scholarly journals Chemical Profile, Cytotoxic Activity and Oxidative Stress Reduction of Different Syringa vulgaris L. Extracts

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3104
Author(s):  
Daniela Hanganu ◽  
Mihaela Niculae ◽  
Irina Ielciu ◽  
Neli-Kinga Olah ◽  
Melania Muntean ◽  
...  

Syringa vulgaris L. (common lilac) is one of the most popular ornamental species, but also a promising not comprehensively studied source of bioactive compounds with important therapeutic potential. Our study was designed to characterize the chemical composition and to assess the antioxidant and cytotoxic properties of ethanolic extracts obtained from S. vulgaris L. flowers, leaves, bark, and fruit. The chemical profile of the ethanolic extracts was investigated using chromatographic (HPLC-DAD-ESI+, GC-MS) and spectral (UV-Vis, FT-IR) methods, while the protective effect against free radicals was evaluated in vitro by different chemical assays (DPPH, FRAP, CUPRAC). The cytotoxic activity was tested on two tumoral cell lines, HeLa, B16F10, using the MTT assay. Significant amounts of free or glycosylated chemical components belonging to various therapeutically important structural classes, such as phenyl-propanoids (syringin, acteoside, echinacoside), flavonoids (quercetin, kaempferol derivatives) and secoiridoids (secologanoside, oleuropein, 10-hydroxy oleuropein, demethyloleuropein, syringalactone A, nuzhenide, lingstroside) were obtained for the flowers, leaves and bark extracts, respectively. Furthermore, MTT tests pointed out a significant cytotoxic potential expressed in a non-dose-dependent manner toward the tumoral lines. The performed methods underlined that S. vulgaris extracts, in particular belonging to flowers and leaves, represent valuable sources of compounds with antioxidant and antitumoral potential.

Blood ◽  
1998 ◽  
Vol 91 (7) ◽  
pp. 2452-2458 ◽  
Author(s):  
Hiromichi Matsushita ◽  
Masahiro Kizaki ◽  
Hiroyuki Kobayashi ◽  
Hironori Ueno ◽  
Akihiro Muto ◽  
...  

Complete remission is achieved in a high proportion of patients with acute promyelocytic leukemia (APL) after all-trans retinoic acid (RA) treatment, but most patients relapse and develop RA-resistant APL. We have previously reported that both RA-resistant HL-60 (HL-60R) and APL cells express P-glycoprotein and MDR1 transcripts; and these cells differentiate to mature granulocytes after culture with RA and P-glycoprotein antagonist. Ribozymes have been shown to be able to intercept a target RNA by catalytic activity. To address the role of MDR1 in overcoming RA-resistance in APL cells, we investigated the biologic effects of ribozymes against the MDR1 transcript in HL-60R cells. These ribozymes efficiently cleaved MDR1 mRNA at a specific site in vitro. The 196 MDR1 ribozyme was cloned into an expression vector, and stably transfected (HL-60R/196Rz) cells were obtained. Expression of MDR1 transcripts was decreased in HL-60R/196Rz cells compared with parental HL-60R and empty vector-transfected (HL-60R/neo) cells. Interestingly, RA inhibited cellular proliferation and induced differentiation of HL-60R/196Rz cells in a dose-dependent manner, suggesting reversal of drug resistance in HL-60R cells by the MDR1 ribozyme. These data are direct evidence that P-glycoprotein/MDR1 is responsible in part for acquired resistance to RA in myeloid leukemic cells. The MDR1 ribozyme may be a useful tool for investigating the biology of retinoid resistance and may have therapeutic potential for patients with RA-resistant APL.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Myeong A Choi ◽  
Sun You Park ◽  
Hye Yun Chae ◽  
Yoojin Song ◽  
Chiranjeev Sharma ◽  
...  

Abstract To develop novel CNS penetrant HDAC inhibitors, a new series of HDAC inhibitors having benzoheterocycle were designed, synthesized, and biologically evaluated. Among the synthesized compounds, benzothiazole derivative 9b exhibited a remarkable anti-proliferative activity (GI50 = 2.01 μM) against SH-SY5Y cancer cell line in a dose and time-dependent manner, better than the reference drug SAHA (GI50 = 2.90 μM). Moreover, compound 9b effectively promoted the accumulation of acetylated Histone H3 and α-tubulin through inhibition of HDAC1 and HDAC6 enzymes, respectively. HDAC enzyme assay also confirmed that compound 9b efficiently inhibited HDAC1 and HDAC6 isoforms with IC50 values of 84.9 nM and 95.9 nM. Furthermore, compound 9b inhibited colony formation capacity of SH-SY5Y cells, which is considered a hallmark of cell carcinogenesis and metastatic potential. The theoretical prediction, in vitro PAMPA-BBB assay, and in vivo brain pharmacokinetic studies confirmed that compound 9b had much higher BBB permeability than SAHA. In silico docking study demonstrated that compound 9b fitted in the substrate binding pocket of HDAC1 and HDAC6. Taken together, compound 9b provided a novel scaffold for developing CNS penetrant HDAC inhibitors and therapeutic potential for CNS-related diseases.


2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Na Dong ◽  
Zhong Dong ◽  
Ying Chen ◽  
Xiaosu Gu

Parkinson’s disease (PD) is the second most common neurodegenerative disease. Crocetin, derived from saffron, exerts multiple pharmacological properties, such as anti-inflammatory, antioxidant, antifatigue, and anticancer effects. However, the effect of crocetin on PD remains unclear. In this study, we designed experiments to investigate the effect of crocetin against MPTP-induced PD models and the underlying mechanisms. Our results showed that crocetin treatment attenuates MPTP-induced motor deficits and protects dopaminergic neurons. Both in vivo and in vitro experiments demonstrated that crocetin treatment decreased the expression of inflammatory associated genes and inflammatory cytokines. Furthermore, crocetin treatment protected mitochondrial functions against MPP+ induced damage by regulating the mPTP (mitochondrial permeability transition pore) viability in the interaction of ANT (adenine nucleotide translocase) and Cyp D (Cyclophilin D) dependent manner. Therefore, our results demonstrate that crocetin has therapeutic potential in Parkinson’s disease.


2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Yin Lu ◽  
Xiangtao Du ◽  
Lidan Lai ◽  
Hao Jin

The antioxidant potential ofActinidia macrospermaC. F. Liang (Actinidiaceae) was investigated in vitro for total phenolic content, along with total antioxidant activity (TAA), 1,1-diphenyl 2-picryl hydrazyl (DPPH), and lipid peroxidation (LP). The results indicated that different polarity extracts ofA. macrospermaexhibit different biological activities, which depends mainly on the presence of phenolic compounds. The antioxidant activity was in the following decreasing order: MeOH extract > EtOAc extract > aqueous extract > CHCl3extract > Hexane extract. Moreover, the cytotoxic activity of this plant by MTT dye assay using SMMC-7721 has been determined also. The hexane, EtOAc, and CHCl3extracts showed cytotoxicity in a dose-dependent manner. Methanol and aqueous extracts, however, showed weak activities in this test. And a very significant cytotoxic activity, not significantly different from the positive control of quercetin, was observed in CHCl3extract.


Author(s):  
Hassan Mohammed Al-Mahbashi ◽  
Mohammad Abobakr Al-Ghazali ◽  
Hassan A. Al-Shamahy ◽  
Azhar Azher Mohammed Al-Ankoshy

 Background and aims: Natural products, in particular plant extracts, have opened up great chance in the area of drug progress owing to their chemical variety. The Aloe genus has long been known to be used for medicinal uses in countless parts of the world. This study was planned to inspect the phytochemicals and anti-cancer capabilities of Aloe rubroviolaceae, Aloe vera and Aloe sabaea flowers. Materials and Methods: Three types of ethanolic extracts of plants traditionally used in Yemen to treat a variety of diseases have been tested in vitro for their potential anticancer activity on different human cancer cell lines. The cytotoxic activity of the ethanolic extracts of tested plants was determined using eleven strains of human cancer cells, namely: MCF-7 (breast cancer), PC-3 (prostate cancer), HEP-2(human epithelial carcinoma), MNFS-60 (myelogenous leukemia), CACO (intestinal cancer), A-549 (lung adenocarcinoma), HeLa (cervical cancer),RD (rhabdomyosarcoma), HepG2 (hepatocellular carcinoma), HCT-116 (colon cancer),  and CHO-K1(Chinese hamster ovary). A colorimetric sulforhodamine B assay was applied to assess the in vitro cytotoxic activity of various extracts. Growth inhibition of 50% (IC50) for each extract was calculated from the optical density of treated and untreated cells. Doxorubicin, a broad-spectrum anticancer drug was used as a positive control. Results: More interesting cytotoxic activity was observed for Aloe vera extract more than Aloe sabaea and Aloe rubroviolaceae, extract.  Conclusions: This study presents an initial screening for anti-proliferative activity of a variety of Aloe species flowers extracts on diverse cancer cell lines. Different extracts of Aloe species significantly inhibit the growth of various cancer cell lines  in a concentration-dependent manner. Advance researches are necessary to understand the possible mechanism(s) of action of these extract on a variety of cancer cells and separation of active phyto-chemicals.                   Peer Review History: Received: 18 July 2021; Revised: 17 August; Accepted: 8 September, Available online: 15 September 2021 Academic Editor:  Dr. Muhammad Zahid Iqbal, AIMST University, Malaysia, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.  Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 6.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewers: Dr. U. S. Mahadeva Rao, Universiti Sultan Zainal Abidin, Terengganu Malaysia, [email protected] Dr. Nazim Hussain, BFIT, Dehradun, Uttarakhand, India, [email protected] Similar Articles: ANTIFUNGAL, CYTOTOXIC AND PHYTOTOXICITY OF AERIAL PART OF RANUNCULUS MURICATUS IN VITRO INHIBITORY ACTIVITY OF BERBERIS VULGARIS L. AGAINST LEISHMANIA TROPICA PROMASTIGOTES


Author(s):  
Yamini N ◽  
Lahari S ◽  
Phani deepthi V

Using an in vitro model, the anti-thrombolytic efficacy of ethanolic extracts of Ocimum kilimandscharicum Linn was investigated. The researchers discovered that different concentrations of the extract had significant anti-thrombolytic activity in a dose-dependent manner , which was comparable to a standard drug. As a result of the presence of flavonoids and polyphenols in the plant extract, it can be concluded that it has a promising future in the treatment of thrombosis. This knowledge will be useful in the clinical development of thrombolytic therapeutics by identifying more potent anti-thrombolytic principles from natural resources..    


Author(s):  
Deepak Kumar U ◽  
Nivetha L ◽  
Devipriya Nisha P

Recent research is focusing on the search for new types of natural chemotherapeutic agents derived from plants which are proving to be excellent sources of new compounds. The present research article was aimed to study the antioxidant activity of ethanolic extracts of Dombeya wallichii, which is an invasive plant (Plants that do not occur naturally in a region but proliferate in the area they have been introduced into) by DPPH radical scavenging method which exhibited antioxidant activity with IC50 value of 744.04 µg /ml. The cytotoxic activity of ethanolic extracts from the leaves of Dombeya wallichii, by in-vitro cytotoxic assays like MTT against lung adenocarcinoma epithelial cell line A549 which exhibited anticancer activity with IC50 value of 2.50 µg /ml concentration. This study creates the awareness about this plant which is having potential antioxidant activity, cytotoxic activity and the outcomes propose that D. wallichii as a potential source of alternative medication drugs for treating cancer. Further research is required to find out the effective mechanisms responsible for anticancer properties and for curating the therapeutic benefits of the less explored and exploited invasive species.


Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1598 ◽  
Author(s):  
William Meza-Morales ◽  
M. Mirian Estévez-Carmona ◽  
Yair Alvarez-Ricardo ◽  
Marco A. Obregón-Mendoza ◽  
Julia Cassani ◽  
...  

At the present time, scientists place a great deal of effort worldwide trying to improve the therapeutic potential of metal complexes of curcumin and curcuminoids. Herein, the synthesis of four homoleptic metal complexes with diacetylcurcumin (DAC), using a ligand designed to prevent the interaction of phenolic groups, rendering metal complexes through the β-diketone functionality, is reported. Due to their physiological relevance, we used bivalent magnesium, zinc, copper, and manganese for complexation with DAC. The resulting products were characterized by ultraviolet-visible (UV-Vis), fluorescence spectroscopy, infrared spectroscopy (IR), liquid and solid-state nuclear magnetic resonance (NMR), electron paramagnetic resonance (EPR), magnetic moment, mass spectrometry (MS), single crystal, and powder X-ray diffraction (SCXRD and PXRD). Crystallization was achieved in dimethylsulfoxide (DMSO) or N,N-dimethylformamide (DMF) as triclinic systems with space group P-1, showing the metal bound to the β-diketone function, while the 1H-NMR confirmed the preference of the enolic form of the ligand. Single crystal data demonstrated a 1:2 metal:ligand ratio. The inhibition of lipid peroxidation was evaluated using the thiobarbituric acid reactive substance assay (TBARS). All four metal complexes (Mg, Zn, Cu, and Mn) exhibited good antioxidant effect (IC50 = 2.03 ± 0.27, 1.58 ± 0.07, 1.58 ± 0.15 and 1.24 ± 0.10 μM respectively) compared with butylated hydroxytoluene (BHT) and α-tocopherol. The cytotoxic activity in human cancer cell lines against colon adenocarcinoma (HCT-15), mammary adenocarcinoma (MCF-7), and lung adenocarcinoma (SKLU-1) was found comparable ((DAC)2Mg), or ca. 2-fold higher ((DAC)2Zn) than cisplatin. The acute toxicity assays indicate class 5 toxicity, according to the Organization for Economic Co-operation and Development (OECD) guidelines at doses of 3 g/kg for all complexes. No mortality or changes in the behavior of animals in any of the treated groups was observed. A therapeutic potential can be envisaged from the relevant cytotoxic activity upon human cancer cell lines in vitro and the undetected in vivo acute toxicity of these compounds.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Victor M. Lu ◽  
Toni Rose Jue ◽  
Kerrie L. McDonald

Abstract Glioblastoma (GBM) is a malignant brain tumour with a dismal prognosis, despite best treatment by surgical resection, radiation therapy (RT) and chemotherapy with temozolomide (TMZ). Nanoparticle (NP) therapy is an emerging consideration due to the ability of NPs to be formulated and cross the blood brain barrier. Lanthanum oxide (La2O3) NPs are therapeutically advantageous due to the unique chemical properties of lanthanum making it cytotoxic to cancers, and able to enhance existing anti-cancer treatments. However, La2O3 NPs have yet to be thoroughly investigated in brain tumors. We show that these NPs can reach the brain after venous injection, penetrate into GBM cells via endocytosis, dissociate to be cytotoxic, and enhance the therapeutic effects of RT and TMZ. The mechanisms of cell death by La2O3 NPs were found to be multifaceted. Increasing NP concentration was correlated to increased intrinsic and extrinsic apoptosis pathway markers in a radical oxygen species (ROS)-dependent manner, as well as involving direct DNA damage and autophagic pathways within GBM patient-derived cell lines. NP interactions to sensitize GBM to RT and TMZ were shown to involve these pathways by enhancing ROS and apoptotic mechanisms. We therefore demonstrate the therapeutic potential of La2O3 NPs to treat GBM cells in vitro, and encourage translational exploration in the future.


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