Phytochemicals Derived from Catharanthus roseus and Their Health Benefits

Catharanthus roseus (C. roseus) is an important medicinal plant distributed in many countries. It has attracted increasing attention due to it being shown to possess a range of phytochemicals with various biological activities such as antioxidant, antibacterial, antifungal, antidiabetic and anticancer properties. Remarkably, vinblastine and vincristine isolated from this plant were the first plant-derived anticancer agents deployed for clinical use. Recently, new isolated indole alkaloids from this plant including catharoseumine, 14′,15′-didehydrocyclovinblastine, 17-deacetoxycyclovinblastine and 17-deacetoxyvinamidine effectively inhibited human cancer cell lines in vitro. Moreover, vindoline, vindolidine, vindolicine and vindolinine isolated from C. roseus leaf exhibited in vitro antidiabetic property. These findings strongly indicate that this plant is still a promising source of bioactive compounds, which should be further investigated. This paper provides an overview of the traditional use and phytochemical profiles of C. roseus, and summarises updated techniques of the preparation of dried material, extraction and isolation of bioactive compounds from this plant. In addition, purported health benefits of the extracts and bioactive compounds derived from this plant were also addressed to support their potential as therapeutic agents.

Download Full-text

Semi-Synthesis and In Vitro Anti-Cancer Evaluation of Magnolol Derivatives

Molecules ◽

10.3390/molecules26144302 ◽

2021 ◽

Vol 26 (14) ◽

pp. 4302

Author(s):

Xiao-Long Sun ◽

Mei-Lin Zhu ◽

Yi-Qun Dai ◽

Hong-Mei Li ◽

Bo-Han Li ◽

...

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

Biological Activities ◽

Migration And Invasion ◽

Dependent Manner ◽

Anticancer Activities ◽

Antitumor Effects ◽

Concentration Dependent Manner ◽

Human Cancer Cell Lines

Magnolol (MAG), a biphenolic neolignan, has various biological activities including antitumor effects. In this study, 15 MAG derivatives were semi-synthesized and evaluated for their in vitro anticancer activities. From these derivatives, compound 6a exhibited the best cytotoxic activity against four human cancer cell lines, with IC50 values ranging from 20.43 to 28.27 μM. Wound-healing and transwell assays showed that compound 6a significantly inhibited the migration and invasion of MDA-MB-231 cells. In addition, Western blotting experiments, performed using various concentrations of 6a, demonstrated that it downregulates the expression of HIF-1α, MMP-2, and MMP-9 in a concentration-dependent manner. Overall, these results suggest that substituting a benzyl group having F atoms substituted at the C2 position on MAG is a viable strategy for the structural optimization of MAG derivatives as anticancer agents.

Download Full-text

Evaluation of Pyrano[3,2 C] Quinoline Analogues as Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666190308122734 ◽

2019 ◽

Vol 19 (10) ◽

pp. 1285-1292 ◽

Cited By ~ 2

Author(s):

Kuldip D. Upadhyay ◽

Anamik K. Shah

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

Biological Activities ◽

Cytotoxic Agents ◽

Tumor Growth Inhibition ◽

Mice Model ◽

One Pot ◽

Aryl Ring ◽

Hct 116

Background: Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. Objective: The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from the fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity. Methods: A library of pyrano[3,2-c]quinoline analogues was prepared from one-pot multi component synthesis using various aromatic aldehydes, malononitrile and 2,4-dihydroxy-1-methylquinoline. The new synthetics were primarily screened for its cytotoxicity (IC50) against different human cancer cell lines in vitro. The promising synthetics were further evaluated in vitro for their potency against different kinase activity. The promising compounds were finally tested for their in vivo efficacy in SCID type mice HCT-116 tumor model. Results: The screening results revealed that compounds 4c, 4f, 4i and 4j showed promising activity in in vitro study. However, compound 4c was found to be the most potent candidate with 23% tumor growth inhibition in HCT-116 tumor mice model. Conclusion: The structure activity relationship suggested that 3-substitution on the aryl ring at C4 position of the pyrano[3,2 c]quinolone moiety seems to have an important position for cytotoxicity activity. However, 3- chloro substitution at C4 aryl ring showed a significant alteration of the bioactive conformer of the parent scaffold and outcome with compound 4c as the most potent candidate of the series.

Download Full-text

Structurally Simple Phenanthridine Analogues Based on Nitidine and Their Antitumor Activities

Molecules ◽

10.3390/molecules24030437 ◽

2019 ◽

Vol 24 (3) ◽

pp. 437

Author(s):

Shu-Qin Qin ◽

Lian-Chun Li ◽

Jing-Ru Song ◽

Hai-Yun Li ◽

Dian-Peng Li

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

A549 Cells ◽

Anticancer Activities ◽

Human Cancer Cell Lines ◽

Ic50 Value ◽

Ic50 Values ◽

Diphenyl Tetrazolium Bromide ◽

Conjugated Compounds

A series of novel structurally simple analogues based on nitidine was designed and synthesized in search of potent anticancer agents. The antitumor activity against human cancer cell lines (HepG2, A549, NCI-H460, and CNE1) was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay in vitro. The results showed that some of them had good anticancer activities, especially derivatives with a [(dimethylamino)ethyl]amino side chain in the C-6 position. Planar conjugated compounds 15a, 15b, and 15c, with IC50 values of 1.20 μM, 1.87 μM, and 1.19 μM against CNE1 cells, respectively, were more active than nitidine chloride. Compound 15b and compound 15c with IC50 values of 1.19 μM and 1.37 μM against HepG2 cells and A549 cells demonstrated superior activities to nitidine. Besides, compound 5e which had a phenanthridinone core displayed extraordinary cytotoxicity against all test cells, particularly against CNE1 cells with the IC50 value of 1.13 μM.

Download Full-text

Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Acta Pharmaceutica ◽

10.2478/acph-2018-0039 ◽

2018 ◽

Vol 68 (4) ◽

pp. 471-483 ◽

Cited By ~ 2

Author(s):

Kristina Pavić ◽

Zrinka Rajić ◽

Zvonimir Mlinarić ◽

Lidija Uzelac ◽

Marijeta Kralj ◽

...

Keyword(s):

Antitumor Activity ◽

Anticancer Agents ◽

Human Cancer ◽

Human Cancer Cell ◽

Urea Derivatives ◽

Design Synthesis ◽

Human Cancer Cell Lines ◽

Lead Compounds ◽

Insight Into

Abstract In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

Download Full-text

Design, Synthesis, and Molecular Docking Study of Novel Heterocycles Incorporating 1,3,4-Thiadiazole Moiety as Potential Antimicrobial and Anticancer Agents

Molecules ◽

10.3390/molecules24061066 ◽

2019 ◽

Vol 24 (6) ◽

pp. 1066 ◽

Cited By ~ 10

Author(s):

Mohamed El-Naggar ◽

Hanan A. Sallam ◽

Safaa S. Shaban ◽

Salwa S. Abdel-Wahab ◽

Abd El-Galil E. Amr ◽

...

Keyword(s):

Molecular Docking ◽

Cell Lines ◽

Anticancer Agents ◽

Human Cancer ◽

Docking Study ◽

Molecular Docking Study ◽

Reference Drug ◽

Human Cancer Cell Lines ◽

Dhfr Inhibitors

A new series of 5-(3,5-dinitrophenyl)-1,3,4-thiadiazole derivatives were prepared and evaluated for their in vitro antimicrobial, antitumor, and DHFR inhibition activity. Compounds 9, 10, 13, and 16 showed strong and broad-spectrum antimicrobial activity comparable to Amoxicillin and Fluconazole as positive antibiotic and antifungal controls, respectively. Compounds 6, 14, and 15 exhibited antitumor activity against four human cancer cell lines, CCRF-CEM leukemia, HCT-15 colon, PC-3 prostate, and UACC-257 melanoma cell lines using Doxorubicin as a reference drug. Compounds 10, 13, 14, and 15 proved to be the most active DHFR inhibitors with an IC50 range of 0.04 ± 0.82–1.00 ± 0.85 µM, in comparison with Methotrexate (IC50 = 0.14 ± 1.38 µM). The highly potent DHFR inhibitors shared a similar molecular docking mode and made a critical hydrogen bond and arene‒arene interactions via Ser59 and Phe31 amino acid residues, respectively.

Download Full-text

Design, Synthesis, and Cytotoxic Evaluation of Novel Lupane Triterpenoid Derived Hydroxamates

Natural Product Communications ◽

10.1177/1934578x20931967 ◽

2020 ◽

Vol 15 (6) ◽

pp. 1934578X2093196

Author(s):

Dang Thi Tuyet Anh ◽

Dinh Thi Cuc ◽

Le Nhat Thuy Giang ◽

Nguyen Thi Hien ◽

Vu Ngoc Doan ◽

...

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

Human Cancer Cell ◽

Design Synthesis ◽

Human Cancer Cell Lines ◽

Lupane Triterpenoids ◽

Lead Compounds ◽

Diphenyltetrazolium Bromide ◽

Derivatives Of

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.

Download Full-text

Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

Croatica Chemica Acta ◽

10.5562/cca3535 ◽

2019 ◽

Vol 92 (3) ◽

pp. 393-402

Author(s):

B. Ramalingeswara Rao ◽

Mohana Rao Katiki ◽

Dileep Kommula ◽

SaiShyam Narayanan ◽

Ruby John Anto ◽

...

Keyword(s):

Anticancer Agents ◽

Human Cancer ◽

In Vitro Cytotoxicity ◽

Sensitive Cell Line ◽

Human Cancer Cell Lines ◽

Ic50 Values ◽

Different Origins ◽

New Compounds ◽

A549 Lung

The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.

Download Full-text

Cytotoxicity and Anti-cancer Activity of the Genus Achillea L.

Current Medicinal Chemistry ◽

10.2174/0929867327666200505092514 ◽

2020 ◽

Vol 27 (41) ◽

pp. 6910-6925 ◽

Cited By ~ 1

Author(s):

Konstantina Papakosta ◽

Maria-Eleni Grafakou ◽

Christina Barda ◽

Ioannis V. Kostopoulos ◽

Ourania Tsitsilonis ◽

...

Keyword(s):

Secondary Metabolites ◽

Traditional Medicine ◽

Human Cancer ◽

Biological Activities ◽

Northern Greece ◽

Human Cancer Cell Lines ◽

Anti Cancer ◽

Analgesic Agents ◽

Selection Of

Background: The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. Objective: Following a literature survey, we discuss the anti-cancer properties of Achillea species, taking into consideration ethnopharmacological data on their use in traditional medicine for the treatment of cancer. In addition, we screened extracts and isolated secondary metabolites from A. coarctata for cytotoxicity, upon information based on local traditional medicine. The plant was collected in Kozani (Northern Greece), where it is locally used for treating gastrointestinal disorders, including stomach cancer. Methods: A selection of the relevant data was performed through a search in PubMed, Scopus, Google Scholar and Science Direct databases. In addition, extracts and isolated compounds from A. coarctata were tested for their in vitro activity against the human cancer cell lines MCF-7 and HeLa. Conclusion: The genus Achillea L. is a valuable source of bioactive secondary metabolites. The most significant outcome of the investigation of medicinal plants is the documentation and the assessment of the traditional information and its use and perspectives in the light of modern pharmacology.

Download Full-text

IN VITRO CYTOTOXIC ANTICANCER POTENTIAL OF BIOACTIVE FRACTION ISOLATED FROM INDONESIAN TIDAL SPONGE CALTHROPELLA SP.

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v12i1.23655 ◽

2019 ◽

Vol 12 (1) ◽

pp. 380

Author(s):

Fitria Susilowati ◽

Respati Tri Swasono ◽

Tatsufumi Okino ◽

Winarto Haryadi

Keyword(s):

High Resolution ◽

Cytotoxic Activity ◽

Cell Lines ◽

Bioactive Compounds ◽

Human Cancer ◽

Human Cancer Cell Lines ◽

Anticancer Properties ◽

Bioactive Fraction ◽

Mcf 7

Objective: This study was taken to examine the cytotoxicity of the bioactive fraction isolated from marine sponge Calthropella sp. as a preliminary anticancer assay and identify its bioactive compounds.Methods: The cytotoxic activity was assessed by 3-(4,5-dimethylthiazol-2-y1)-2,5-diphenyltetrazolium bromide assay against three human cancer cell lines, namely human breast (MCF-7), human lung (H-460), and human liver (HepG-2). The bioactive compounds were identified using a high-resolution liquid chromatography–mass spectroscopy (LC–MS).Results: The active fraction 7 showed moderate to strong cytotoxic activity on all cell lines tested and promising a strong potent cytotoxicity against MCF-7 cell lines with IC50 value as low as 1.925 μg/mL comparable to control, cisplatin (IC50 0.977 μg/mL). In regard to the promising bioactive compounds, the high-resolution LC–MS predicted the existing of several known compounds such as bengamide Q, clavepictine A, 4’-N-methyl-5’- hydroxystaurosporine, carteriofenone A, and one strong possibility of a new compound.Conclusion: This study has revealed that the isolated bioactive fraction of Indonesian tidal sponge, Calthropella sp., possesses potential anticancer properties with a promising significant cytotoxicity on MCF-7 cell lines (IC50 1.925 μg/mL).

Download Full-text

Ethnomedicinal Use, Phytochemistry, Pharmacology, and Toxicology of Salvia verbenaca L. : A Review

Biointerface Research in Applied Chemistry ◽

10.33263/briac122.14371469 ◽

2021 ◽

Vol 12 (2) ◽

pp. 1437-1469

Keyword(s):

Essential Oils ◽

Bioactive Compounds ◽

Biological Activities ◽

Traditional Use ◽

Toxicological Effects ◽

Stomach Pain ◽

Toxicological Investigation ◽

Phytochemical Compounds

Salvia verbenaca L. is a Mediterranean medicinal plant used traditionally to treat several diseases such as burns, ocular wounds, contusion, stomach pain, eye diseases, dermal inflammation. This review highlighted previous reports, including the botanical, taxonomical, geographical distribution, traditional use, phytochemical, biological, and toxicological effects of S. verbenaca. The data were gathered from scientific databases PubMed, Scopus, Web of Science, Google Scholar, ScienceDirect, SpringerLink. The presented data on S. verbenaca were organized according to ethnomedicinal use, bioactive compounds, pharmacology, and toxicological investigation. Ethnobotanical studies reported that many folk medicines use S. verbenaca, especially against wounds, burns, and cicatrization. The phytochemical compounds in different parts of S. verbenaca belonged to different classes of chemical compounds, including terpenoids, flavonoids, phenolic acids, phenolic diterpenoids, and fatty acids. The extracts and essential oils from S. verbenaca have a wide variety of in vitro and in vivo pharmacological activities, i.e., antioxidant, antifungal, antidiabetic, anti-inflammatory, antitumor, antihemolytic, antihypertensive, antileishmanial, and immunomodulatory activities. This research suggests that the biological activities of S. verbenaca prove its traditional uses. However, in-depth investigations are required, such as pharmacokinetic, pharmacodynamic, and toxicological experiments, to prove the efficacy and safety of S. verbenaca extracts and essential oils and their bioactive compounds.

Download Full-text