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The chemical composition of the essential oils obtained from the aerial parts of four Apiaceae species, namely Elaeosticta allioides (EA), E. polycarpa (EP), Ferula clematidifolia (FC), and Hyalolaena intermedia (HI), were determined using gas chromatography. Altogether, 100 volatile metabolites representing 78.97, 81.03, 85.78, and 84.49% of the total components present in EA, EP, FC, and HI oils, respectively, were reported. allo-Ocimene (14.55%) was the major component in FC, followed by D-limonene (9.42%). However, in EA, germacrene D (16.09%) was present in a high amount, while heptanal (36.89%) was the predominant compound in HI. The gas chromatographic data were subjected to principal component analysis (PCA) to explore the correlations between these species. Fortunately, the PCA score plot could differentiate between the species and correlate Ferula to Elaeosticta species. Additionally, the antioxidant activity was evaluated in vitro using the 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), and the ferric reducing power (FRAP) assays. In addition, the antimicrobial activity using the agar diffusion method was assessed, and the minimum inhibitory concentrations (MICs) were determined. Furthermore, the cell viability MTT assay was performed to evaluate the cytotoxicity of the essential oils against hepatic (HepG-2) and cervical (HeLa) cancer cell lines. In the DPPH assay, FC exhibited the maximum activity against all the antioxidant assays with IC50 values of 19.8 and 23.0 μg/mL for the DPPH and ABTS assays, respectively. Ferula showed superior antimicrobial and cytotoxic activities as well. Finally, a partial least square regression model was constructed to predict the antioxidant capacity by utilizing the metabolite profiling data. The model showed excellent predictive ability by applying the ABTS assay.

A series of iridoid glycosides were isolated from the leaves of Lasianthus verticillatus (Lour.) Merr., belonging to family Rubiaceae. A new iridoid glycoside, lasianoside F (1), and three new bis-iridoid glycosides, lasianosides G&ndash, I (2&ndash, 4), together with four known compounds (5&ndash, 8) were isolated. The structures were established by spectroscopic methods, including 1D and 2D NMR experiments (1H, 13C, DEPT, COSY, HSQC, HMBC, and NOESY) in combination with HR-ESI-MS and CD spectra.

A new abietane diterpene namely plectrabarbene (2), together with two known compounds: sugiol (1) and 11,14-dihydroxy-8,11,13-abietatrien-7-one (3) have been isolated from the aerial parts of Plectranthus barbatus Andr. (Labiatae). The structures of these compounds were determined by various spectral techniques (e.g., UV, IR, NMR, and FAB) and by comparison with the literature data. A molecular docking study of the isolated diterpenes (1&ndash, 3) was performed with AChE to gain an insight into their AChE inhibition mechanism. The results of docking experiments revealed that the all tested compounds showed binding affinity at the active site of AchE in comparison to donepezil.

Labdane diterpenes are important substances due to their remarkable biological activities such as, antibacterial, antiprotozoal, antifungal and cytostatic and cytotoxic effects against human cancer cells. We have isolated a labdane diterpene named “leoheterin” from the aerial parts of the Otostegia fruticosa Forssk (Briq) obtained from south west Arabian mountains of Saudi Arabia. The isolated compound was characterized by 1HNMR, 13CNMR, IR and UV–visible spectroscopies. Due to the pharmaceutical importance of this class of compounds we have studied the interaction of HSA with leoheterin by using several spectroscopic methods. The change in the UV spectrum of HSA in presence of leoheterin gives a primary idea about the interaction between them. Congruently, leoheterin quenches the fluorescence of HSA with a prominent blue shift of 5 nm, reminiscent of involvement of hydrophobic interactions. There was 1:1 binding between leoheterin and albumin which was taken place via static quenching mechanism. From CD it was revealed that leoheterin induces the secondary structure of HSA which is further supported by 3-d fluorescence measurements which shows a decrease in the size of the HSA-leoheterin complex as compared to the HSA alone. Molecular docking simulations presented that among the first three conformers, which have been arranged according to the least binding energies and are also in good corroboration with the free energies of binding obtained experimentally, the first two conformers shown the binding in hemin binding site of subdomain IB while in third conformer the binding site was near to the drug binding site 1 located in subdomain IIA. All conformers exhibited the involvement of hydrogen bonding as well as hydrophobic interactions.

A new ursane-type triterpene ester, plectraterpene [3β-(decanoyloxy)-19-hydroxy-urs-12-ene] and four known steroidal compounds have been isolated from the aerial parts of Plectranthus montanus Benth. (syn. Plectranthus cylindraceus Hochst. ex Benth.), Lamiaceae. The known compounds were stigmasterol, sitosteryl ferulate, cholest-5-en-3-O-β-d-glucopyranoside and stigmasterol-3-O-β-d-glucopyranoside. Compounds plectraterpene, sitosteryl ferulate and stigmasterol-3-O-β-d-glucopyranoside are reported for the first time from this plant whereas compound cholest-5-en-3-O-β-d-glucopyranoside first time from the genus. The structures of these compounds were determined through spectral analysis, including extensive 2D NMR data as well as chemical methods and comparison with literature. Keywords: Plectranthus cylindraceus, Lamiaceae, Plectraterpene, Ursane-type triterpene

From the culture of the endophytic fungus Fusarium sp. isolated from the roots of Mentha longifolia L. (Labiatae) growing in Saudi Arabia, a new cyclodepsipeptide, namely fusaripeptide A (1), along with three known compounds adenosine (2), 2[(2-hydroxypropionyl)amino]benzamide (3), and cyclopentanol (4), have been isolated. Their structures were determined, using extensive 1D and 2D NMR and HRESI and GC mass spectral data. That is the first report for the isolation of compound 4 from natural source. In addition, compounds 2 and 3 are reported here for the first time from Fusarium sp. The absolute configuration of the amino acid residues of 1 was assigned by chiral GCMS and Marfey's analysis after acid hydrolysis. Fusaripeptide A differs from the reported ones from Fusarium sp. in the length of fatty acidic alkyl chain. Compound 1 was evaluated for its antifungal, anti-malarial, and cytotoxic activities. It exhibited potent antifungal activity toward C. albicans, C. glabrata, C. krusei, and A. fumigates with IC50 values of 0.11, 0.24, 0.19, and 0.14 μM, respectively. Furthermore, it had significant anti-malarial activity toward P. falciparum (D6 clone) with IC50 value of 0.34 μM. However, it showed cytotoxic activity toward the tested cell lines.

To overcome multi-drug resistance in microbes, highly efficient antimicrobial substances are required that have a controllable antibacterial effect and are biocompatible. In the present study, an efficient phototherapeutic antibacterial agent, human serum albumin (HSA)/reduced graphene oxide (rGO)/Cladophora glomerata bionanocomposite was synthesized by the incorporation of rGO nanoparticles with HSA, forming protein-rGO, and decorated with a natural freshwater seaweed Cladophora glomerata. The prepared HSA/rGO/Cladophora glomerata bionanocomposite was characterized by spectroscopic (UV-vis, FTIR, XRD and Raman) and microscopic (TEM and SEM) techniques. The as-synthesized bionanocomposite showed that sunlight/NIR irradiation stimulated ROS-generating dual-phototherapic effects against antibiotic-resistant bacteria. The bionanocomposite exerted strong antibacterial effects (above 96 %) against amoxicillin-resistant P. aeruginosa and S. aureus, in contrast to single-model-phototherapy. The bionanocomposite not only generated abundant ROS for killing bacteria, but also expressed a fluorescence image for bacterial tracking under sunlight/NIR irradiation. Additionally, the bionanocomposite displayed pronounced antioxidant activity.

Context: Premna resinosa (Hochst.) Schauer (Lamiaceae) is used in many places to treat bronchitis, respiratory illness and convulsions of the rib cage. Objective: This study evaluates the anticancer, antimicrobial and antioxidant activities of P. resinosa, and isolates some responsible constituents. Materials and methods: The methanol extract of P. resinosa aerial parts and its fractions (n-hexane, dichloromethane, ethyl acetate and n-butanol) were tested. Antimicrobial activity was tested using microdilution method against three Gram-positive and four Gram-negative bacteria. The tested concentrations ranged from 4000 to 7.8 μg/mL and MIC values were determined after 24 h incubation. Anticancer activity was evaluated against three human cancer cell lines (Daoy, HepG2 and SK-MEL28) using MTT assay. Antioxidant activity was investigated by DPPH scavenging method and β-carotene-linoleic acid assay. Results: The greatest antimicrobial activity was exhibited by n-hexane fraction (MIC 10 μg/mL) against Staphylococcus aureus, Enterococcus faecalis, and Shigella flexneri. The n-hexane fraction induced the greatest cytotoxic activity against Daoy, HepG2, and SK-MEL28 cell lines with IC50 values of 9.0, 8.5 and 13.2, respectively. Moreover, the dichloromethane and ethyl acetate fractions showed the highest antioxidant potential. A bioassay-guided fractionation led to the isolation and characterization of seven compounds for the first time, namely, quercetin (1), 3-methoxy quercetin (2), kaempferol (3), 3-methoxy kaempferol (4), myricetin 3,7,3′-trimethyl ether (5), lupeol (6), and stigmasterol (7). Conclusion: Our results indicate that P. resinosa is a source for antimicrobial and cytotoxic compounds. However, further work is required to isolate other active principles and to determine the mechanism of action.

The naphthalene glycosidecurviflorside [1,5-dihydroxy-8-methoxynaphthalene-2-O-β-D-xylopyranoside] (3) and the flavanol curviflorin [(+)-catechin-7-O-3″,4″-dihydroxybenzoate] (4), along with two known flavonoids: (+)-catechin (1) and quercetin (2) were isolated from the shoots of Plicosepalu scurviflorus Benth. (Loranthaceae) growing in Saudi Arabia and the chemical structures were elucidated by 2D-NMR spectroscopy.

Herein, we have reported the study of interaction of model protein, bovine serum albumin (BSA), and a sipholane triterpenoid, named Sipholenone A. This triterpenoid in known to possess anticancer properties and was isolated from the Red Sea sponge Siphonochalina siphonellais. 1H and 13C NMR were used to characterize the triterpenoid. Binding studies were carried out by using UV–visible and fluorescence spectroscopies and the conformational transition was seen by means of circular dichroism and FTIR spectroscopies. The hypochromic shift in UV spectrum of BSA in presence of Sipholenone A is an indication of the complex formation. The results also indicated that the fluorescence quenching of BSA at 340 nm by Sipholenone A caused due to the formation of Sipholenone A-BSA complex. The number of binding sites for Sipholenone A binding on BSA was found to be roughly equal to 1. Stern-Volmer analysis at various temperatures showed the involvement of the static quenching in the binding process. Sipholenone A binds to the site I of subdomain IIA and also causes changes in the secondary and tertiary structure of BSA and a consequent partial unfolding.

A sipholane triterpenoid, named sipholenone A, with anti-cancer properties was isolated from the Red Sea sponge Siphonochalina siphonella and characterized by proton and carbon-13 nuclear magnetic resonance (1 H NMR and 13 C NMR) spectroscopies. The goal of this study was to visualize the binding of this triterpenoid with human serum albumin (HSA) and to determine its binding site on the biomacromolecule. The interaction was visualized using fluorescence quenching, synchronous fluorescence, far- and near-UV circular dichroism (CD), UV-visible and Fourier transform-infrared (FT-IR) spectroscopies. UV-visible spectroscopy indicated the formation of a ground-state complex as a result of the interaction. Sipholenone A quenches the fluorescence of HSA via a static quenching mechanism. A small blue shift in the fluorescence quenching profiles suggested the involvement of hydrophobic forces in the interaction. Sipholenone A binding takes place at site I of subdomain II A with a 1:1 binding ratio, as revealed by displacement binding studies using warfarin, ibuprofen and digitoxin. Far-UV CD and FT-IR studies showed that the binding of sipholenone A to HSA also had a small effect on the protein's secondary structure with a slight decrease in the α-helical content. Several thermodynamic parameters were calculated, along with Forster's radiative energy transfer analysis.

The compositions of volatile components in the aerial parts of six Astragalus species, namely A. campylotrichus (Aca), A. chiwensis (Ach), A. lehmannianus (Ale), A. macronyx (Ama), A. mucidus (Amu) and A. sieversianus (Asi), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of Aca, Ach, Ale, Ama, Amu and Asi whole oils, respectively. Sylvestrene was the most predominant component in Asi, Amu and Ama, with highest concentration in Asi (64.64%). In addition, (E)-2-hexenal was present in a high percentage in both Ale and Ach (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all Astragalus species and a high correlation between the Amu and Ama species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), &alpha, amylase, &alpha, glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, Ama exhibited the maximum activity (24.12 &plusmn, 2.24 mg TE/g sample), and the volatiles from Amu exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both Ale and Ama showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). Asi demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for Ale (138.42 mg KAE/g). Accordingly, Astragalus species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer&rsquo, s disease, diabetes mellitus and oxidative stress-related diseases.

Distinct morphological MgO nanoparticles (MgONPs) were synthesized using biomasses of Saussurea costus roots. The biomass of two varieties of Saussurea costus (Qustal hindi and Qustal bahri) were used in the green synthesis of MgONPs. The physical and chemical features of nanoparticles were confirmed by spectroscopic and microscopic techniques. The surface morphology of the obtained nanoparticles was detected at different magnifications by SEM and TEM microscopy and the size of nanoparticles were found to be 30 and 34 nm for Qustal hindi and Qustal bahri, respectively. The antimicrobial activity of the prepared MgONPs was screened against six pathogenic strains. The synthesized nanoparticles by Qustal bahri biomass exerted significant inhibition zones 15, 16, 18, 17, 14, and 10 mm against E. coli, P. aeruginosa, C. tropicalis and C. glabrata, S. aureus and B. subtilis as compared to those from Qustal hindi 12, 8 and 17 mm against B. subtilis, E. coli and C. tropicalis, respectively. MgONPs showed a potential cytotoxicity effect against MCF-7 breast cancer cell lines. Cellular investigations of MgONPs revealed that the prepared nanoparticles by Qustal bahri exhibited high cytotoxicity against MCF-7 cancer cell lines. IC50 values in MCF-7 cells were found to be 67.3% and 52.1% for MgONPs of Saussurea costus biomasses, respectively. Also, the photocatalytic activity of MgONPs of each Saussurea costus variety was comparatively studied. They exhibited an enhanced photocatalytic degradation of methylene blue after UV irradiation for 1 h as 92% and 59% for those prepared by Qustal bahri and Qustal hindi, respectively. Outcome of results revealed that the biosynthesized MgONPs showed promising biomedical potentials.

The present study focused on the prospect of fabricating a polymeric naturally extracted Moringa oleifera oil bionanocomposite film enriched with silver nanoparticles for antimicrobial activity. In this study, a standard concentration of Moringa oleifera oil (5-10 wt%) was used to fabricate a polymeric bionanocomposite film using polyvinyl chloride (PVC) enriched with silver nanoparticles. The active constituents of the extracted Moringa oleifera oil were verified using gas chromatography-mass spectrometry. Spectroscopic and microscopic techniques, including scanning electron microscopy, X-ray diffraction, and energy-dispersive X-ray analysis, were employed to characterize and study the surface morphology of the fabricated bionanocomposite film. The antimicrobial activity of the fabricated bionanocomposite film was investigated using different strains of bacteria and fungus. The results revealed well-oriented and excellently dispersed silver nanoparticles in the PVC-Moringa oleifera oil matrix. The bionanocomposite was able to inhibit the growth of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Salmonella typhi, Pseudomonas aeruginosa, Shigella flexneri, and Candida albicans. The combination of nanoparticles with polymers is opening new routes for engineering fixable composites, which showed antimicrobial properties.

The objective of this study was to develop a validated high-performance thin layer chromatography (HPTLC) method for the concurrent analysis of two diterpenes Sugiol (compound 1) and 11,14-dihydroxy-8,11,13-abietatrien-7-one (compound 2) in Plectranthus barbatus chloroform extract (PBCE) and to investigate cytotoxicity of both compounds. The chromatographic estimations were carried out using toluene : ethyl acetate : formic acid (8.2:1.3:0.5 v/v/v) as mobile phase. The compact spots of biomarkers were scanned at λ max = 275 nm. Cytotoxic evaluation of both compounds was performed using follicular thyroid cancer cells (FRO cells). A well resolved, compact and intense peaks of compound 1 ( R f = 0.550 ± 0.001) and compound 2 ( R f = 0.700 ± 0.002) were recorded. The proposed method for both compounds was recorded as simple, linear, precise (% RSD = 1.02-1.25), accurate (98-100%), robust and sensitive for the analysis of both compounds. Cytotoxicity evaluation showed significant cell cytotoxicity at 100 μg/mL concentration against the FRO cancer cells after 72 h of incubation. Both compounds were recorded as cytotoxic, however compound 1 showed significant cytotoxic effects. The proposed HPTLC method was found to be suitable for routine analysis of these two biomarkers in chloroform extract of P. barbatus . Both compounds were found to be cytotoxic against FRO cancer cells. KEY WORDS : Diterpenes, Sugiol, Plectranthus barbatus , Cytotoxicity, HPTLC Bull. Chem. Soc. Ethiop. 2018 , 32(3), 407-419. DOI: https://dx.doi.org/10.4314/bcse.v32i3.1

Phytochemical investigation of Polyscias guilfoylei leaves extract (PGE) led to the isolation of nine compounds, that is, ent-labda-8(17),13-diene-15,18-diol (1), stigmasterol (2), spinasterol (3), N-(1,3-dihydroxyoctadecan-2-yl) palmitamide (4), panaxydiol (5), 3-O-β-d-glucopyranosylstigmasta-5,22-diene-3-β-ol (6), (8Z)-2-(2 hydroxypentacosanoylamino) octadeca-8-ene-1,3,4-triol (7), 4-hydroxybenzoic acid (8), and tamarixetin 3,7-di-O-α-L-rhamnopyranoside (9). Compound 4 is reported in this study for the first time in nature whereas compound 9 is reported for the second time. Structural elucidation of the compounds was carried out using Nuclear Magnetic Resonance and Electrospray Ionization coupled with Mass Spectrometry spectroscopic analyses. PGE and compounds 4 and 9 exhibited weak cytotoxicity against both MCF-7 and HCT-116 cell lines using 3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide assay. The antimicrobial activity of PGE and compounds 4 and 9 was evaluated using the agar diffusion method. Escherichia coli was the most susceptible Gram-negative bacteria toward PGE with a minimum inhibitory concentration value of 9.76 μg/mL, whereas compounds 4 and 9 did not show any antimicrobial activity. Compound 4 exhibited promising inhibition of histamine release using U937 human monocytes with an IC50 value of 38.65 μg/mL.

Periplocain A (2), a new naphthalene derivative together with four known compounds: 2-ethylhexyl benzoate (1), quercetin-3-O-α-l-rhamnopyranoside (3), quercetin-3-O-β-d-glucopyranoside (4), and quercetin-3-(6-O-α-l-rhamnopyranosyl-β-d-glucopyranoside) (5) were isolated from the AcOEt fraction of the aerial parts of Periploca aphylla (Asclepiadaceae). Their structures were established by multiple spectroscopic methods in addition to HR-ESI-MS and by comparison with literature data.

The present study focused on the phytochemical chromatographic isolation of two chemical constituents, sterol and flavonoid (stigmasterol glucoside and luteolin) from Plectranthus asirensis. A novel, eco-friendly, and cost benefit, ultrasensitive sequential injection analysis chemiluminescence (SIA-CL) approach based on the enhanced catalytic activity of silver nanoparticles (AgNPs) was suggested to evaluate the isolated compounds. Silver nanoparticles were synthesized using the biomass of an ethanolic extract of aerial parts of P. asirensis as a reducing agent. Spectroscopic and microscopic characterization of the prepared AgNPs were performed, including UV-Vis spectrometry, XRD and FT-IR as well as TEM and SEM. UV-spectroscopic method detected the formed AgNPs at an absorbance wavelength of 420 nm. Furthermore, antioxidant activity of the isolated compounds was also determined using 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity protocol.

We report isolation of a new sesquiterpene (compound 2: plectranol A) along with three known compounds (1: maaliol, 3: penduletin and 4: chrysosplenol D) from the aerial parts of Plectranthus cylindraceus Hoechst. Ex. Benth ethyl acetate extract (PCEAE). Their structures were established by UV, IR, NMR (1H & 13C), HRESIMS and HSQC methods. The MTT cell proliferation assay of the compounds and the extract performed on human breast, skin and cervical cancer cell lines showed high toxicity, and their IC50 (μg/mL) values were determined. The validated HPTLC analyses of maaliol and PCEAE (method I) and, penduletin, chrysosplenol D and PCEAE (method II) furnished sharp and compact peaks. The estimated high contents (μg/mg) of maaliol (17.06), penduletin (39.36) and chrysosplenol D (31.66) in PCEAE approved the plant’s cytotoxic property. Since, P. cylindraceus contains a variety of cytotoxic terpenoids and flavonoids; our data warrant its further phytochemical and biological characterisation towards developing promising anti-cancer drugs.

Pristine β-sitosterol or in combination with other phytosterols is utilized in an array of enriched commercial foods. Considering the presence of β-sitosterol in different functional foods and its potential role in prevention and cure of neurodegenerative diseases, the aims of our investigation were to encapsulate β-sitosterol in nanofibers and to estimate influence of β-sitosterol on proliferation of fibroblasts. Electrospun nanofibers have widely been used as scaffolds to mimic natural extracellular matrix. Herein, our group for the first time establishes an innovative scaffold based on β-sitosterol and polyurethane using electrospinning. β-Sitosterol promotes epithelialization and possesses anti-oxidant and anti-inflammatory activities, whereas polyurethane, besides possessing biomedical uses, also enhances epithelial growth. We optimized the concentration (5%) of β-sitosterol in polyurethane to obtain homogenous solution, which can be spun without difficulty for the synthesis of β-sitosterol amalgamated scaffold. The resulted twisted nanofibers have been characterized via scanning electron microscopy and Fourier transform infrared spectroscopy. The viability of cells on twisted scaffold was examined using NIH 3T3 fibroblasts as model cell line. Incorporation of β-sitosterol in polyurethane changed the structure and size of nanofibers, and the twisted scaffolds were non-cytotoxic. Thus, the twisted nanoribbons, which contain anti-inflammatory β-sitosterol, can be utilized as a promising future material, which will help to ease inflammation and also aid in wound healing. In conclusion, the outcome of the preliminary research evidently points out the potential of twisted scaffold in biomedical applications.

Background: Genus Ficus (Moraceae) constitutes more than 850 species and about 2000 varieties and it acts as a golden mine that could afford effective and safe remedies combating many health disorders. Objectives: Discrimination of Ficus cordata, Ficus ingens, and Ficus palmata using chemometric analysis and assessment of their role in combating oxidative stress. Materials and Methods: Phytochemical profiling of the methanol extracts of the three Ficus species and their successive fractions was performed using high-performance liquid chromatography/electrospray ionization mass spectrometry. Their discrimination was carried out using the obtained spectral data applying chemometric unsupervised pattern-recognition techniques, namely, principal component analysis and hierarchical cluster analysis. In vitro hepatoprotective and antioxidant evaluation of the samples was performed using human hepatocellular carcinoma cells challenged by carbon tetrachloride (CCl4). Results: Altogether, 22 compounds belonging to polyphenolics, flavonoids, and furanocoumarins were identified in the three Ficus species. Aviprin is the most abundant compound in F. cordata while chlorogenic acid and psoralen were present in high percentages in F. ingens and F. palmata, respectively. Chemometric analyses showed that F. palmata and F. cordata are more closely related chemically to each other rather than F. ingens. The ethyl acetate fractions of all the examined species showed a marked hepatoprotective efficacy accounting for 54.78%, 55.46%, and 56.42% reduction in serum level of alanine transaminase and 56.82%, 54.16%, and 57.06% suppression in serum level of aspartate transaminase, respectively, at 100 μ g/mL comparable to CCl4-treated cells. Conclusion: Ficus species exhibited a notable antioxidant and hepatoprotective activity owing to their richness in polyphenolics and furanocoumarins. Abbreviations used: ALT: Alanine transaminase, AST: Aspartate transaminase, CCl4:Carbon tetrachloride, DMEM: Dulbecco's Modified Eagle's medium, DMSO: Dimethyl sulfoxide, EDTA: Ethylenediaminetetraacetic acid, FBS: Fetal bovine serum, FCA: Ficus cordata remaining aqueous fraction, FCB: Ficus cordata n-butanol fraction, FCE: Ficus cordata ethyl acetate fraction, FCP: Ficus cordata petroleum ether fraction, FCT: Ficus cordata total methanol extract, FIA: Ficus ingens remaining aqueous fraction, FIB: Ficus ingens n-butanol fraction, FIE: Ficus ingens ethyl acetate fraction, FIP: Ficus ingens petroleum ether fraction, FIT: Ficus ingens total methanol extract, FPA: Ficus palmata remaining aqueous fraction, FPB: Ficus palmata n-butanol fraction, FPE: Ficus palmata ethyl acetate fraction, FPP: Ficus palmata petroleum ether fraction, FPT: Ficus palmata total methanol extract, GSH: Reduced glutathione,HepG2 cells: Human hepatocellular carcinoma, HPLC-ESI-MS: High-performance liquid chromatography/electrospray ionization mass spectrometry, and SOD: Superoxide dismutase.