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result(s) for
"Antineoplastic Agents - isolation "
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Bioactivity-Directed Isolation of Anticancer Constituents from Underexplored Folklore: Rhus punjabensis Stewart
by
Ali, Joham Sarfraz
,
Ahmad, Abdul Momin Rizwan
,
Akhtar, Myra
in
Animals
,
Antimitotic agents
,
Antineoplastic agents
2025
Background: Medicinal plants continue to offer a promising source of novel bioactive compounds for cancer therapy due to their affordability, biocompatibility, and low toxicity. Rhus punjabensis Stewart, an ethnomedicinal species from the family Anacardiaceae, has long been used in the traditional medicine of northern Pakistan to treat inflammatory, hepatic, and infectious diseases. However, its phytochemical composition and anticancer potential remain largely unexplored. Methods: This study employed a bioactivity-guided isolation strategy to identify and characterize anticancer constituents from R. punjabensis leaves. The plant material was sequentially fractionated using solvents of increasing polarity, followed by purification via column chromatography. Each fraction and purified compound was evaluated using antioxidant (DPPH, total antioxidant capacity, and total reducing power) and cytotoxic assays, including brine shrimp lethality, Sulfo-rhodamine B (SRB) against five human cancer cell lines, protein kinase inhibition, and NF-κB chemo-preventive assays. Results: Comparative analysis of spectral data (UV, 1D/2D NMR, and ESI-MS) led to the identification of three triterpenoid compounds—Lupeol, Cycloartenol, and β-sitosterol—reported for the first time from R. punjabensis. Among them, Lupeol displayed the most potent cytotoxicity against DU-145 prostate (IC50 = 11.2 ± 1.2 μg/mL) and HL-60 leukemia (IC50 = 15.2 ± 1.1 μg/mL) cell lines and showed significant NF-κB inhibitory activity (IC50 = 19.4 ± 1.1 μg/mL), indicating its chemo-preventive potential. Cycloartenoland β-sitosterol exhibited moderate antioxidant and antimicrobial activities. Conclusion: The findings validate the ethnopharmacological use of R. punjabensis and confirm it as a new source of triterpenoids with notable anticancer activity. This study provides the first comprehensive account of its bioactive metabolites, reinforcing the significance of bioactivity-directed isolation as a powerful approach for discovering natural anticancer agents. Further in vivo and mechanistic evaluations are warranted to establish their therapeutic efficacy and safety profiles.
Journal Article
Ultrasound-Assisted Pressurized Fluid Extraction of Antioxidant and Anticancer Molecules from a Mangaba, Cambuí and Red Propolis Blend
by
Dariva, Claudio
,
Corrêa, Cristiane B.
,
Santos, Klebson S.
in
Antineoplastic Agents - chemistry
,
Antineoplastic Agents - isolation & purification
,
Antineoplastic Agents - pharmacology
2025
This study explored the antioxidant and anticancer potential of extracts obtained from the mangaba, cambuí, and red propolis blend. The extracts were obtained using ultrasound-assisted pressurized fluid extraction (UAPFE) at 50 bar, 60 °C, and a flow rate of 2 mL/min. Both sequential extraction with solvents of increasing polarity (propane followed by ethanol/water) and one-step extraction were employed for 30 min. Extracts were characterized by ultra-high-resolution mass spectrometry, total phenolic content, antioxidant activity (via DPPH and FRAP assays), and cytotoxicity using the sulforhodamine B colorimetric method. Among the tested conditions, the sequential extraction with ethanol/water (UAPFE-SE) yielded 16.2 ± 3.0% (overall extraction yield), with high phenolic content (24.1 ± 0.4 µg/mg). Mass spectrometry revealed the presence of antiproliferative phenolics. The UAPFE-SE extract demonstrated moderate antioxidant activity, with FRAP values of 394.0 ± 6.0 µg Fe2+/mg and DPPH scavenging capacity of 28.5 ± 0.3 µg Trolox equivalents/mg. Additionally, it exhibited cytotoxic inhibition of 82.3 ± 1.7% against lung carcinoma cells at a concentration of 100 μg/mL. The results suggest that the antioxidant properties and cytotoxic effect against lung cancer cells in vitro warrant further investigation to assess therapeutic potential.
Journal Article
Purification of Lepidilines A, B, C, and D from Lepidium meyenii Walpers by Centrifugal Partition Chromatography Followed by Semi-Preparative HPLC and Preliminary Evaluation of Anticancer Activity Against Neuroblastoma Cell Lines
by
Skaltsounis, Leandros A.
,
Okoń, Estera
,
Kukula-Koch, Wirginia
in
Analysis
,
Antineoplastic Agents - chemistry
,
Antineoplastic Agents - isolation & purification
2025
Lepidium meyenii Walpers (syn. Lepidium peruvianum Chacon) has been cultivated for centuries in the Peruvian Andes as both a vegetable and a traditional medicine resource. Maca is classified as a superfood and is widely used as a dietary supplement, particularly noted for its potential to enhance endurance, fertility, and endocrine balance. In recent years, there has been a growing interest in the cytotoxic effects of lepidilines and their derivatives; however, these compounds have been less extensively studied due to challenges associated with their isolation. This study aims to establish optimal extraction conditions to enrich lepidiline content in the extracts and to propose an efficient isolation method for four lepidilines using a green purification technique known as Centrifugal Partition Chromatography (CPC). The isolated compounds will be evaluated for their anticancer potential utilizing the MTT assay on SK-N-SH (ATCC® HTB-11™) and SK-N-AS (ATCC® CRL-2137™) neuroblastoma cell lines. The findings indicate that Soxhlet extraction with dichloromethane resulted in the highest recovery of lepidilines, with a content of 10.24% expressed as lepidiline A. The optimal biphasic solvent mixture suitable for CPC chromatographic applications was identified as a combination of chloroform, methanol, and water (4:3:2 v/v/v) containing 60 mM HCl. When utilized in conjunction with semi-preparative high-performance liquid chromatography (HPLC), this method successfully isolated lepidilines A–D, achieving a purity exceeding 95%. Notably, lepidiline B exhibited the highest cytotoxic potential, with an IC50 value of 14.85 µg/mL in SK-N-AS cells.
Journal Article
Extraction of Curcuminoids and Carvacrol with Biobased Ionic Liquids—Evaluation of Anti-Cancer Properties of Curcuminoid Extracts
by
Salami, Chefikou
,
Brassart-Pasco, Sylvie
,
Mbakidi, Jean-Pierre
in
Acids
,
anti-cancer
,
Antineoplastic Agents - chemistry
2025
Six biobased ionic liquids were prepared from saturated fatty acids (octanoic, decanoic and dodecanoic acids) and choline with yields up to 90% following procedures respecting green chemistry principles. These ionic liquids were fully characterized (NMR, IR, elemental analysis, viscosimetry and TGA) and used as extraction solvents for bioactive compounds (curcuminoids and carvacrol) using classical conditions, and the ionic liquids were able to be recovered after five runs without loss of activity. The ionic liquid containing a C12 carbon chain was the best extracting solvent, extracting 95% of the total curcuminoids contained in turmeric and 69% of the total carvacrol contained in oregano, which are higher yields compared to the extraction procedures described in the literature. As C12 ionic liquids were more cytotoxic than C8 ones, the biological activity of the curcuminoids extracted with C8 ionic liquids was evaluated on a MIAPaCa-2, a pancreatic adenocarcinoma cell line for which antitumor activity of curcuminoids had previously been reported. Compared to the cytotoxicity of the commercially available extract, the cytotoxic activity of the extracts was slightly weaker.
Journal Article
Phytochemical Study and In Vitro Antioxidant Activity of Helianthemum cinereum Along with Antitumor Activity of the Isolated trans-Tiliroside and Luteolin 4′-O-β-Xyloside
by
Salvador, Diana
,
Smadi, Abla
,
Benhabrou, Hakim
in
Acids
,
Antineoplastic Agents - chemistry
,
Antineoplastic Agents - isolation & purification
2024
Twelve compounds (1–12), kaempferol (1), luteolin (2), luteolin 4′-O-β-xyloside (3), luteolin 4′-O-β-glucoside (4), quercetin 4′-O-β-xyloside (5), kaempferol-3-O-[6″-O-(E)-p-coumaroyl]-β-D-glucoside (trans-tiliroside) (6), protocatechuic acid (7), gallic acid (8), methyl gallate (9), ethyl gallate (10), shikimic acid-3-O-gallate (11), and 3,3′,4′-tri-O-methyl-ellagic acid 4-sulfate (12), were isolated and identified from the aerial parts of Helianthemum cinereum (Cav.) Pers (synonym: Helianthemum rubellum C. Presl. All compounds were isolated by applying different chromatographic procedures, such as silica gel, RP-18 and Sephadex LH-20 columns. The structures were elucidated by extensive spectroscopic methods, mainly nuclear magnetic resonance NMR 1D and 2D, and mass spectrometry, as well as by comparison with the reported spectroscopic data. The two organic extracts, ethyl acetate (EtOAc) and butanol (BuOH), were evaluated for their potent phenolic and flavonoid contents using the Folin–Ciocalteu and aluminum chloride colorimetric methods. Furthermore, the antioxidant activity of the two extracts was determined using the DPPH, FRAP, and ABTS methods. Pure trans-tiliroside (6), the main isolated compound, and luteolin 4′-O-β-xyloside (3) were evaluated for their antitumor activity against the lung cancer (A549), melanoma (A375) and pancreatic cancer (Mia PaCa-2 and Panc-1) cell lines by MTT assay.
Journal Article
Analysis of Macroporous Resin Combined Extraction and Purification of Polyphenols from Agrimonia pilosa Ledeb. and Anti-Tumor Effect In Vitro
by
Li, Tingting
,
Taoli, Huiping
,
Pan, Linmei
in
Adsorption
,
Agrimonia - chemistry
,
Agrimonia pilosa Ledeb
2025
Agrimonia pilosa Ledeb. (APL), a traditional Chinese herb frequently employed by Professor Zhou Zhongying, a master of traditional Chinese medicine, for colorectal cancer treatment, is rich in polyphenols with potential anti-tumor properties. To elucidate its bioactive components, this study developed a two-step purification process combining macroporous resin adsorption and liquid–liquid extraction to enrich polyphenols from APL (APLs). The adsorption/desorption mechanisms of APLs on macroporous resins were systematically investigated through resin screening, adsorption kinetics, and thermodynamics. The Langmuir isotherm model confirmed the adsorption process as spontaneous and exothermic. Pseudo-second-order kinetics effectively described the adsorption behavior of D101 resin. Optimized adsorption and column elution parameters were established, followed by liquid–liquid extraction for further purification. The components were compared and analyzed by ultra-performance liquid chromatography and quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-Zeno-TOF-MS/MS). It was preliminarily identified that 29 polyphenols were mainly concentrated in water-saturated n-butanol (BEA) and ethyl acetate (ECA) extract fractions. Quantitative analysis using ultra-high performance liquid chromatography–triple quadrupole liquid chromatography–mass spectrometry (UHPLC-C-QTRAP-MS/MS) revealed higher contents of catechin (66.67 ± 1.33 ng·mg−1), hyperoside (382.56 ± 3.65 ng·mg−1), and chlorogenic acid (10.60 ± 0.05 ng·mg−1) in BEA compared to ECA (46.00 ± 2.00, 239.40 ± 2.60, and 3.42 ± 0.01 ng·mg−1, respectively). In vitro experiments demonstrated that BEA exhibited superior antiproliferative activity (IC50: 434.5 μg·mL−1) and significantly inhibited CT26 tumor cell migration compared to ECA (IC50: 672.5 μg·mL−1). The enhanced biological activity of BEA may be due to its higher polyphenol content, suggesting that these compounds mediate their anti-tumor effects through different biochemical pathways. This work lays the foundation for exploring the multi-target mechanism of anti-tumor effects of APLs.
Journal Article
Enhancement of anti-cancer compounds in fungal elicited-Oldenlandia umbellata culture
by
Saranya, S.
,
Chellapandi, P.
,
Velayutham, P.
in
Anthraquinone
,
Anthraquinones - isolation & purification
,
Anthraquinones - pharmacology
2024
Our study focused on enhancing the production of anthraquinone derivatives in
Oldenlandia umbellata
using fungal elicitors.
Aspergillus niger
,
Mucor prayagensis
, and
Trichoderma viride
were used to elicit the anthraquinone derivatives in root cultures. The elicitation process led to an increase in the production of phytochemicals and secondary metabolites, with the highest total protein content observed in
A. niger
-elicited plants. We performed qualitative and quantitative phytochemical screening of the 80% methanol extract of the plants. Using reverse phase-ultra-fast liquid chromatography, we identified and quantified five anthraquinone compounds: aloe-emodin, rhein, emodin, chrysophanol, and alizarin. The in vitro root samples elicited with
A. niger
and
M. prayagensis
exhibited four and three anthraquinone derivatives, respectively, whereas those elicited with
T. viride
showed only two derivatives. Interestingly, chrysophanol content was the highest in
A. niger
-elicited root samples. We constructed a system pharmacology framework consisting of 40 nodes and 45 edges with 34 interacting genes. We also identified human proteins that interact with these derivatives, and inferred their roles in cancer-associated pathways. These anthraquinone derivatives interact with various proteins in multiple pathways, including apoptosis, human cytomegalovirus infection, proteoglycans in cancer, MAPK signaling, and hepatitis C, highlighting their potential therapeutic applications in cancer treatment.
Journal Article
Evaluation of the Antioxidant, Anticancer, and Antibacterial Activities of Flower and Leaf Extracts of Chrysanthemum indicum
by
Alsayed, Mashail Fahad
,
Aziz, Ibrahim M.
,
Farrag, Mohamed A.
in
A549 Cells
,
Acids
,
Anti-Bacterial Agents - chemistry
2025
Chrysanthemum has been studied for its anti‐inflammatory, antibacterial, anticancer, antioxidant, and other pharmacological properties. However, there is little knowledge about the methanol–pharmaceutical activities of Chrysanthemum indicum leaves and flowers. This study is designed to assess the in vitro antioxidant, anticancer, and antibacterial activities of C. indicum extracts. The flowers and leaves of C. indicum are extracted. Gas chromatography–mass spectrometry is used to analyze the chemical components. The antioxidant activity is evaluated using 2,2‐diphenyl‐1‐picrilhidrazine (DPPH) and 2,2′‐azino‐bis (3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS) assays. Cytotoxic effect against A549 cell line is identified. The antibacterial properties are evaluated against both Gram‐positive and Gram‐negative bacteria. Antioxidant activity is detected and observed to be maximum at higher concentrations. The IC50 values of flowers and leaves are 77.19 ± 2.4 and 101.94 ± 2.34 μg mL−1, respectively, in the DPPH method, whereas the ABTS assay shows 93.21 ± 3.42 and 98.22 ± 3.34 μg mL−1, respectively. The flower extract has more cytotoxic activity than the leaves (P < 0.05). The IC50 values for flowers and leaves are 72.49 ± 3.14 and 102.54 ± 4.17 μg mL−1, respectively. Furthermore, the flower and leaf extracts exhibit the most pronounced antibacterial activity. These results provide a strong basis for further research into its potential therapeutic uses as well as opportunities for the creation of natural pharmaceutical products. The tested methanolic extract of Chrysanthemum indicum flower and leaf is a rich source of bioactive molecules with significant antioxidant activity at low doses, potential anticancer effects at lower concentrations, and antimicrobial activities against Gram‐positive and Gram‐negative species, which is consistent with the plant's traditional applications.
Journal Article
Marine Rare Actinomycetes: A Promising Source of Structurally Diverse and Unique Novel Natural Products
by
Sipkema, Detmer
,
Subramani, Ramesh
in
Actinobacteria - chemistry
,
Actinomycetes
,
Anti-Bacterial Agents - chemistry
2019
Rare actinomycetes are prolific in the marine environment; however, knowledge about their diversity, distribution and biochemistry is limited. Marine rare actinomycetes represent a rather untapped source of chemically diverse secondary metabolites and novel bioactive compounds. In this review, we aim to summarize the present knowledge on the isolation, diversity, distribution and natural product discovery of marine rare actinomycetes reported from mid-2013 to 2017. A total of 97 new species, representing 9 novel genera and belonging to 27 families of marine rare actinomycetes have been reported, with the highest numbers of novel isolates from the families Pseudonocardiaceae, Demequinaceae, Micromonosporaceae and Nocardioidaceae. Additionally, this study reviewed 167 new bioactive compounds produced by 58 different rare actinomycete species representing 24 genera. Most of the compounds produced by the marine rare actinomycetes present antibacterial, antifungal, antiparasitic, anticancer or antimalarial activities. The highest numbers of natural products were derived from the genera Nocardiopsis, Micromonospora, Salinispora and Pseudonocardia. Members of the genus Micromonospora were revealed to be the richest source of chemically diverse and unique bioactive natural products.
Journal Article
Health Properties and Composition of Honeysuckle Berry Lonicera caerulea L. An Update on Recent Studies
by
Gołba, Marta
,
Sokół-Łętowska, Anna
,
Kucharska, Alicja Z.
in
Acids
,
anthocyanins
,
Anthocyanins - chemistry
2020
Lonicera caerulea L., also known as haskap or honeysuckle berry, is a fruit commonly planted in eastern Europe, Canada and Asia. The fruit was registered as a traditional food from a third country under European Union regulations only on December 2018. It is resistant to cold, pests, various soil acidities and diseases. However, its attractiveness is associated mostly with its health properties. The fruit shows anticancer, anti-inflammatory, and antioxidant activity—important factors in improving health. These features result from the diverse content of phytochemicals in honeysuckle berries with high concentrations of phytocompounds, mainly hydroxycinnamic acids, hydroxybenzoic acids, flavanols, flavones, isoflavones, flavonols, flavanones and anthocyanins but also iridoids, present in the fruit in exceptional amounts. The content and health properties of the fruit were identified to be dependent on cultivar, genotype and the place of harvesting. Great potential benefits of this nutritious food are its ability to minimize the negative effects of UV radiation, diabetes mellitus and neurodegenerative diseases, and to exert hepato- and cardioprotective activity.
Journal Article