KB Cancer Cell Lines Research Articles

Chemical Composition, Anti-microbial, and Cytotoxic Activities of Essential Oil from Magnolia bidoupensis Q. N. Vu leaves, an Endemic Species to the Central Highlands of Vietnam.

An analysis was conducted on the essential oil extracted from the leaves of Magnolia bidoupensis utilizing GC-MS, revealing thirty-three constituents that account for 98.9% of the essential oil. The main components included pogostol (22.4%), δ-selinene (16.2%), and α-amorphene (14.7%). Bioassays were then performed to evaluate the oil's biological activity. The essential oil exhibited antimicrobial activity against all tested microorganisms (six bacterial strains and one fungal strain) using the minimum inhibitory concentration (MIC) method. Additional cytotoxicity tests were conducted on KB, HepG2, MCF-7, and A549 cancer cell lines using the MTT method. The essential oil exhibited strong cytotoxic effects on all four cell lines, with IC50 values ranging from 1.37 ± 0.05 μg/mL (KB) to 2.40 ± 0.06 μg/mL (A549).

Chemical Composition, Anti-Microbial, and Cytotoxic Activities of Essential Oils from Blumea densiflora var. hookeri (C.B. Clarke ex Hook.f.) C.C. Chang & Y.Q. Tseng Leaves from Vietnam.

The essential oil from the leaves of Blumea densiflora var. hookeri was analyzed using GC-MS, and bioassays were performed. GC-MS identified thirty-four constituents, representing 79.1 % of the oil composition. The major compounds identified in the oil were (E)-caryophyllene (15.3 %), viridiflorol (5.5 %), trans-dauca-4(11),7-diene (4.6 %), spathulenol (4.4 %), and isolongifolan-7-α-ol (4.3 %). The antimicrobial activity of the oil was assessed to determine its efficacy against six bacterial strains and one fungal strain using minimum inhibitory concentration (MIC) methods. The essential oil demonstrated antimicrobial activity against all tested microorganisms. A cytotoxicity assay was performed on KB and A549 cancer cell lines using the MTT method. The essential oil displayed strong cytotoxic effects on both cell lines, with IC50 values of 1.40±0.05 μg/mL for KB and 1.72±0.04 μg/mL for A549.

Improving chemoradiotherapy strategy with PEGylated doxorubicin loaded gold nanoparticles against oral cancers

Chemoradiotherapy, a combination treatment paradigm in oncology, where chemotherapy and radiation therapy are administered concurrently. Nanomedicine based Drug delivery at tumour site and radiosensitizer can minimize the adverse effects of chemoradiation. In this study, one pot and facile method was used to synthesize two nanotherapeutics Doxorubicin reduced gold nanoparticles (Au Dox NPs) and Doxorubicin complexed in PEGylated gold nanoparticles (Au Dox PEG NPs). Both were physico-chemically characterized by spectroscopy methods to confirm formation of gold nanoparticles and conjugation of Dox. Advanced electron microscopy was used to analyze morphology and nano architect of the nanotherapeutics. Drug release kinetics was analyzed by dialysis method. KB cells were X-ray irradiated by LINAC facility at 4 Gy dose. Cytotoxicity, radiation and chemoradiation damage was measured by MTT assay. Stability assay to measure the agglomeration and stability in biological medium. The resultant two nanotherapeutics synthesized, Au Dox NPs and Au Dox PEG NPs are stable nanoformulations successfully loaded with Dox. Both had average size of ∼20 nm and negative surface charge and near spherical morphology. Conjugated Dox molecule is conserved. KB cancer cell line in vitro cellular studies revealed that the Au Dox NPs had enhanced drug uptake and superior cytotoxicity and radiosensitization in comparison to Au Dox PEG NPs and free Dox, thereby providing a synergistic approach for treatment of oral cancer. In the current study promising results obtained at preclinical in vitro model, the potential of Au Dox PEG NPs for drug delivery system can be enhanced by tagging with antibodies/small molecules for targeted treatment of oral cancers, also further investigation in vivo model warranted.

New nor-lignans from the leaves of styrax annamensis guillaumin

Phytochemical study of the leaves of Styrax annamensis Guillaumin resulted in the isolation of a new natural product egonol-3’’-sulphate (1), and two new derivatives egonol-3-methyl-D-galactopyranoside (2) and 7-methoxy-2-(3’,4’-methylenedioxyphenyl)-benzofuran-5-carboxamide (3). Their chemical structures were ­elucidated by spectroscopic data. Compounds 1 and 3 significantly established a great role for the chemotaxonomic aspect. Compound 1 showed cytotoxicity against four cancer cell lines KB, HepG2, Lu, and MCF7 with the IC50 values of 84.90–101.69 µg/mL, and exhibited acetylcholinesterase (AChE) inhibitory activity with the IC50 value of 97.08 µg/mL.

Anti-oral cancer properties of potential probiotic lactobacilli isolated from traditional milk, cheese, and yogurt

This study investigates the probiotic and anti-cancer effects of 21 isolated Lactobacillus strains from cheese, milk, and yogurt in Kermanshah, Iran, on oral cancer cell lines KB and OSCC. Four selected isolates (Y33, M45, C5, and C28) displayed good viability and resistance to specific antibiotics. Notably, strains C28 and Y33 exhibited the best results, showing susceptibility or semi-susceptibility to five antibiotics. Y33, with high cell surface hydrophobicity (62%), demonstrated significant anti-pathogenic activity, inhibiting the growth of tested pathogens and displaying strong adhesion to human intestinal Caco-2 cells (52%). Further assessments, including acridine orange/ethidium bromide staining and mRNA expression analysis, revealed four isolates (C5, C28, M45, and Y33) with promising probiotic properties. Particularly, Y33’s protein-based extract metabolites showed dose- and time-dependent inhibition of KB and OSCC cancer cell lines, inducing apoptosis without significant cytotoxic effects on normal cells. Y33 (Lactiplantibacillus plantarum) exhibited the strongest probiotic potential, surpassing conventional anti-cancer drugs, suggesting its therapeutic potential for preventing oral cancer cell proliferation and improving survival rates in oral cancer patients.

A new cucurbitane − type triterpenoid from the bark of Elaeocarpus hygrophilus Kurz.

A new cucurbitacin, 3β-(β-D-glucopyranosyloxy)-5β,6β:16α,23α-diepoxycucurbit-24-en-11-one or hygrocucurbin A (1), along with two known compounds, including 3β-(β-D-glucopyranosyloxy)-16α,23α-epoxycucurbita-5,24-dien-11-one (2) and (+)-lyoniresinol (3), were isolated from the bark of Elaeocarpus hygrophilus. Their chemical structures were elucidated by spectroscopic NMR, HR-IDA- TOF-MS analysis, and by comparison with the spectral data of corresponding compounds in the literature. Two cucurbitacins (1) and (2) were evaluated for their α-glucosidase inhibitory activity and cytotoxic against KB, MCF-7, Hep G2, and A549 cancer cell lines. For the α-glucosidase inhibitory activity, compound 1 showed an equivalent effect (IC50 197.4 ± 4.1 µM) compared to the acarbose, a positive control (IC50 208.5 ± 4.7 µM). And for the cytotoxicity, 2 was inactive while 1 was slightly sensitive against KB cells (IC50 233.3 ± 2.5 µM).

Biosynthesis of Gold Nanoparticles Using Aqueous Extract of Paramignya trimera Roots and Its Anticancer Activity

Developing environment-friendly processes for metal nanoparticle synthesis without using toxic chemical is very necessary to meet the demand for biological and medical applications. In this work, biosynthesis of gold nanoparticles (AuNPs) using aqueous extract of Paramignya trimera roots as the reducing and stability agents was carried out. The formation of gold nanoparticles was confirmed by the presence of an absorption peak at 550 nm using UV–Visible spectrophotometry. The size and morphology of gold nanoparticles was monitored by Field emission scanning electron microscopy (FE-SEM) and High resolution transmission electron microscopy (HR-TEM). Analysis of these particles showed the synthesized AuNPs were spherical in shape, with the particle size range of 10 nm–15 nm. The element gold and the crystalline nature of AuNPs were finalized using Energy dispersive X-ray (EDX) and X-ray diffraction (XRD) spectrometer, respectively. Fourier transform infrared (FTIR) spectroscopy revealed possible involvement of reductive groups on the surfaces of nanoparticles. The synthesized AuNPs are evaluated for its activity against MCF-7, HepG2, KB, LU-1 and MKN7 cancer cell lines with inhibition concentration 50% (IC50) of 2.01, 7.60, 3.89, 3.99 and 3.53 ppm respectively after 72 hours of treatment.

Five undescribed aryltetralin lignans with cytotoxic activities from the fruits of Cleistanthus eberhardtii

Five undescribed lignans, cleiseberharnins A–D (1–4), cleiseberharside A (5) were isolated from the fruits of Cleistanthus eberhartii (Phyllanthaceae), together with six known aryltetralin lignans, cleistantoxin (6), picroburseranin (7), neocleistantoxin (8), 7-hydroxypicropolygamain (9), cleisindoside D (10), and cleisindoside A (11). Their structures and relative configurations were established by analysis of HRESIMS and NMR data, and quantum chemical calculations of JH,H coupling constants. The absolute configurations of 1–5 were determined by analysis of their experimental CD spectra and comparison with calculated electronic circular dichroism (ECD) spectra. All compounds (1−11) were evaluated for their cytotoxicity against KB, MCF-7, HepG-2, and Lu-1 human cancer cell lines. Among the tested compounds, compounds 6 and 7 showed strong activity against KB, MCF7, HepG2 and Lu-1 cell lines with IC50 values in the range of 0.02–0.62 μM. Compound 1 showed activity against three cancer cell lines KB, HepG2, and Lu-1 with IC50 values of 6.98, 7.61 and 11.75 μM, respectively. Compound 2 exhibited a selective inhibition with moderate cytotoxicity against Lu-1 with IC50 value of 15.30 μM. Compounds 4, 5 and 9 showed moderate activity against the three cancer cell lines with IC50 values in the range of 8.73–19.70 μM.

Acylation of Oleanolic Acid Oximes Effectively Improves Cytotoxic Activity in In Vitro Studies.

(1) Background: The aim of the presented work was to obtain a set of oleanolic acid derivatives with a high level of anticancer activity and a low level of toxicity by applying an economic method. Three types of oleanolic acid derivatives were obtained: (i) derivatives of methyl oleanonate oxime, (ii) derivatives of methyl oleanonate oxime with an additional 11-oxo function, and (iii) derivatives of morpholide of oleanonic acid oxime. (2) Methods: The above oximes were acylated with aliphatic or aromatic carboxylic acid. The newly obtained compounds were subjected to ADMETox analysis and were also tested for cytotoxicity activity on the HeLa, KB, MCF-7, A-549, and HDF cell lines with the MTT assay. (3) Results: Among the tested acylated oximes of oleanolic acid, some derivatives, particularly those with two nitro groups attached to the aromatic ring, proved to be the most potent cytotoxic agents. These triterpene derivatives significantly inhibited the growth of the HeLa, KB, MCF-7, and A-549 cancer cell lines in micromolar concentrations. (4) Conclusions: The introduction of different moieties, particularly the 3,5-dinitro group, resulted in the synthesis of highly potent cytotoxic agents with favorable SI and ADMETox parameters.

Screening for Antimycobacterial Activity of Actinomycetes Collected in Vietnam – Isolation and Activity of Metabolites from Streptomyces alboniger (A121)

Objective Actinomycetes have been known to be the great natural sources to explore antibiotics for the treatment of tuberculosis (TB). The isolation of actinomycetes from the samples in Vietnam followed by the screening of their antimycobacterial activity was performed in this study. The metabolites isolated from the most active strain were further evaluated for their antimycobacterial, antimicrobial and cytotoxic activity. Methods Actinomycetes were growth in culture media, isolated and identified by colony, spore chain morphology and 16S rRNA gene sequencing. Agar diffusion assay was used for the screening of the isolated strains against Mycobacterium smegmatis, a safety surrogate for Mycobacterium tuberculosis. The metabolites produced from the most active strain were investigated by actinomycete fermentation, extraction and isolation from biomass and cultures. The structures of the isolated compound were elucidated by spectral data and comparison with the reported literatures. Results 181 strains were isolated from nine regions along the north to central Vietnam. The five most active strains against Mycobacterium smegmatis were detected. Following the bioassay-guided result, the strain A121 ( Streptomyces alboniger) was selected for further isolation of the bioactive metabolites. As a result, obscurolide B2β (1) and chartreusin (2) were obtained and evaluated for their antimycobacterial activity against M. smegmatis. Compound 2 displayed potential antimycobacterial activity, antimicrobial effect against the Gram positive bacteria Staphylococcus aureus, Bacillus subtilis, Lactobacillus fermentum and cytotoxicity against four cancer cell lines KB, HepG-2, Lu-1 and MCF-7. Conclusions Five strains possessing potential antimycobacterial activity were identified from the samples collected in Vietnam. Two compounds including obscurolide B2β (1) and chartreusin (2) were isolated from the most active strain A121 ( Streptomyces alboniger). This is the first time these compounds have been isolated from this strain. Chartreusin (2) exhibited notable antimycobacterial, antimicrobial and cytotoxic activity, making its worthy attention for further drug development, particularly for antituberculosis therapeutic agents.

Chemical Constituents, Cytotoxicity, and Molecular Docking Studies of Tetragonula iridipennis Propolis

Objective: Propolis of Tetragonula iridipennis, which is one of the most popular stingless bees found in Vietnam, has been used to promote health and prevent disease. This study aims to identify the chemical constituents of T iridipennis propolis and their cytotoxic activity. Methods: The propolis sample was extracted with ethanol. The crude extract was isolated by combined chromatographic methods. The structures of isolated compounds were determined by electrospray ionization mass spectrometry and nuclear magnetic resonance spectra. The cytotoxicity was evaluated by 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide method. The protein interactions of active compounds were explored by molecular docking study. Results: Sixteen known compounds, including 11 triterpenes, 3 xanthones, a sterol, and a flavonoid were isolated and identified. The propolis ethanol extract displayed good cytotoxicity against A-549 and KB cancer cell lines. 24 S,25-Dihydroxytirucall-7-en-3-one was the most active compound with IC50 values ranging from 18.75 ± 0.21 to 19.62 ± 0.36 µg/mL. Conclusions: Sixteen known constituents were identified from T. iridipennis propolis, of which 8 compounds were discovered for the first time. The propolis of T iridipennis has multiple sources of plant resin, among that Ailanthus triphysa (Simaroubaceae) was identified as a new plant source. A molecular docking study revealed that cytotoxic effects of 24 S,25-dihydroxytirucall-7-en-3-one, α-mangostin, 6-methoxy–bispyrano xanthone, and 3-isomangostin related to the inhibition of all 3 targets epidermal growth factor receptor, human epidermal growth factor receptor 2, and mammalian target of rapamycin (mTOR), while other isolated triterpenes exert their cytotoxicity by the inhibition of mTOR protein activity.

Essential Oils of Alpinia vietnamica Rhizomes and Leaves: Chemical Composition, Cytotoxicity, α-Glucosidase Inhibition, and Molecular Docking Approach

Objective: Alpinia is a big genus of flowering plants in the family Zingiberaceae. The plants of this genus are generally aromatic due to their essential oils. The current study aims to identify chemical compositions in the rhizome and leaf oils of Alpinia vietnamica H.Đ. Trần, Luu & Škorničk. Methods: Essential oils of A vietnamica rhizomes and leaves obtained by hydrodistillation were investigated by the gas chromatography–flame ionization detection/mass spectrometry (GC–FID/MS) analysis. A vietnamica essential oils have been subjected to cytotoxic and α-glucosidase inhibitory assays. The protein interactions of the major compounds were viewed by molecular docking study. Results: In general, monoterpene hydrocarbons (60.4%-62.5%) and their oxygenated derivatives (18.1%-29.0%) were the main chemical classes of the rhizome and leaf oils. In the meantime, 1,8-cineole (25.7%-29.0%), β-pinene (12.8%-21.3%), geraniol (9.0%-15.2%), and α-pinene (6.1%-7.5%) can be seen as the main compounds. A vietnamica essential oils showed cytotoxicity toward four cancer cell lines KB, Hep-G2, Lu-1, and MCF-7 with IC50 values of 82.39 to 254.1 µg/mL. Significantly, the leaf oil (IC50 115.18 µg/mL) was better than the standard compound acarbose (IC50 156.68 µg/mL) in the α-glucosidase inhibitory assay. The results of molecular docking simulation suggested that 1,8-cineole, geraniol, α-pinene, and β-pinene could generate a similar inhibition (binding affinities) with acarbose, and the hydrogen and hydrophobic interactions played contributory roles in the binding to α-glucosidase enzyme. Conclusion: Further phytochemical investigations on this species, especially chromatographic separations to isolate bioactive metabolites, are needed. As well, pharmacological experiments are welcome since the current study is the first result.

Cytotoxic and Antimicrobial Secondary Metabolites from Penicillium hetheringtonii IMBC-NMTP04

Chemical investigation of the sesame-associated fungal strain Penicillium hetheringtonii IMBC-NMTP04 resulted in isolation of five compounds, penicitrinone A (1), dihydrocitrinin (2), janthinone (3), coniochaetone B (4), and 9-oxo-10(E),12(E)-octadecadienoic acid (5). Their chemical structures were elucidated by spectroscopic methods, including 1D and 2D NMR and mass spectra in comparison with the literature data. Compound 1 showed modest cytotoxicity toward LNCaP, HepG2, MCF-7, KB, SK-Mel-2, and HL-60 human cancer cell lines, with IC50 values ranging from 60.1 to 84.2 mM while 5 was cytotoxic toward only HL-60 cell line (IC50 = 71.6 mM). All the compounds significantly inhibited E. faecalis, S. enterica, and C. albicans growth, with MIC values ranging from 12.5 to 50.0 mM. Compounds 2, 4, and 5 suppressed the growth of B. cereus, while both 1 and 2 showed antimicrobial effect against E. coli, with the same MIC value of 200 mM. This is the first time to report the chemical constituents of Penicillium hetheringtonii and the antimicrobial effect of 2–4.

Cytotoxic effect of potential probiotic Lactiplantibacillus plantarum KUMS-Y8 isolated from traditional dairy samples on the KB and OSCC human cancer cell lines

Oral cancer is one of the leading causes of death worldwide, and its prevalence is especially high in developing countries. As an oral cancer treatment, traditional therapies are commonly used. Nonetheless, these treatments frequently result in a variety of side effects. As a consequence, there is an urgent need to enhance oral cancer therapies. Probiotics have recently demonstrated intriguing properties as therapeutic options for cancer treatment. Thus, the purpose of this study was to investigate the anticancer effect of probiotic Lactobacillus strains on the mouth epidermal carcinoma cells (KB) and oral squamous cell carcinoma (OSCC) cell lines. In this study, we looked at 21 Lactobacillus strains isolated from traditional dairy products in the Kermanshah province of western Iran to see if they had any inhibitory effects on oral cancer cell lines in vitro. We isolated and characterized Lactobacillus strains before assessing and comparing their probiotic potential and safety. Using the MTT assay, the bacterial extract was then prepared and used as an anti-proliferative agent on oral cancer (KB and OSCC) and normal (fibroblast and human umbilical vein endothelial cells (HUVEK) cell lines. Finally, acridine orange/ethidium bromide staining was used to determine whether cell death was caused by apoptosis. Four Lactobacillus isolates (C14, M22, M42, and Y8) were shown to have beneficial probiotic qualities. Lactobacillus extracts (of a protein nature) decreased the survival and proliferation of the KB and OSCC cancer cell lines (dose- and time-dependent) by inducing apoptosis, with no basic damaging effects on normal cells. The staining with acridine orange/ethidium bromide revealed that the cell death was caused by apoptosis. Furthermore, of the four Lactobacillus strains examined, isolate Y8 (Lactiplantibacillus plantarum) showed the strongest probiotic potential for suppressing KB and OSCC cell proliferation when compared to anticancer medicines (doxorubicin and paclitaxel). The current research found that Lactobacillus extract might reduce the growth and viability of the KB and OSCC cancer cell lines by inducing apoptosis, increasing the survival rate of oral cancer patients.

Antimicrobial, Cytotoxic, and α-Glucosidase Inhibitory Activities of Ethanol Extract and Chemical Constituents Isolated from Homotrigona apicalis Propolis-In Vitro and Molecular Docking Studies.

The chemical investigation of Homotrigona apicalis propolis collected in Binh Dinh province, Vietnam, led to the isolation of nine compounds, including four sesquiterpenes: spathulenol (1), 1αH,5βH-aromandendrane-4β,10α-diol (2), 1β,6α-dihydroxy-4(15)-eudesmene (3), and 1βH,5βH-aromandendrane-4α,10β-diol (4); three triterpenes: acetyl oleanolic acid (5), 3α-hydroxytirucalla-8,24-dien-21-oic acid (6), and ursolic acid (7); and two xanthones: cochinchinone A (8) and α-mangostin (9). Sesquiterpens 1-4 and triterpene 6 were isolated for the first time from stingless bee propolis. Plants in the Cratoxylum and Aglaia genus were suggested as resin sources of the propolis sample. In the antibacterial activity evaluation, the EtOH extract only showed moderate activity on S. aureus, while the isolated compounds 7-9 showed good antibacterial activity, with IC50 values of 0.56 to 17.33 µg/mL. The EtOH extract displayed selective cytotoxicity against the A-549 cancer cell line, with IC50 values of 22.82 ± 0.86 µg/mL, and the xanthones 8 and 9 exhibited good activity against the KB, HepG-2, and A-549 cancer cell lines, with IC50 values ranging from 7.55 ± 0.25 µg/mL to 29.27 ± 2.07 µg/mL. The cytotoxic effects of xanthones 8 and 9 were determined by the inhibition of the EGFR and HER2 pathways using a molecular docking study. Compounds 8 and 9 displayed strong binding affinity with EFGR and HER2, with values of -9.3 to -9.9 kcal/mol. Compounds 5, 8, and 9 showed potential α-glucosidase inhibitory activities, which were further confirmed by computational studies. The binding energies of compounds 5, 8, and 9 were lower than that of arcabose.

Bioactivities of β-mangostin and its new glycoside derivatives synthesized by enzymatic reactions.

Beta-mangostin is a xanthone commonly found in the genus Garcinia. Unlike α-mangostin, to date, there have only been a few studies on the biological activity and derivatization of β-mangostin. In this study, two novel glycosylated derivatives of β-mangostin were successfully synthesized via a one-pot enzymatic reaction. These derivatives were characterized as β-mangostin 6-O-β-d-glucopyranoside and β-mangostin 6-O-β-d-2-deoxyglucopyranoside by TOF ESI/MS and 1H and 13C NMR analyses. Beta-mangostin showed cytotoxicity against KB, MCF7, A549 and HepG2 cancer cell lines, with IC50 values ranging from 15.42 to 21.13 µM. The acetylcholinesterase and α-glucosidase inhibitory activities of β-mangostin were determined with IC50 values of 2.17 and 27.61 µM, respectively. A strong anti-microbial activity of β-mangostin against Gram-positive strains (Bacillus subtilis, Lactobacillus fermentum and Staphylococcus aureus) was observed, with IC50 values of 0.16, 0.18 and 1.24 µg ml-1, respectively. Beta-mangostin showed weaker activity against Gram-negative strains (Salmonella enterica, Escherichia coli and Pseudomonas aeruginosa) as well as Candida albicans fungus, with IC50 and MIC values greater than the tested concentration (greater than 32 µg ml-1). The new derivatives of β-mangostin showed weaker activities than those of β-mangostin, demonstrating the important role of the hydroxyl group at C-6 of β-mangostin in its bioactivity.

Lignans and some other non-alkaloid compounds from the stem bark of Zanthoxylum rhetsa and their biological activities

Four lignans, asarinin (1), horsfieldin (2), 5-(4-(3,4,5-trimethoxyphenyl)hexahydrofuro[3,4-c]furan-1-yl)benzo[d][1,3]dioxole (3), 5-(4-(3,5-dimethoxyphenyl)hexahydrofuro[3,4-c]furan-1-yl)benzo[d][1,3]dioxole (4), and four non-alkaloid compounds, piperonylic acid (5), hesperidin (6), syringin (7), and β-sitosterol (8) were isolated from the stem bark of Zanthoxylum rhetsa grown in Vietnam. Their chemical structures were elucidated by spectroscopic analysis and compared with the references. Except for compound 6, all the remaining compounds (1–5, 7, and 8) were isolated for the first time from Z. rhetsa. The isolated compounds were tested for their cytotoxic activity against three human cancer cell lines, LU-1, Hep-G2, and KB. Compound 5 showed moderate cytotoxic activity against all three cell lines with IC50 values ranging from 48.13 to 49.06 µg mL−1. Notably, compound 6 demonstrated selective cytotoxicity against LU-1, Hep-G2, and KB cancer cell lines (IC50 66.48–67.41 µg mL−1) while non-toxic toward normal Vero cell. Compound 6 also exhibited its ability to inhibit main protease (Mpro) enzyme in vitro with an IC50 value of 55.49 µg mL−1 and in silico with the binding affinity toward targeted protein of −14.36 kcal mol−1.

Anti-imflammatory and cancer cell inhibitory activities of isolated compounds from Aspidistra triradiata N. Vislobokov

Background: The genus Aspidistra possesses biological activities such as antivirus, anti-cancer, anti-inflammation. The study aimed to isolate compounds, evaluate the anti-inflammatory and cytotoxic activities of A. triradiata. Materials and methods: The whole plant of A. triradiata was isolated by chromatographic methods, determined the structure of isolated compounds by NMR spectrum. The anti-inflammatory effect was evaluated by the inhibitory activity against nitric oxide production. The cytotoxic activity was determined by SRB method. Results: Four compounds were isolated from A. triradiata, including (25R)-spirostane-1β,2β,3β,4β,5β,6β-hexol (1), (25R)-17α-hydroxy-spirost-5-en-3β-yl α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)-β-D-glucopyranoside (2), 2-methoxy pancracin (3) and 2-methyl-3-(4,5,7-trihydroxy-8-hydroxymethyltetrahydro-6H-4-pyranyl)-2-propenoic acid (4). Compounds 1, 2 and 4 exhibited moderate anti-inflammatory activities with IC50 values in the range of 59.84 - 98.96 µg/mL. Compound 3 exhibited potent cytotoxicity against the LU-1 and KB cancer cell lines with IC50 values in the range of 0.95 - 0.98 µg/mL, compound 1 showed moderate activity with IC50 values ranging from 47.55 to 72.32 µg/mL. Conclusion: The chemical composition of A. triradiata has been elucidated and some isolated compounds possessing potential anti-inflammatory and cytotoxic activities were discovered. Key words: anti-inflammatory, nitric oxide, cancer, Aspidistra triradiata, NMR spectra.

Phenolic compounds from knema pachycarpa leaves

Knema (Myristicaceae family) is a large genus, comprising over 100 species found in of South East Asian countries, among that over 10 species was found in Vietnam. Knema pachycarpa is a native tree distributed in central provinces of Viet Nam. Until now, only few chemical studies of Knema species in Viet Nam have been reported. Phytochemical study of Knema pachycarpa leaves led to the isolation of seven known compounds including six flavonoids 5,7,3′-trihydroxy-5′-methoxy isoflavone (1), luteolin (2), (-)-narigenin (3), (+)-catechin (4), isoquercetrin (5), and nicotiflorin (6), and a biphenyl compound 3,3',4,4'-tetrahydroxybiphenyl (7). Their structures were elucidated by MS and NMR data analysis and compared with those previously reported. Compounds 3 and 6-7 were found from Knema genus for the first time. In the cytotoxic assay, biphenyl compound (7) exhibited strong cytotoxicity to KB cancer cell line with IC50 value of 2.38 ± 0.11 mg/mL. Compound 7 also displayed showed activity against HepG2, Lu and MCF7 cancer cell lines with IC50 ranges from 18.25 ± 0.92 mg/mL to 35.56 ± 1.17 mg/mL, whereas flavonoids 1-6 were weakly active or inactive against tested cell lines.

Nature-Inspired Chemistry of Complex Alkaloids: Combining Targeted Molecular Networking Approach and Semisynthetic Strategy to Access Rare Communesins in a Marine-Derived Penicillium expansum.

Communesins are rare alkaloids isolated from fungi of the genus Penicillium. In this work, the extract of a marine-derived Penicillium expansum strain was studied using targeted molecular networking approach allowing to detect 65 communesins including 55 new ones. A fragmentation pattern for dimethylvinyl communesins was established and a script was implemented allowing to predict the structure and map all communesins in a global molecular network. A semisynthetic strategy was carried out to obtain some minor congeners from the two isolated communesins A and B. Nine communesins were then synthetised: two of them were already described as produced by the studied strain; four are new natural products which occurrence in the extracts was confirmed; three are new semi-synthetic analogues never described so far. These communesins were evaluated for their cytotoxicity on two human cancer cell lines KB and MCF-7 leading to a preliminary study of their structure-activity relationships.