: CYP-only, GP4: OFPE 0.25 + CYP, and GP5: OFPE 0.5 + CYP. Results: Twenty-nine compounds of polyphenolic nature, mainly flavonoids, anthocyanidins, phenolic acids and limonoids were characterized by HPLC-MS/MS analysis. Among these compounds, naringin, hesperidin, diosmin, rutin, neohesperidin and limonin were the predominant compounds in the examined extract. Serum cellular markers were found to be decreased significantly upon treatment with OFPE (especially high dose). Also, a significant prophylactic effect against liver, kidney, and heart injuries induced by CYP via decreasing inflammation (serum TNF-α, IL-1β & IL-6) and lipid peroxidation (MDA) was also revealed. Also, an increase in antioxidant levels (serum TAO, and cellular GSH & CAT in tissue homogenates) confirmed the protective efficacy of OFPE against CYP toxicity. Conclusions: The present study reveals some chemopreventive properties and beneficial effects of OFPE on CYP-induced organ toxicity via its antioxidant status and immunoregulatory activities.

A new kaurene derivative with a new 6/6/6/5/6 ring system structure, given the trivial name caspicaiene, was isolated from the fungal culture of the Aspergillus N830 isolate identified by ITS region DNA sequencing. The compound was characterized by 1, 2 D NMR, and HR-ESI-MS-MS and revealed a promising anti-tubercular effect using the Alamar Blue Assay (MABA), in a dose dependent manner, with MIC value of 124.5 µM. Furthermore, six known compounds were isolated and showed significant MIC values against Mycobacterium tuberculosis, ranging between 15.63 µg/mL (26.5 µM) to 125 µg/mL (500 µM), compared to the positive control isoniazid whose MIC value was 0.24 µg/mL (1.75 µM), which sets them forth as potentially natural anti-tubercular agents. To gain further insight of the underlying mechanism, in-silico molecular docking, using the C-Docker protocol, was conducted and demonstrated various interactions between the isolated compounds and three key mycobacterial enzymes. Additionally, the cytotoxic activity was reported and showed the safety of these molecules according to the calculated safety index in the human hepatic cancer cell line (HepG2) and Vero cell lines.

Gastric ulcer is a very common illness that adversely affects a significant number of people all over the globe. Phytochemical investigation of P. glabra leaf alcohol extract (PGLE) resulted in the isolation and Characterization of a new nature compound, quercetin-3- O-α -L-rhamnosyl-(1′''-6′')-(4′'- O -acetyl)-β -D-galactoside (4), in addition to seven known compounds. They are ferulic acid (1), p- coumaric acid (2), quercetin 3-O-α-L-rhamnoside-3′-O-β-D-glucoside (3), quercetin-3- O-α -L-rhamnosyl-(1′''-6′')-(4′'- O -acetyl)- β –Dgalactoside (4), quercetin-3- O—β -D-galactoside (5), 7-hydroxy maltol-3-O-β-D-glucoside (6), maltol-3- O-β -D-glucoside (7), and methyl coumarate (8) that were first to be isolated from the genus Pachira. PGLE demonstrated in vitro anti-Helicobacter pylori activity. Moreover, the in vivo gastroprotective assessment of PGLE at different dosses, 100, 200, and 400 mg/kg against ethanol induced ulceration revealed a dose-dependent gastroprotection comparable to omeprazole. PGLE attenuated gastric lesions and histopathological changes triggered by ethanol. Interestingly, PGLE exhibited an anti-inflammatory effect through down-regulating the expression of nuclear factor-ĸB and pro-inflammatory enzyme cyclooxygenase-2 in the ulcer group. It also hindered apoptosis through decreasing Bax and increasing Bcl-2 expression hence decreasing Bax/Bcl2 ratio with a subsequent reduction in caspase 3 expression. Collectively, P. glabra is a rich reservoir of various phytochemicals reflecting a promising potential for alleviation of gastric ulcer through the mediation of inflammatory and apoptotic cascades.

The Caspian Locust is the common name of Gleditsia caspica, a tree cultivated in the southern and western Caspian Sea in Russia and Iran. Herein, a qualitative characterization of the chemical constituents of Gleditsia caspica leaves extract using ultra-performance liquid chromatography coupled to electrospray ionization tandem mass fragmentation (UPLC-ESI/MS/MS) analysis was performed revealing the presence of nine compounds: six flavonoids, one triterpenoid, one phytosterol, and one long chain ester. Six compounds were newly reported from Gleditsia caspica and two for the first time from genus Gleditsia. Moreover, the in-vivo anti-inflammatory activities of two different doses; 50 and 100 mg/kg of the aqueous-alcoholic extract of Gleditsia caspica leaves were evaluated in the carrageenan-induced paw edema model. The percentage of edema inhibition was calculated after 1, 2, 3, and 4 h of the administration showing a significant reduction in edema thickness in a dose and time-dependent manner compared to the control drug, indomethacin. These results put forward Gleditsia caspica extract as a potential natural anti-inflammatory agent with minimal side effects.

Schinus polygamus (Anacardiaceae) is a shrub cultivated in Egypt for ornamental purpose. The major components of bark oil were dl-limonene (29.74%), followed by myrtenal (14.02%) and caryophyllene oxide (11.34%), while E-caryophyllene (55.86%), dl-limonene (27.71%) and β-pinene (3.54%) were predominant in the leaf oil. These isolated oils were screened for their antimicrobial activity against Staphylococcus aureus ATCC 33591, Staphylococcus aureus ATCC 29213, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 10145, Candida albicans MTCC183 and Aspergillus niger NRRL 595, and two clinical isolates of Staphylococcus aureus. The leaf oil showed a remarkable inhibitory effect against all tested bacterial strains with minimum inhibitory concentration (MIC) range of 25 to 300 µg/mL, while the bark oil was active against Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 10145 only. Furthermore, the bark and leaf oils revealed potent cytotoxic effects on HepG2 and Caco-2 cells with IC50 values of 1.56 to 24.12 µg/mL.

Pachira glabra is a medium sized tree that is famous for its delicious edible seeds and leaves. Phytochemical investigation of Pachira glabra leaf alcohol extract led to the isolation of a new γ-pyrone glycoside, 7-hydroxy maltol-3-O-β-d-glucoside (HMGlu). In vivo assessment of the gastro-protective activity of HMGlu demonstrated superior gastro-protection at a dose of 100 mg kg-1, close to the value triggered by the standard reference omeprazole drug (evidenced by morphological and histopathological examinations). This was further confirmed by immunohistochemical staining where pretreatment with HMGlu (100 mg kg-1) markedly reduced NFκB, COX-2 and BAX positively-stained cells. Thus, it can be concluded that 7-hydroxy maltol-3-O-β-d-glucoside can be a new pharmaceutically active agent with promising gastro-protective activity of natural origin.

The genus

Genus Sophora L. belonging to family Fabaceae comprises about 80 species. It is a heterogeneous genus, ranging from tall trees to small, herbaceous plants. Morphological and genetic characteristics of two Sophora species, viz. S. secundiflora (Ortega) DC. and S. tomentosa L. were subjected to detailed study to delimit these species, where such data are lacking. During this study comparative morphology and anatomy of stem, leaves and petioles of both species was carried out. Moreover, DNA fingerprinting of both plants was carried out using 11 decamer random primers. The obtained results revealed that, many differences in morphological characters viz. the color of the flower, shape of the petiole and leaf dimensions. While the anatomical study reflecting other differential characters among them: the non-glandular hairs and the dimensions of some microelements. The features of the powdered stems and leaves are also described. Moreover, the DNA fingerprinting; created a total of 232 bands, out of the 99 were polymorphic representing a level of polymorphism of 42.67%. The primer (OPO-02) showed the highest degree of similarities (85.71%), while the lowest (35.29%) was recorded by the primer (OPO-10). This study concludes that the retrieved morphological, anatomical and genetic features provide a powerful identification and characterization tool for both of the studied Sophora species; even when used as powdered material. This study is a pioneer regarding the detailed botanical structure of both species; in addition to, the DNA fingerprinting to distinguish these species; in different prescriptions.

Breast cancer is the most common among women cancers and the most likely to cause death. Citrus plants essential oils are reported for having potential cytotoxic activities. Thirty three and thirty...

The volatile oils isolated from both Ocimum basilicum var. purpurascens and Ocimum basilicum var. basilicum, in Yemen, were analyzed by GC/FID and GC/MS. Twenty peaks were detected (100%) in Ocimum basilicum var. basilicum oil where l-Linalool was the highest one (39.0%) followed by cis-anethole (20.0%), guaiol (8.9%) and 1,8-cineole (7.2%). Ocimum basilicum var. purpurascens chromatogram revealed the presence of twenty peaks which represented 100% of the total peaks. l-Linalool (41.8%), α-copaene (22.3%) and 1,8-cineole (10.6%) were the most representative components. Ocimum basilicum var. basilicum, was more effective as antimicrobial agent than Ocimum basilicum var. purpurascens where it showed potent activity against Bacillis subtilis (MIC is 3.90 μL/mL) and moderate activities against both Staphylococcus aureus and Escherichia coli (MIC value for both 7.8 μL/Ml). Ocimum basilicum var. basilicum induced potent antifungal activities against Saccharomyces cerevisiae (MIC 3.90 μL/mL).

A polyphenolic-rich fraction (CG50) was obtained from the methanol extract of Coccinia grandis leaves by chromatographic fractionation over a Diaion column using 50% aqueous methanol. LC-ESI-MS/MS analysis of CG50 showed the presence of six flavonoids, namely quercetin-hexoside deoxyhexoside (rutin), quercetin-hexoside deoxyhexoside (quercetin-3-O-neohesperidoside), kaempferol-hexoside deoxyhexoside (kaempferol-3-O-rutinoside), kaempferol-hexoside deoxyhexoside (kaempferol-3-O-neohesperidoside), kaempferol-3-O-glucoside, and kaempferol-hexoside in addition to the presence of two secoiridoids which are oleuropein and ligstroside. CG50 hydrogel showed a pronounced inhibition of the bacterial growth in wounds infected by Bacillus cereus in rats comparable to those treated with hydrogel base only showing 85.08 and 16.50% inhibition for the bacterial growth for the CG50 hydrogel and hydrogel base, respectively. The antimicrobial activity of CG50 hydrogel was close to that of fucidin during all days of treatment. Rats treated with CG50 hydrogel showed remarkable healing ability of the wound compared to other groups and approaching that of fucidin. This was clearly manifested by the clear formation of scars with obvious reduction in the wound size together with the appearance and re-growth of hair. This was further confirmed by the histopathological study of skin tissues as well as by the evaluation of the percentages of collagen fiber deposition. CG50 hydrogel showed 18.71% collagen fiber deposition comparable to the untreated group that showed 6.84% collagen fiber deposition and approaches that of the fucidin group. It was concluded that Coccinia grandis could be used as a natural wound healing agent that further consolidated its traditional use as a wound dressing.

Morphological and anatomical characters of stem, petiole and leaves of 16 selected medicinal taxa of family Lamiaceae collected from Bani Matar district, Sana'a (Yemen) were examined using both stereo-and light microscopes. The obtained macro-and micromorphological characters (298) were analysed using the software jmp version 13. The resulted dendrogram was discussed on the light of the current taxonomic treatments of Lamiaceae. The measurement of the quantitative characters of macro-and micromorphological characters for the studied taxa was established by multivariate analysis of variance (ANOVA). Evaluation of obtained results revealed that, many characters viz. leaf composition, stomatal types and distribution, number of stamens, stem and petiole vasculature, types of trichomes, nutlet features, number of palisade and spongy layers and types of crystals are of diagnostic value in species identification and delimitation and are potentially valuable at different taxonomic levels. All the quantitative macro- and micromorphological characters except nutlet length are highly significant in species delimitation.

Phytochemical investigation of

Here, we investigated the chemical composition of the edible Phlomis aurea oil and its anticancer potential on three human cancer cell lines, as well as its antiviral activity against Herpes simplex-1 (HSV-1). Exploring Phlomis aurea Decne essential oil by gas chromatography coupled with mass spectrometry (GC/MS) revealed the presence of four major components: germacrene D (51.56%), trans-β-farnesene (11.36%), α-pinene (22.96%) & limonene (6.26%). An antiproliferative effect, as determined by the MTT assay, against human hepatic, breast and colon cancer cell lines, manifested IC50 values of 10.14, 328.02, & 628.43 μg mL-1, respectively. Cytotoxicity assay of the Phlomis oil against Vero cell lines revealed a safe profile within the range of 50 μg ml-1. Phlomis essential oil induced the apoptosis of HepG2 cells through increasing cell accumulation in sub G1 & G2/M phases, decreasing both S & G0/G1 phases of the cell cycle, triggering both caspases-3 &-9, and inhibiting cyclin dependent kinase-2 (CDK2). The antiviral activity of the oil against HSV-1 was investigated using the plaque reduction assay, which showed 80% of virus inhibition. Moreover, the molecular docking in silico study of the four major chemical constituents of the oil at the CDK2 binding site demonstrated marked interactions with the ATP-binding site residues through alkyl & Pi-alkyl interactions. Cell cycle distribution of HepG2 cells was studied using flow cytometry to highlight the apoptotic mechanistic approaches by measuring caspases-3 &-9 and CDK2 activities. Thus, the edible Phlomis oil can be regarded as a candidate for in vivo studies to prove that it is a promising natural antiviral/anticancer agent.

In this study, phytochemical investigations of Aspergillus N830 extract resulted in the isolation and structure elucidation of seven compounds, one of them is a novel carbon skeleton kaurene derivative and is named caspicaiene. The phytoconstituents of Gleditsia caspica leaves were tentatively identified using UPLC-ESI/MS/MS analysis. Eight compounds were identified including six flavonoids, one triterpenoid, and one long chain ester. Our findings suggested for the first time that the new natural product, caspicaiene as well as Aspergillus N830, brassicadiol, aspergillitine and β-sitosterol ferulate could be used in the development of new safer and less resistant alternatives for the management of tuberculosis. The results showed very promising in vivo and in vitro anti-inflammatory activities for both Aspergillus N830 and Gleditsia caspica extracts. Further studies are needed to isolate other anti-inflammatory candidates. Results showed that both Aspergillus N830 and Gleditsia caspica extracts possessed potent anti-allergic activities and were very promising for further anti-allergic studies.

Inflammatory lung diseases such as asthma can be defined as a widely spread chronic inflammatory disease presented with airway hyperresponsiveness, mucus hypersecretion, and remodeling. These diseases may be triggered by genetic predisposition or allergen. Patients are manifested with recurrent episodes of dyspnea, wheezing, shortness of breath, chest tightness, and cough. Conventional therapies used to treat inflammatory lung diseases suffer from limited patient adherence due to their high cost and side effects. Medicinal plants are gaining considerable attention by health care providers due to their favorable therapeutic role, limited side effects, and their potential to be used as adjuvant therapies in the management of inflammatory lung diseases. This book chapter is a summary of pharmacologically studied plant extracts, fractions, and isolated compounds as anti-inflammatory lung diseases agents, especially asthma in different in vitro and in vivo models in the past decade (2010–2020). We also highlighted the medicinal plants, fractions, and isolated compounds with their pharmacological and immunological mechanism of action.

A new biflavonoid, luteolin-(6→8'')-apigenin was isolated from 80% methanol extract of

Phytochemical investigations of Bombacoideae resulted in the identification of almost 160 secondary metabolites belonging to various chemical classes, including flavonoids, lignans, procyanidinds, naphthoquinones, sesquiterpenes, and triterpenes. This chapter sheds light on the recently isolated constituents, as well as the pharmacological activities of different genera of this medicinally valuable Bombacoideae. Flavonoids constituted the most prevailing class of secondary metabolites, representing 27% of total isolated compounds, followed by sesquiterpenes and fatty acids. Inhibition of nitric oxide synthase, cyclooxygenases, and pro-inflammatory cytokines, together with the antioxidant potentials were the major mechanisms adopted by the most-studied Bombacoideae members and their isolated compounds. The anti-inflammatory potential was most commonly ascribed to the flavonoid content and to a lesser extent to other metabolites, such as fatty acids, despite the possibility of contribution of other reported secondary metabolites having anti-inflammatory potential, such as tannins and triterpenes. Major compound classes identified include naphthoquinone derivatives, flavonoids, coumarins, sesquiterpenes, and triterpenes.

Background and study aim Peptic ulcer is one of the most serious diseases in Egypt, affecting more than one-third of the population. Helicobacter pylori is the main organism responsible for peptic ulcer formation. These ulcers can lead to chronic active gastritis and lymphoma. As such, in this study, we evaluate the efficacy of Pelargonium graveolens oil for the treatment of H pylori, as well as its synergistic effects with the antibiotic clarithromycin (CLR). Patients and methods We evaluated the chemical composition of P. graveolens volatile oil as well as its anti-Helicobacter activities. We assessed the volatile oil components using gas chromatography coupled with mass spectrometry. We determined anti-H. pylori potential using a micro-well dilution method. Results We identified 92 compounds from the oil. Citronellol , geraniol , citronellyl formate , and isolongifolan-7- α-ol were the predominant components (15.64%, 11.31%, 10.19%, and 7.84%, respectively). The oil exhibited a good activity against H. pylori at an minimal inhibitory concentration of 15.63 µg/ml. Once we combined the volatile oil with CLR, a significant synergistic effect appeared at an fractional inhibitory concentration index of 0.38 µg/ml. Conclusion The in-vitro interaction between the P. graveolens oil and CLR improved the antimicrobial activity of the latter, suggesting that further studies are needed to determine formulations for potential antimicrobial applications in food and pharmaceuticals.

A new kaurene derivative with a new 6/6/6/5/6 ring system structure, given the trivial name caspicaiene, was isolated from the fungal culture of the

Five flavonoids were isolated from the ethyl acetate fraction of leaves of

Rhoifolin (Rho) exerts many biological activities such as anticancer, antidiabetic, hepatoprotective, antirheumatic, antibacterial, and antiviral properties. The neuroprotective action of this compound has not been studied. The goal of this study was to investigate the improvement impact of Rho on scopolamine (Sco)-induced zebrafish anxiety, amnesia, and brain oxidative stress and to elucidate the underlying mechanisms involved. Zebrafish were treated with Rho (1, 3, and 5 &mu, g/L) for nine consecutive days and were subsequently subjected to Sco (100 &mu, M) 30 min before behavioral tests (novel tank diving test, Y-maze, and novel object recognition tests). Rho was isolated from Chorisia crispiflora (Malvaceae) leaves and identified by different spectroscopic techniques. To further assess the possible mechanisms of Rho in enhancing the memory capacities in zebrafish, the in vivo antioxidant status and acetylcholinesterase (AChE) activity was also evaluated. Rho from Chorisia crispiflora leaves was identified. Rho could alleviate anxiety, memory deficits, and brain oxidative stress in Sco-treated zebrafish and could regulate the cholinergic function by inhibiting the AChE activity. Our results demonstrated that Rho could be a promising candidate compound against anxiety and amnesia by restoring the cholinergic activity and the amelioration of brain oxidative stress.

Gastric ulcer is a very common illness that adversely affects a significant number of people all over the globe. Phytochemical investigation of P. glabra leaf alcohol extract (PGLE) resulted in the isolation and Characterization of a new nature compound, quercetin-3- O-α -L-rhamnosyl-(1'''-6'')-(4''- O -acetyl)-β -D-galactoside (4), in addition to seven known compounds. They are ferulic acid (1), p- coumaric acid (2), quercetin 3-O-α-L-rhamnoside-3'-O-β-D-glucoside (3), quercetin-3- O-α -L-rhamnosyl-(1'''-6'')-(4''- O -acetyl)- β -Dgalactoside (4), quercetin-3- O-β -D-galactoside (5), 7-hydroxy maltol-3-O-β-D-glucoside (6), maltol-3- O-β -D-glucoside (7), and methyl coumarate (8) that were first to be isolated from the genus Pachira. PGLE demonstrated in vitro anti-Helicobacter pylori activity. Moreover, the in vivo gastroprotective assessment of PGLE at different dosses, 100, 200, and 400 mg/kg against ethanol induced ulceration revealed a dose-dependent gastroprotection comparable to omeprazole. PGLE attenuated gastric lesions and histopathological changes triggered by ethanol. Interestingly, PGLE exhibited an anti-inflammatory effect through down-regulating the expression of nuclear factor-ĸB and pro-inflammatory enzyme cyclooxygenase-2 in the ulcer group. It also hindered apoptosis through decreasing Bax and increasing Bcl-2 expression hence decreasing Bax/Bcl2 ratio with a subsequent reduction in caspase 3 expression. Collectively, P. glabra is a rich reservoir of various phytochemicals reflecting a promising potential for alleviation of gastric ulcer through the mediation of inflammatory and apoptotic cascades.

Background: Diabetes mellitus (DM) represents a global health problem characterized by hyperglycemia due to insufficient insulin secretion or failure of insulin activity. There is an imperative need for the discovery of alternative therapeutic agents that overcome the drawbacks of the current synthetic antidiabetic drugs. Objectives: This review critically summarizes the reports on the known and novel natural compounds, including alkaloids, flavonoids, and saponins with a potent antidiabetic activity that were recently published from 2014 to 2019. We discussed the underlying mechanisms of action that put these compounds in the category of effective antidiabetic candidates. Discussion and Conclusion: The reported natural compounds showed promising antidiabetic activity through different mechanisms such as the inhibition of α-amylase, α-glucosidase, insulin-sensitizing effect, direct action on protein tyrosine phosphatase 1B (PTP1B), peroxisome proliferator-activated receptors (PPARs), GLUT4 expression, insulin receptor substrate-1 (IRS-1) and glycogen synthase kinase-3β (GSK-3β) as well as dipeptidyl peptidase-4 (DPP-4) enzyme. Some compounds inhibited the formation of advanced glycation end products (AGEs). Other compounds prevented the risk of diabetic complications such as cardiovascular diseases, retinopathy, and nephropathy. This review provides a critical overview of the most recent discoveries of antidiabetic agents from natural sources. This overview could help researchers to focus on the most prominent candidates aiming to develop new drug leads.

Metabolic profiling of the hexane extract and essential oil of

Five flavonoids were isolated from the ethyl acetate fraction of leaves of Sophora secundiflora; formononetin (1), 5-hydroxy-4’-methoxyflavone (2), genistein (3), 5-hydroxy-8-(1-hydroxy-1-methyl-ethyl)-2-(4-hydroxyphenyl)-4H-furo-[2, 3-h]-chromen-4-one (4) and ononin (5). Additionally, LC-ESI-MS/MS analysis of the ethyl acetate fraction of S. secundiflora leaves had led to tentative identification of eighteen compounds. Formononetin, S. tomentosa and S. secundiflora leaves methanolic extract were evaluated in vivo for their neuroprotective activity where formononetin and S. tomentosa showed promising neuroprotective activity with reduction in acetylcholine esterase (AchE) enzyme activity and elevation of acetylcholine (Ach) and glutathione(GSH) brain levels and attenuation of dopamine (DA), nor-adrenaline (NA) and malonedialdehyde (MDA) brain level significantly, However S. secundiflora leaves methanolic extract didn’t attenuate the AchE enzyme activity, DA and NA brain levels.

A new biflavonoid, luteolin-(6→8'')-apigenin was isolated from 80% methanol extract of Schinus polygama (Cav.) Cabrera leaves (Anacardiaceae). The structure was elucidated by 1D and 2D-NMR spectroscopic data. This compound exhibited in vitro antidiabetic effect via α-amylase assay. Furthermore, it possesses anti-inflammatory activity through membrane stabilization effect on erythrocytes.

Metabolic profiling of the hexane extract and essential oil of Cordia africana Lam., an economically important agroforestry species, was performed using GC-FID and GC-MS. Cytotoxicity was assessed in MCF-7 cancer cells using sulphorhodamine-B assay. Caspase-8, BcL-2 and Ki-67 levels were evaluated using enzyme-linked immunosorbent assay. Forty-one compounds were identified in the hexane extract, meanwhile, eighty compounds were annotated in the essential oil. n-Decane (9.52%), β-sitosterol (8.13%), undecane (6.32%) and palmitaldehyde (5.50 %) were the major compounds identified in the hexane extract, whereas, β-caryophyllene (32.0%), germacrene D (10.12%) and δ-cadinene (7.20%) predominated in the essential oil. The half maximal inhibitory concentrations (IC50) of the extract and oil were 4.55 µg/mL and 12.90 µg/mL, respectively. Caspase-8 activity increased significantly in hexane extract treated cells. Furthermore, BcL-2 and Ki-67 protein expression levels were significantly decreased. Cordia africana Lam exhibit potent cytotoxicity against breast cancer cell line, most likely through apoptosis regulation.

The leaves and stems of the two Pachira species cultivated in Egypt, namely Pachira aquatica, and Pachira glabra were qualitatively and quantitatively examined for their volatile constituents emplo...

The gastroprotective effect of Ocimum basilicum L. (Basil) hexane extract (OBHE) in aspirin-induced gastric ulcers in mice and its ameliorative effect on behavioral alterations were determined. Pretreatment with OBHE (100 or 200 mg kg-1) or misoprostol (50 μg kg-1) alleviated the aspirin-induced oxidative stress by significantly decreasing (p < 0.001) gastric ulcer index scores (57, 76 and 79%), gastric TBARS (by 49, 51 and 52%), NO (21, 28 and 29%), H2O2 (24, 42 and 45%), and the serum pro-inflammatory mediator TNF-α (21, 53 and 53%) and IL-6 (29, 30 and 31%), as well as by markedly increasing gastric GSH (41, 61 and 70%), GSH-Px (21, 32 and 34%), GST (33, 63 and 70%), GR (90, 99 and 112%), CAT (167, 211 and 267%) and serum PGE-2 levels (22, 135 and 200%) and IL-4 (64, 81 and 104%), respectively, compared with the aspirin-treated group. Meanwhile, OBHE and misoprostol induced a significant decrease (p < 0.001) in the freezing time (53, 56 and 64%), and the grooming time (by 25, 43 and 44%), respectively, compared to the aspirin treated group. This study provides evidence that OBHE confers anxiolytic, antioxidant and anti-inflammatory prophylactic effects on aspirin-induced gastric ulcers. GC/MS was used for the characterization of OBHE components. Based on the findings of this study, basil may be used as a nutritional supplement or therapeutic drug to protect against aspirin-induced gastric ulcers, a common problem resulting from the use of aspirin.

Rheumatoid arthritis (RA) is the most common human autoimmune disease. A petroleum ether extract of Eugenia aquea (E. aquea) was analyzed by GC/MS. Antioxidant and anti-inflammatory activities were investigated in rats with adjuvant-induced arthritis (AIA). An AIA rat model received orally/daily a vehicle, diclofenac (100 mg per kg b.w.), and E. aquea extract (50 or 100 or 200 mg per kg b.w.; for 21 days). Fifty-five out of 70 compounds (97.77%) were identified: eucalyptol (34.14%), α-pinene (15.91%), l-verbenone (8.01%), camphor (7.38%) and borneol (6.74%). In an acute oral toxicity study, the E. aquea extract did not show any toxic effects in rats at 2000 mg/ kg-1. Only a high dose of the E. aquea extract or diclofenac significantly alleviated (P < 0.05-0.001) all complications observed in arthritic rats, including body weight loss, articular/extra-articular oxidative injury and synovial joint inflammation by increasing food intake as well as improving the antioxidant defense system and inflammatory marker. The dose-dependent modulatory activity of the E. aquea extract was statistically significant. It was equivalent to and sometimes even better than that of diclofenac. The present study proved the antioxidant and anti-inflammatory activities of the E. aquea extract, which could be attributed to the presence of eucalyptol and α-pinene.

Preclinical Research Nine known phenolic compounds were isolated from an aqueous methanolic extract of Acrocarpus fraxinifolius Weight and Arn leaves (AFL) family Fabaceae. This extract of AFL contained approximately 169 mg gallic acid/g as assessed by HPLC. The AFL extract had marginal antitumor activity (IC50 > 200 µL/mL) but showed a concentration-dependent hepatoprotective effect against CCl4 -induced hepatotoxicity in vitro. Cell viability was increased, ALT and AST activity declined and reduced GSH concentration and SOD activity were restored as compared with silymarin. In vivo concurrent administration of AFL extract (500 mg/kg po) showed a hepatoprotective effect against gamma irradiation and CCl4 as evidenced by reduction of TNF-α, interleukin-6, malondialdehyde, nitric oxide, DNA fragmentation, caspase-3 activity, and downregulation of its m-RNA level and decreased proapoptotic protein Bax expression. AFL extract enhanced glutathione peroxidase, superoxide dismutase, and catalase activities, reduced glutathione concentrations and upregulated the expression of antiapoptotic Bcl-2. The extract could ameliorate hepatic injuries induced by gamma irradiation and CCl4 in rats suggesting potent hepatoprotective activity. Drug Dev Res 78 : 210-226, 2017. © 2017 Wiley Periodicals, Inc.

High-Performance Liquid Chromatography (HPLC) was developed for the standardization and quantification of gallic acid in the methanolic extract of Acrocarpus fraxinifolius Weight & Arn leaves. Linearity was observed in the range of 0.4–2 mg/mL with a correlation coefficient (r2) of 0.9978. The limit of detection (LOD) and limit of quantification (LOQ) were 0.0054 mg/mL and 0.0163 mg/mL, respectively indicating the sensitivity of the applied method. Recovery values of 100.377 % indicate the best accuracy of the method. Gallic acid content was quantified as 168.75 ± 1.05 mg/g methanolic extract. This developed method was simple, accurate and precise to be used as a reference standard method for determination of gallic acid content in the plant extract.

The chemical composition, pharmacological activity and traditional uses of 20 species attributed to the genus Enterolobium (Fabaceae) as used in the South and Central America, and Tropical Africa, were revised and compared. A survey of the available literature shows that these species are used mostly for their anti-inflammatory and cytotoxic activities. Additionally, some of these Enterolobium species showed antibacterial, antifungal, insecticidal, molluscicidal and larvicidal activities. Generally, the triterpenes or the phenolic compounds isolated from these plant extracts are assumed to be the bioactive principles.

Context: Nothing could be found in the literature concerning Cinnamomum glanduliferum (Wall) Meissn (Lauraceae) bark (CG) in Egypt. Objective: To investigate CG volatile oil chemically and its anti-inflammatory and gastroprotective effects. Materials and methods: Essential oils were investigated by GC-MS. Leaves oil was assessed at doses of 250, 500 and 1000 mg/kg for its anti-inflammatory effect against carrageenan-induced rat oedema model. Serum inflammation markers were measured. The gastro-protective effect of the same doses of the volatile oil was also tested in ethanol-induced non-ulcerative gastritis model in rats. Stomach oxidative stress markers were examined following 1 h after intragastric ethanol administration. Results: Twenty-five and 20 compounds were identified from leaf and branch oils, respectively (98.85 and 99.13%). The major ones were: eucalyptol (59.44%; 55.74%), sabinene (14.99%; 7.12%), α-terpineol (6.44%; 9.81%), α-pinene (5.27%; 4.71%). Following 4 h of treatment leaves volatile oil at doses of 250, 500 and 1000 mg/kg significantly reduced paw volume to 94, 82 and 69%, respectively. The same doses significantly reduced COX-2 activity to 73.8, 50.7 and 21.4 nmol/min/mL, respectively. A significant reduction of PGE2 concentration was observed (2.95 ± 0.2, 2.45 ± 0.15 and 1.75 ± 0.015 pg/mL). CG oil exhibited a significant modulatory effect on ethanol-induced gastritis in rats as the level of NO reduced to 32, 37 and 41 μM nitrate/g and also a significant inhibition of lipid peroxidation was observed via reduction of MDA concentration (1.15, 1.11 and 1.04 nmol/g). Conclusion: CG volatile oil exhibited an anti-inflammatory effect and protected against ethanol-induced non-ulcerative gastritis.

Context: In Egypt, the burden of liver diseases is exceptionally high. Objective: To investigate the components of the n-hexane extract of Acrocarpus fraxinifolius Arn. (Leguminosae) and its hepatoprotective activity against paracetamol (APAP)-induced hepatotoxicity in rats. Material and methods: TRACE GC ultra gas chromatogaphic spectrometry was used for extract analysis. Thirty albino rats were divided into six groups (five rats in each). Group 1 was the healthy control; Groups 2 and 3 were healthy treated groups (250 and 500 mg/kg b.w. of the extract, respectively) for seven days. Group 4 was hepatotoxicity control (APAP intoxicated group). Groups 5 and 6 received APAP + extract 250 and APAP + extract 500, respectively. Results: Chromatographic analysis revealed the presence of 36 components. Major compounds were α-tocopherol (18.23%), labda-8 (20)-13-dien-15-oic acid (13.15%), lupeol (11.93%), phytol (10.95%) and squalene (7.19%). In the acute oral toxicity study, the mortality rates and behavioural signs of toxicity were zero in all groups (doses from 0 to 5 g/kg b.w. of A. fraxinifolius). LD50 was found to be greater than 5 g/kg of the extract. Only the high dose (500 mg/kg b.w.) of extract significantly alleviated the liver relative weight (4.01 ± 0.06) and biomarkers, as serum aspartate aminotransferase (62.87 ± 1.41), alanine aminotransferase (46.74 ± 1.45), alkaline phosphatase (65.96 ± 0.74), lipid profiles (180.39 ± 3.51), bilirubin profiles (2.30 ± 0.06) and hepatic lipid peroxidation (114.20 ± 2.06), and increased body weight (11.58 ± 0.20), serum protein profile (11.09 ± 0.46) and hepatic total antioxidant capacity (23.78 ± 0.66) in APAP-induced hepatotoxicity in rats. Conclusion: Our study proves the antihepatotoxic/antioxidant efficacies of A. fraxinifolius hexane extract.

This study investigated the antifibrotic effect of Prosopis juliflora leaves crude methanolic extract (PJEL) against thioacetamide (TAA)-induced liver fibrosis. The phytochemical analysis of PJEL was performed via HPLC/MS in association with evaluating its free radical scavenging and cytotoxic activities. The antifibrotic activity of PJEL was assessed by dividing Wistar rats into 8 groups: normal control, PJEL1-administered rats (2 mg/ Kg b.w.), PJEL2-administered rats (4 mg/ Kg b.w.), PJEL3-administered rats (8 mg/Kg b.w.), TAA-induced hepatic fibrosis, TTA + PJEL1, TAA + PJEL2, and TAA + PJEL3. Results indicated that PJEL crude methanolic extract is rich in polyphenolic compounds and alkaloids. PJEL exerted free radical scavenging activity with IC50 of 123.5 μg/mL and cytotoxic activity against a well-differentiated hepatocellular cell line (IC50 = 11.1 μg/mL). PJEL at a dose of 4 mg/Kg b.w. ameliorated serum ALT activity and improved serum albumin level and hepatic hydroxyproline content in association with a reduction in the fibrosis stage. PJEL elevated hepatic tumor necrosis factor-α and interleukin-6 contents with less necrosis grade. PJEL post-therapy ameliorated the relative expression of Bcl-2, Col1A1, Mmp-9, and Mmp-2 genes in liver. Conclusion PJEL possesses a good therapeutic activity against TAA-induced liver fibrosis via enhancing extracellular matrix removal and stimulating hepatic regeneration to decrease hepatic necrosis.

Background The genus Sophora (Fabaceae) represents one of the important medicinal plant genera regarding its chemical constituents and outstanding pharmacological activities. Purpose In this review, we surveyed the latest findings on the bioactivities of different Sophora extracts and isolated phytochemicals during the past 8 years (2011–2019) updating the latest review article in 2011. The aim of this review is to focus on the molecular pharmacology of Sophora species to provide the rationale basis for the development of novel drugs. Results Sophora and its bioactive compounds possess outstanding pharmacological properties, especially as anticancer and anti-inflammatory drugs, in addition to its antioxidant, antibacterial, antifungal and antiviral properties. Conclusion Based on their use in traditional medicine, Sophora species exert a plethora of cellular and molecular activities, which render them as attractive candidates for rationale drug development. Randomized, placebo-controlled clinical trials are required for further integration of Sophora-based phototherapies into conventional medicine.

In this study, preliminary phytochemical screening of dried leaves of Coccinia grandis showed presence of triterpenoids, phenolics, flavonoids, saponins and sterols. As well as, five phenolic compounds namely; ferulic acid (1), methyl caffeate (2), ligstroside(3), trans-p- coumaric acid (4) and kaempferol-3-O-β-D-glucoside (5) were isolated from selected fraction of the methanol extract of Coccinia grandis leaves. The structures of the isolated compounds were identified using different NMR spectroscopic techniques (1H, 13C NMR, COSY, HSQC, HMBC) and mass spectrometry. Compounds (1), (2), (4) and (5) were isolated for the first time from Coccinia grandis species while compound (3) was isolated for the first time from Cucurbitaceae family. Moreover, the anti-microbial activity of the selected fraction of the methanol extract of Coccinia grandis leaves was tested against a panel of Gram-positive, Gram-negative bacteria and yeast. A considered activity was recorded against Bacillus cereus (inhibition zone of 20 mm with MIC 1mg/ml).

Schinus terebinthifolius is a plant well recognized for its therapeutic profile such as anti-inflammatory and antitumor activities, promoting antibacterial activity and antioxidant and antidiabetic properties. This study aimed at examining whether Schinus terebinthifolius memory-enhancing activities are mediated by cholinergic and brain antioxidant systems in a scopolamine zebrafish model. Schinus terebinthifolius essential oil (10, 25, and 50 μL/L) was delivered to zebrafish by immersion in water for 8 days. Memory deficits were induced by scopolamine (100 μM) administration. Zebrafish were divided into seven groups (n = 15/group): vehicle group, scopolamine (100 μM) group, Schinus terebinthifolius essential oil groups (STF; 10, 25, and 50 μL/L), the imipramine group (IMP; 20 mg/L, as the positive control in the NTT test), and the donepezil group (DP; 10 mg/L, as the positive control in the Y-maze test). Memory status was estimated by the novel tank diving test (NTT) and the Y-maze test and finally was validated by comparison with imipramine (20 mg/L) and donepezil (10 mg/L). Gas chromatography-mass spectrometry (GC-MS) was used to detect oil compounds. Brain levels of acetylcholinesterase (AChE) and antioxidant enzymes were measured. After being exposed to Schinus terebinthifolius essential oil, the scopolamine zebrafish exhibited an improvement of memory processes in the NTT and Y-maze tests. The essential oil attenuated the elevated level of AChE and brain oxidative stress. Schinus terebinthifolius essential oil was found to support memory formation through the inhibition of the AChE activity and decreasing oxidative stress in the scopolamine-treated zebrafish brains.

Ethnopharmacological relevance Pulicaria incisa sub. candolleana E. Gamal-Eldin (Asteraceae) was traditionally used by Bedouins as a refreshing tea and as hypoglycemic, in gastrointestinal ailments, sinusitis and headache. Recently a great correlation has been established between liver cirrhosis and gastrointestinal dysfunction reflected by abdominal bloating, pain, diarrhea, constipation, besides decreased food intake. So far, the hepatoprotective effect of P. incisa sub. candolleana E. Gamal-Eldin was not studied before although other Pulicaria species have previously shown hepatoprotective and antioxidant effects. Aim of the study In this study, we aimed to identify the phytochemical constituents of the P. incisa sub. candolleana E. Gamal-Eldin hydroethanolic extract (PICE), as well as to evaluate the hepatoprotective, anti-inflammatory and antioxidant activities in methotrexate (MTX)- intoxicated rats. Besides, the molecular interaction between the isolated compounds and cyclooxygenase-2 (COX-2) and phospholipase 2 (PLA-2) were assessed by in-silico screening. Material and methods The main phytoconstituents were characterized using liquid chromatography-tandem mass spectrometry (LC-MS-MS). Vacuum liquid chromatography (VLC) aided by preparative high-performance liquid chromatography (HPLC) were also used to isolate the major phenolics from the hydroethanolic extract. Their structures were elucidated using different spectroscopic analysis methods, including 1D and 2D nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI/MS). The hepatoprotective activity of three doses (100, 250, 500 mg/kg) of PICE in MTX-intoxicated rats was assessed and compared to silymarin as a standard. Additionally, in silico docking study on cyclooxygenase-2 (COX-2) and phospholipase 2 (PLA-2) was performed to justify the anti-inflammatory activity of the isolated compounds. Results Thirteen compounds were tentatively identified, including flavonoids and phenolic acids. Four main isolated compounds were identified as, eugenol-1-O-β-glucoside, 5-O-caffeoylquinic acid, 3, 5-di-O-caffeoylquinic acid and quercetin-3-O-β-glucoside. Treatment of MTX-intoxicated rats with the 250 mg/kg extract reversed the altered levels of biochemical markers of liver damage, ameliorated the oxidant status and reduced the inflammatory mediators, similar to treatment with silymarin. Quercetin-3-O-β-glucoside showed the best docking energy score of −19.12 kcal/mol against COX-2, forming four binding interactions with residues Leu 353, Arg 121, Tyr 356 and Ala 528, followed by 3,5-di-O-caffeoylquinic acid (−18.01 kcal/mol). Conclusion This study reveals P. incisa sub. candolleana as a rich source of phenolics including flavonoids, supporting its anti-inflammatory and hepatoprotective effects and suggesting its usage as a promising candidate in inflammatory conditions.