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Tuberculosis is a highly infectious ailment worldwide. The emergence of multi-drug resistance and serious adverse effects of anti-TB drugs have led to the continuous search of natural candidates. This study aimed to analyse the chemical profile of Vitex pinnata (VP) bark lipophilic extract using GC-MS also evaluating its anti-TB and cytotoxic activities. GC-MS revealed a total of 81 compounds which representing 86% identified compounds. In vitro anti-TB of VP lipophilic extract was evaluated using the Microplate Alamar Blue Assay which exhibited MIC value of 62.5 µg/mL. In vitro cytotoxicity was evaluated using Water Soluble formazan assay recording IC50 > 100 and 200 µg/mL using Vero and A-549 cell lines, respectively. In silico docking study was performed on the major identified compounds, n-nonane showed the most favourable binding affinity (ΔG) equals to −33.34 Kcal/mol. The results obtained herein unravelled the potential use of VP n-hexane extract as a natural anti-TB.

Rising awareness about the ecological burden of agricultural by-products and their potential industrial and medicinal applications spurred the research of waste valorization. Egypt is a chief producer of jasmine oils. However, jasmine-dense foliage is an agricultural waste that merits exploitation. Herein, Jasminum grandiflorum leaves were profiled using UPLC-MS, revealing a promising phytochemical composition rich in secoiridoids. A good safety profile was confirmed in vitro on cancerous and normal cell lines and in vivo (LD50>4000mg/kg). The radioprotective effect of 3500 mg/kg jasmine leaves extract against irradiation-induced lung injury was demonstrated. Biochemical analysis indicated that jasmine extract decreased malondialdehyde level and enhanced the endogenous antioxidants GSH-Px, SOD and CAT levels. Jasmine alleviated the inflammatory response by downregulating the expression of COX-2 and iNOS and reducing the inflammatory mediators, TNF-α, IL-6, NO, and PGE2. Jasmine leaves offer interesting application prospects that add economic and industrial value to agricultural waste.

Phytochemical investigation of Sophora secundiflora alkaloid fraction led to isolation of one new quinolizidine alkaloid (1) 13-methoxyanagyrine together with six known ones (2–7). The insecticidal activity of 70% methanol extract of leaves of S. secundiflora, S. tomentosa and the isolated alkaloids were assessed against 3rd instar larvae of Culex pipiens (Diptera: Culicidae) using different concentrations and mortality rate was recorded. Sophora tomentosa extract showed highest mortality rate with median lethal concentration LC50 3.11 ppm after 24 h and 0.66 ppm after 48 h and anagyrine (6) exhibited remarkably insecticidal activity with LC50 value of 3.42 ppm after 24 h of exposure. Additionally, cytotoxic activity of alkaloid fraction of S. secundiflora, S. tomentosa and isolated alkaloids was also studied using crystal violet assay against MCF-7 and HEPG-2 cell lines. Anagyrine (6) exhibited IC50 values of 27.3 ± 0.7 and 30.2 ± 0.9 µg/mL against MCF-7 and HEPG-2 cancer cells, respectively.

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.

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.

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...

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.

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.

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.

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.

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...

Two new oleanane-type saponins: β-d-xylopyranosyl-(1 → 4)-6-deoxy-α-l-mannopyranosyl-(1 → 2)-1-O-{(3β)-28-oxo-3-[(2-O-β-d-xylopyranosyl-β-d-glucopyranosyl)oxy]olean-12-en-28-yl}-β-d-glucopyranose (1) and 1-O-[(3β)-28-oxo-3-{[β-d-xylopyranosyl-(1 → 2)-α-l-arabinopyranosyl-(1 → 6)-2-acetamido-2-deoxy-β-d-glucopyranosyl]oxy}olean-12-en-28-yl]β-d-glucopyranose (2), along with two known saponins: (3β)-3-[(β-d-Glucopyranosyl-(1 → 2)-β-d-glucopyranosyl)oxy]olean-12-en-28-oic acid (3) and (3β)-3-{[α-l-arabinopyranosyl-(1 → 6)-[β-d-glucopyranosyl-(1 → 2)]-β-d-glucopyranosyl]oxy}olean-12-en-28-oic acid (4) were isolated from the acetone-insoluble fraction obtained from the 80% aqueous MeOH extract of Albizia anthelmintica Brongn. leaves. Their structures were identified using different NMR experiments including: 1 H- and 13 C-NMR, HSQC, HMBC and 1 H,1 H-COSY, together with HR-ESI-MS/MS, as well as by acid hydrolysis. The four isolated saponins and the fractions of the extract exhibited cytotoxic activity against HepG-2 and HCT-116 cell lines. Compound 2 showed the most potent cytotoxic activity among the other tested compounds against the HepG2 cell line with an IC50 value of 3.60μm. Whereas, compound 1 showed the most potent cytotoxic effect with an IC50 value of 4.75μm on HCT-116 cells.

A novel biflavonoid [kaempferol (6→8″) apigenin] was isolated from the leaves of Jacaranda acutifolia. The structure was elucidated based on chemical evidence, 1D and 2D spectroscopic analyses as well as spectrometric techniques. The compound showed promising cytotoxic activity against breast cancer cell line MCF-7. The anticancer activity was explained via virtual docking of the isolated compound to the main sites in the human cyclin-dependent kinase2 (CDK2) crystal structure.

Hepatocellular carcinoma is considered the third most common cause of cancer-related death worldwide. Thus, the present study was designed to test for the first time the putative cytotoxic effect of Delonix regia extract, besides its hepatoprotective activity. In this context, this study targets four specific aims; first, the phytochemical investigation of D. regia extract which led to the isolation of seven flavonoid glycosides; Kaempferol 3-rhamnoside 1, Quercetin 3-rhamnoside 2, Kaempferol 3-glucoide 3, Kaempferol 3-rutinoside 4, Kaempferol 3-neohesperidoside 5, Quercetin 3-rutinoside 6 and Quercetin 3-glucoside 7. Second, the evaluation of in vitro cytotoxic activity of the extract, where the extract exhibited a potent cytotoxic effect against HepG2 cell line. Third, the hepatoprotective activity was investigated using carbon tetrachloride (CCl4)-induced liver injury. The plant extract at dose of 50, 100 and 200 mg/kg body weight reduced serum aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase as well as total and direct bilirubin in a dose dependent manner. The fourth aim was the investigation of the antioxidant activity of the extract as the treatment of rats with the extract at different doses significantly increased the liver tissue level of superoxide dismutase, catalase, reduced glutathione and total antioxidant capacity and decreased the level of malondialdehyde as compared to CCl4 treated group. The current findings concluded that the extract of D. regia possessed not only a significant anticancer effect against HepG2 cells, but also an effective and a dose dependent hepatoprotective and antioxidant activities due to the presence of flavonoids content.

Results of GC and GC-MS analysis of essential oil isolated from doum fruits (Hyphaene thebaica) revealed the presence of fifty-seven compounds. Fifty of them could be identified with monoterpenes represent 15.97 % including compounds such as sabinene (0.82 %), β-pinene (1.98 %), limonene (2.42 %), terpinen 4-ol (1.77 %) %), α-terpineol (0.95 %). While diterpenes represent 40.49 %, of which incensole (17.52 %) and incensole acetate (19.81 %) were found to be the main components. Oxygenated compounds constituted 66.78 % of the total compounds identified which indicated the economical value of this oil. The scent of doum oil fruits may be attributed to the presence of volatile diterpenes as cembrene A, cembrene C, incensole and incensole acetate; these compounds are reported here for the first time in family Palmae.

Breast cancer constitutes the second most prevalent cancer in Egypt, the problem needs more trends in treatment and treatment development either by regimen modification or introducing new drugs, and the main objective of this study is to screen the effects of the aqueous ethanol herbal extract of Luffa cylindrica leaves on different types of breast cancer cell lines representing different molecular subtypes of the disease. The major active constituents of the extract were tentatively identified by LC/MS which revealed the presence of phenolic compound derivatives and saponin that may be responsible in part for the activity of the extract. The emphasis was laid on the main apoptotic pathways as well as the extract effect on the normal cell line. Results of phytochemical investigation, cell cycle analysis, and molecular analysis of apoptotic and proliferative markers have shown effective anticancer activity against MCF-7, BT-474, and MDA-MB-231 cell lines which represent three subtypes of breast cancer, luminal A, luminal B, and triple negative, respectively. On the other hand, the effects on normal lung fibroblast cell line are less prominent at the dose used for treating breast cancer cell lines.

Flavonoids are agents with strong antioxidant properties and ameliorate many diseases associated with oxidative stress. Leaves of Casimiroa sapota were investigated for components and antioxidant/anti-inflammatory activities against lead acetate ((AcO)2 Pb) induced hepatotoxicity in rats. Three groups of male albino rats were administrated orally with vehicle or C. sapota (100 and 200 mg/kg b.w/day) for 28 days; other group was injected with sub-acute dose (100 mg/kg b.w/day) of (AcO)2 Pb. Three protective groups were injected with (AcO)2 Pb (100 mg/kg b.w/day) for 7 days at day 22 after treatment with either C. sapota (100 or 200 mg/kg b.w/day) or silymarin (SILY) for 28 days. We isolated and identified, from C. sapota, a new compound for the 1st time in nature; 5,6,2',3'-tetramethoxyflavone in addition to the rare compound 5,6,3'-trimethoxyflavone (second report of isolation from nature) and the known compound 5,6,2',3',4'-pentamethoxyflavone. There is an improvement in all hemato-biochemical parameters, antioxidant defense system and anti-inflammatory cytokines of protective groups, which received C. sapota in dose dependent manner. The percentage of changes in all parameters measured in (AcO)2 Pb groups that received vehicle, CS100, CS200 or SILY were 109.2, 37.3, 12.5%, and 1.2% compared with the healthy control group. The C. sapota groups confer a better antioxidant activity by preventing oxidative stress and inflammation in (AcO)2 Pb treated rats. The compounds isolated are responsible at least in part for the observed protective effects.

The essential oils isolated from the leaves and green branches of the Egyptian navel orange trees were analyzed by GC and GC/MS. A total of 33 and 24 compounds were identified from the oils of the leaves and branches accounting for 96.0% and 97.9%, respectively, of the total detected constituents. The major ones were sabinene (36.5; 33.0%), terpinen-4-ol (8.2; 6.2%), δ-3-carene (7.0; 9.4%), limonene (6.8; 18.7%), trans-ocimene (6.7; 6.1%), and β-myrcene (4.5; 4.4%). The antimicrobial activities of both oils were evaluated using the agar-well diffusion method toward three representatives for each of Gram-positive bacteria, Gram-negative bacteria, and fungi. The oil of leaves was more effective as antimicrobial agent than that of the branches. Streptococcus pyogenes, Staphylococcus aureus, Salmonella typhimurium, and Aspergillus fumigatus were the most sensitive bacteria and fungi by the leaves oil.

The composition of the essential oil isolated from leaves and flowers of Pulicaria incisa sub. candolleana E.Gamal-Eldin was analysed by GC and GC-MS. Forty-nine and sixty-eight compounds were identified from the oils of the leaves and flowers accounting for 86.69% and 84.29%, respectively of the total detected constituents. Both leaves and flowers oils were characterized by the high content of each carvotanacetone with 66.01%, 50.87% and chrysanthenone 13.26%, 24.3% respectively. The cytotoxic activity of both essential oils was evaluated against hepatocellular carcinoma cell line HEPG-2, using MTT assay and vinblastine as a reference drug. Leaf oil showed higher activity with IC50 11.4 μg/mL compared with 37.4 μg/mL for flower oil. The antimicrobial activity of both oils was evaluated using agar well diffusion method towards two representatives for each of Gram positive and Gram negative bacteria as well as four representatives for fungi. The minimum inhibitory concentration of both essential oils against bacterial and fungal strains was obtained in the range of 0.49 – 15.63 μg/mL. This article is protected by copyright. All rights reserved.

Objectives The leaf decoctions of Tamarindus indica (TI) have long been traditionally used in liver ailments. The aim of this study was to investigate the anti-apoptotic activity of TI leaf extract against acute ethanol (EtOH)-induced liver injury. The major constituents of the extract were also examined for standardization purposes. Methods Rats (n = 5–7) were orally pretreated with TI leaf extract (25, 50 and 100 mg/kg) for seven days. Silymarin was used as a positive control. Liver tissue biochemical assays included key markers of apoptosis and its redox signalling. Serum enzyme levels were also determined. Key findings All graded doses of TI leaf extract mitigated the EtOH-induced liver caspase-3 activation (42, 57 and 64%) as well as DNA fragmentation (32, 47 and 50%), respectively. The highest dose of the extract demonstrated membrane-stabilizing (38%) in addition to glutathione-replenishing (88%) effects. Also, the leaves improved the liver histopathological alterations. Moreover, major plant bioactive polyphenolics, that might be responsible for the extract's observed effects, were isolated and identified. Conclusions TI leaf extract demonstrated promising anti-apoptotic hepatoprotective effects in rats. The use of TI leaves in different liver diseases, having apoptosis as the underlying pathology, hence warrants further clinical investigation.