scholarly journals Composition Analysis and Anti-Cancer Properties of Two Endemic Phlomis Species (Phlomis cypria Post and Phlomis brevibracteata Turrill) from Cyprus

Proceedings ◽  
2019 ◽  
Vol 40 (1) ◽  
pp. 29
Author(s):  
Kunter ◽  
Kosar

Recently, different herbal compounds have been studied for their curative properties against Hepatocellular Carcinoma (HCC). There are over 100 Phlomis species native to the Mediterranean region, which have pharmacological activities against gastrointestinal system and liver diseases. Phlomis brevibracteata Turrill (PBT) and Phlomis cypria Post (PCP) are endemic plants of North-Cyprus belonging to the Lamiaceae family. In this study, chemical composition of the 70% methanol extracts of Phlomis species were analyzed by LC/MS/MS and antiradical activities were evaluated by DPPH● and ABTS+● radical scavenging activity tests. Anti-carcinogenic activities on HCC cell lines were investigated using MTT and wound healing assays, intercellular ROS scavenging activities were tested by DCFH-DA assay. Forsytoside B and caffeoylquinic acids were found as the main phenolic compounds which are possibly responsible for antiradical activities of the plant extracts. Significant decrease in cell viability was noticed for both extracts at concentrations over 1000 µg/mL. PBT treatment also resulted in cell motility inhibition. Additionally, both basal and induced oxidative states of all cell lines significantly were decreased by PBT. Since extracts showed cytotoxic, antioxidant and motility inhibitory activities, Phlomis species can be a good candidate for further studies with the goal of new anticancer chemotherapeutic discoveries.

2020 ◽  
Vol 20 (13) ◽  
pp. 1516-1529 ◽  
Author(s):  
Zoonish Malghani ◽  
Arif-Ullah Khan ◽  
Muhammad Faheem ◽  
Muhammad Z. Danish ◽  
Humaira Nadeem ◽  
...  

Background: Due to the pressing need and adverse effects associated with the available anti-cancer agents, an attempt was made to develop the new anti-cancer agents with better activity and lesser adverse effects. Objective: Synthetic approaches based on chemical modification of quinoline derivatives have been undertaken with the aim of improving anti-cancer agents’ safety profile. Methods: In the present study, quinoline derivatives 6-hydroxy-2-(4-methoxyphenyl) quinoline-4-carboxylic acid (M1) and 2-(4-chlorophenyl)-6-hydroxyquinoline-4-carboxylic acid (M3) were synthesized by the reaction of aldehyde and pyruvic acid. The complete reaction was indicated by thin-layer chromatography. Newly synthesized M1and M3were tested for in silico and in vitro studies. Results: M1 and M3 were docked against selected targets. Both the test compounds showed good affinity against all targets except the p300\CBP-associated factor target as there was no H-bond formed by M1. IC50 values of M1 and M3 against 1, 1-diphenyl-picrylhydrazyl free radical scavenging activity were 562 and 136.56ng/mL, respectively. In brine shrimp lethality assay, M1 and M3 showed IC50 value of 81.98 and 139.2ng/mL, respectively. IC50 values recorded for M1 and M3 in tumor inhibition activity were 129 and 219μg/mL, respectively. M1 and M3 exhibited concentration-dependent anti-cancer effects against human cell lines of hepatocellular carcinoma (HepG2) and colon cancer (HCT-116). Against HepG2 cells, M1 and M3 exhibited IC50 of 88.6 and 43.62μg/mL, respectively. M1 and M3 utilized against HCT-116 cell lines possessed IC50 values of 62.5 and 15.3μg/mL. M1 and M3 also showed an anti-leishmanial effect with IC50 values of 336.64 and 530.142μg/mL, respectively. Conclusion: From the results of pharmacological studies, we conclude that the newly synthesized compound showed enhanced anti-oxidant, anti-cancer and anti-leishmanial profile with good yield.


2021 ◽  
Vol 33 (2) ◽  
pp. 314-318
Author(s):  
DO THI VIET HUONG ◽  
PHAN MINH GIANG ◽  
DO HUY HOANG ◽  
NGUYEN ANH PHUONG ◽  
TRIEU ANH TRUNG

Plantago major L. in Vietnam was investigated for its chemical composition and also evaluated the biological activities against enzyme α- glucosidase and free radicals activities. The powder mixture of dried leave and roots of this species was extracted separately by three solvents: dichloromethane, water, water:alcohol (50:50, v:v). The chemical composition of dichloromethane extract was analyzed by GC-MS system to identify eighteen components, out of which eight biologically active compounds viz. 5-hydroxymethylfurfural, n-hecxadecanoic acid, 9,12-octadecadienoic acid (Z,Z)-methyl ester, allogibberic acid, β-tocopherol, campesterol, γ-sitosterol, lup-20(29)-en-3-ol and friedenlan-3-one were presented. The concentration of radical scavenging activity DPPH expressed by IC50 for water, water:alcohol (50:50, v:v) and dichloromethane with 208.7, 89.3 and 62.05 μg/mL, respectively. The dichloromethane, water and water:alcohol (50:50, v:v) extract of Plantago major exhibited α-glucosidase inhibitory activity with IC50 values of 116.4, 302.7, 195.9 μg/mL, respectively, which was comparable with acarbose (98.4 μg/mL). Plantago major L. in Vietnam may be effective inhibitors as the antidiabetic candidate and helpful to reduce the postprandial glucose levels.


2021 ◽  
Vol 37 (2) ◽  
pp. 499-507
Author(s):  
Amugoda Kankanamge Dona Malsha Binuwangi ◽  
Madinage Pawani Jayathri Perera ◽  
Asurumunige Anushka Gayathrie Silva ◽  
Renuka Nilmini Attanayake ◽  
Chandima Shashikala Kumari Rajapakse

This study focused on evaluation of antioxidant, α-amylase inhibitory activities and photo protective properties of peels of Nephelium lappaceum Linn. (rambutan); Malwana special. Methanolic extract of peels was sequentially partitioned in hexane, dichloromethane (DCM) and aqueous methanol. The methanol extract showed a significantly (p < 0.05) higher DPPH radical scavenging activity than that of butylated hydroxytoluene. Among the fractions, the highest total phenolic content (TPC) was found in the aqueous methanol fraction. DCM and aqueous methanol fractions were rich in flavonoids. In vitro α-amylase inhibitory activity of the aqueous methanol fraction was also significantly higher than the standard drug, acarbose. Partially purified aqueous methanol fraction of rambutan peels exhibited UV-B absorption with a moderate solar protection factor. The results revealed that the peels of Nephelium lappaceum Linn., Malwana specialcan be considered as a promising source for the development of natural antioxidant, cosmeceutical sunscreen and antidiabetic agents.


2021 ◽  
Vol 17 ◽  
Author(s):  
Rania Helmy Abd El-Hameed ◽  
Samar Said Fatahala ◽  
Amira Ibrahim Sayed

Background: Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules, they can easily interact with biomolecules of living systems. Objective: A series of substituted 2-thiobezimidazoles has been synthesized .Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell-lines. Methods: The spectral data of the synthesized compounds were characterized. Docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib were performed. Results: Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in CDK-ATP binding pocket. 3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib. Conclusion: Against all tested compounds ; two compounds 3c &3l were found active against two types of cell-lines.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Mehdi Farshad Ashraf ◽  
Maheran Abd Aziz ◽  
Johnson Stanslas ◽  
Ismanizan Ismail ◽  
Mihdzar Abdul Kadir

The present paper focused on antioxidant and cytotoxicity assessment of crude and total saponin fraction ofChlorophytum borivilianumas an important medicinal plant. In this study, three different antioxidant activities (2,2-diphenyl-1-picrylhydrazyl radical scavenging (DPPH), ferrous ion chelating (FIC), andβ-carotene bleaching (BCB) activity) of crude extract and total saponin fraction ofC. borivilianumtubers were performed. Crude extract was found to possess higher free radical scavenging activity (ascorbic acid equivalents 2578 ± 111 mg AA/100 g) and bleaching activity (IC50= 0.7 mg mL−1), while total saponin fraction displayed higher ferrous ion chelating (EC50= 1 mg mL−1). Cytotoxicity evaluation of crude extract and total saponin fraction against MCF-7, PC3, and HCT-116 cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) cell viability assay indicated a higher cytotoxicity activity of the crude extract than the total saponin fraction on all cell lines, being most effective and selective on MCF-7 human breast cancer cell line.


Medicines ◽  
2019 ◽  
Vol 6 (2) ◽  
pp. 70 ◽  
Author(s):  
Kusum Sai ◽  
Rashmi Thapa ◽  
Hari Prasad Devkota ◽  
Khem Raj Joshi

Background: More than 700 plants are reported to be used for medicinal purposes in Nepal; however, many of them are not studied for their scientific evidences. The aims of the present study were the estimation of the total phenolic and flavonoid contents, and the evaluation of the free radical scavenging and α-amylase inhibitory activities of five selected medicinal plants from western Nepal: Aeschynanthus parviflorus Wall. (Gesneriaceae), Buddleja asiatica Lour. (Loganiaceae), Carica papaya L. (Caricaceae), Drepanostachyum falcatum (Nees) Keng f. (Gramineae) and Spondias pinnata (L. f.) Kurz (Anacardiaceae). Methods: The total phenolic content (TPC) and total flavonoid content (TFC) were measured using Folin-Ciocalteu’s phenol reagent and aluminium chloride methods, respectively. A 1,1–diphenyl–2–picrylhydrazyl (DPPH) free radical scavenging assay was used to evaluate the free radical scavenging activity and an α-amylase inhibitory assay was carried out to determine the in vitro antidiabetic activity. Results: The phytochemical screening of five hydroalcoholic plant extracts revealed the presence of various secondary metabolites, including alkaloids, flavonoids, reducing sugars, saponins, terpenoids and tannins. The amounts of total phenolics and flavonoids were found to be the highest in B. asiatica leaf extract, which also showed the most potent free radical scavenging activity. Extract of C. papaya fruits showed the highest α-amylase inhibitory activity, whereas the extracts of B. asiatica leaves and S. pinnata leaves exhibited moderate activity. Conclusions: Some of the medicinal plants selected in this study showed high TPC and TFC values and potent bioactivities. These results may provide the scientific evidences of the traditional uses of these plants. However, further detailed studies on bioactive compounds isolation and identification and evaluation of in vivo pharmacological activities should be performed in future.


Author(s):  
Saira Tabassum ◽  
Muhammad Zia ◽  
Esperanza J. Carcahe de Blanco ◽  
Riffat Batool ◽  
Roohi Aslam ◽  
...  

Abstract Background Arisaema jacquemontii is traditionally used in treatment of different diseases. In this study, phytochemical, in vitro biological and chemo-preventive screening of A. jacquemontii was carried out to explore its pharmacological potential. Methods The dried tuber of A. jacquemontii was extracted in 11 organic solvent mixture of different polarity. The extracts were screened for phytochemical assays (phenolics and flavonoids), antioxidants potential (free radical scavenging activity, total antioxidant activity, reducing power), biological activities (antibacterial, antifungal, cytotoxic, antileishmanial, protein kinase inhibition), and chemopreventive activities using different cell lines through standard protocols. Results Significant amount phenolic contents were determined in EtOH and MeOH extracts (210.3 ± 3.05 and 193.2 ± 3.15 μg GAE/mg, respectively). Maximum flavonoid content was determined in MeOH extract (22.4 ± 4.04 μg QE/mg). Noteworthy, DPPH scavenging activity was also recorded for MeOH extract (87.66%) followed by MeOH+EtOAc extract (85.11%). Considerable antioxidant capacity (7.8 ± 0.12 μg AAE/mg) and reducing power (3.1 ± 0.15 μg AAE/mg) was observed in extract of MeOH. The LC50 against brine shrimp and leishmanial parasite was found 9.01 and 12.87 μg/mL for n-Hex and CHCl3 extracts, respectively. The highest zone of inhibition against Streptomyces hyphae formation (12.5 ± 1.77 mm) by n-Hex extract. Growth zone of inhibition 13.8 ± 1.08 mm was recorded for EtOAc and MeOH extracts, respectively against Micrococcus luteus while 10.0 ± 0.11 mm for MeOH extract against Aspergillus flavus. In-vitro cytotoxic assay showed that n-Hex extract had higher cytotoxicity against DU-145 prostate cancer and HL-60 cancer cell lines. NF-kB and MTP potential showed 34.01 and 44.87 μg/mL for n-Hex and CHCl3 extracts, respectively in chemo-preventive potential. Conclusion The study concludes that Arisaema jacquemontii bears significant phytochemical activity and pharmacological activities, this plant can be further explored for isolation of active component against a number of aliments.


2017 ◽  
Vol 1 (1) ◽  
pp. 9
Author(s):  
Ni Made Pitri Susanti ◽  
Ni Kadek Warditian ◽  
I Made Agus Gelgel Wirasuta

Abstract Bitter herbs (Sambiloto) have many pharmacological activities including antioxidant, antidiabetic, anticancer, antihyperlipidemic and anti-inflammation. Andrographolide is a diterpene compounds contained in bitter herbs. It is known that andrographolide compound responsible for the pharmacological activity of the bitter herbs. This study investigated DPPH free radical scavenging activity from andrographolide diterpene lactone. This study was initiated with the isolation of andrographolide compound from bitter herbs and then testing their DPPH free radical scavenging. The results suggested that andrographolide had IC50 value of 5.45 mg. This means andrographolide has 50% DPPH inhibition effect, i.e 5.45 mg.


2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Wael M. El-Sayed ◽  
Warda A. Hussin ◽  
Ahmed A. Mahmoud ◽  
Mohamed A. AlFredan

The discovery of anticancer agents paradigm has been shifted to natural resources to overcome the toxicity of many synthetic agents at early clinical stages. In the present study, the antimutagenic, anticancer, phytochemistry, and free radical scavenging activities of five extracts ofConyza trilobawere investigated. Extracts II (water : methanol), III (methylene chloride), and IV (methylene chloride : methanol) had the highest chlorophyll content and the highest superoxide scavenging, and metal chelating activities comparable to that of trolox. They also showed DPPH•scavenging activities better than that ofα-tocopherol. Virtually all extracts exerted a strong (>40% reduction) antimutagenic activity against sodium azide and benzopyrene. Extracts II, III, and IV showed a remarkable growth inhibition profile with GI50of 0.07–0.87 μg for Hepa1c1c7 and H4IIE1, A549, HT29, and PC3 cell lines and totally abated the growth of all cell lines, except for the breast cells, at 0.3–7.0 μg. The present study found a strong correlation between the chlorophyll content ofConyzaextracts and their DDPH scavenging, metal chelating, and in vitro cytotoxic and cytostatic activities most probably through triggering apoptosis. This study could offer a platform for future studies and help selecting the vital features that identify the extract with potential anticancer activities.


Author(s):  
Taanya Imtiaz ◽  
R. Priyadharshini ◽  
S. Rajeshkumar ◽  
Palati Sinduja

Background: Piper longum, a traditional plant used for regenerative medicine commonly known as the long pepper, is used to treat many pathological conditions. Piper longum is used as a source for obtaining the production of various nanoparticles and testing their efficacy. Piper longum has many beneficial activities, such as antifungal, anti-amoebic, anti-asthmatic, anti-cancer, anti-oxidant, anti-inflammatory, antidepressants activities. Silver nanoparticles are widely and commonly used for its antimicrobial activity against various microorganisms. Our study aimed to synthesize Piper longum based silver nanoparticles and to investigate its anti-oxidant property. Materials and Methods: Piper longum plant extract was prepared and silver nanoparticles extract was synthesized. DPPH assay was then performed to assess the free radical scavenging activity of the Piper longum silver nanoparticle extract. The further analysis was that the formation of brownish-red color observed was evident, resulting in thesynthesization of silver nanoparticles. Results: Brown discolouration represents formation of silver nanoparticles and the antioxidant activity was noted to be from 60% to 70% from 10 to 50μL. But when compared to standard vitamin C values the Piper longum silver nanoparticles showed less antioxidant activity. Conclusion: The Piper longum mediated silver nanoparticles showed remarkable and considerable antioxidant activity but when compared with the standard sample values the antioxidant activity was low.


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