scholarly journals Molecular Networking-Guided Isolation of New Etzionin-Type Diketopiperazine Hydroxamates from the Persian Gulf Sponge Cliona celata

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 439
Author(s):  
Reza Mohsenian Kouchaksaraee ◽  
Fengjie Li ◽  
Melika Nazemi ◽  
Mahdi Moridi Farimani ◽  
Deniz Tasdemir
Keyword(s):  
Persian Gulf ◽  
Chemical Constituents ◽  
Chemical Characterization ◽  
Marine Sponges ◽  
Anticancer Activities ◽  
2D Nmr Spectroscopy ◽  
Molecular Networking ◽  
Cliona Celata ◽  
The Persian Gulf

The Persian Gulf is a unique and biologically diverse marine environment dominated by invertebrates. In continuation of our research interest in the chemistry and biological activity of marine sponges from the Persian Gulf, we selected the excavating sponge Cliona celata for detailed metabolome analyses, in vitro bioactivity screening, and chemical isolation studies. A UPLC-MS/MS (MS2) molecular-networking-based dereplication strategy allowed annotation and structural prediction of various diketopiperazines (DKPs) and etzionin-type diketopiperazine hydroxamates (DKPHs) in the crude sponge extract. The molecular-networking-guided isolation approach applied to the crude extract afforded the DKPH etzionin (1) and its two new derivatives, clioetzionin A (2) and clioetzionin B (3). Another new modified DKP (4) was identified by MS/MS analyses but could not be isolated in sufficient quantities to confirm its structure. The chemical characterization of the purified DKPHs 1–3 was performed by a combination of 1D and 2D NMR spectroscopy, HRMS, HRMS/MS, and [α]D analyses. Compounds 1 and 2 exhibited broad antibacterial, antifungal, and anticancer activities, with IC50 values ranging from 19.6 to 159.1 µM. This is the first study investigating the chemical constituents of a C. celata specimen from the Persian Gulf. It is also the first report of full spectroscopic data of etzionin based on extensive spectroscopic analyses.

scholarly journals Chemical Characterization and Antidiabetic Activity of Essential Oils from Pelargonium graveolens Leaves

2021 ◽  
Vol 9 (1) ◽  
pp. 109-113
Author(s):  
Javed Ahamad ◽  
Subasini Uthirapathy
Keyword(s):  
Essential Oil ◽  
Essential Oils ◽  
Chemical Constituents ◽  
Chemical Characterization ◽  
Study Finding ◽  
Antidiabetic Activity ◽  
Chemical Components ◽  
Diabetic Patients ◽  
Pelargonium Graveolens

Pelargonium graveolens (Geranium) is a source of the finest quality of fragrance and its essential oils are used as antibacterial, and antifungal agents. The aim of the current research is to determine chemical constituents in the essential oil of P. graveolens by GC-MS and evaluate its antidiabetic activity via α-glucosidase inhibition assay. The chemical composition of P. graveolens essential oil was determined by GC/MS and its antidiabetic activity was assessed through inhibition of α-glucosidase enzyme in in-vitro models. GC-MS analysis determines 36 chemical components in the essential oil of P. graveolens leaves, and citronellyl isovalerate (10.41 %), menthol (9.61 %), linalool (8.63 %), p-menthone (6.31 %), and geranyl tiglate (4.99 %) were recorded as major constituents. The essential oil of P. graveolens leaves showed concentration dependant inhibition of α-glucosidase enzyme ranging from 28.13±1.41 to 74.24±2.53 µg/mL for concentration ranging from 31.25 to 1000 µg/mL. The IC50 values for of P. graveolens and acarbose were found as 93.72±4.76 and 80.4±2.17 µg/mL, respectively against the α-glucosidase enzyme. The study finding explores the chemical components of P. graveolens growing in the Iraqi Kurdistan region and scientifically supported its possible use in diabetic patients for controlling postprandial hyperglycemia.

scholarly journals Phosphodiesterase-1 Inhibitory Activity of Two Flavonoids Isolated fromPistacia integerrimaJ. L. Stewart Galls

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Abdur Rauf ◽  
Muhammad Saleem ◽  
Ghias Uddin ◽  
Bina S. Siddiqui ◽  
Haroon Khan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
In Silico ◽  
Molecular Mechanisms ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Folk Medicine ◽  
Chemical Characterization ◽  
Active Constituents ◽  
Isolation And Characterization

Pistacia integerrimais one of twenty species among the genusPistacia. Long horn-shaped galls that develop on this plant are harvested and used in Ayurveda and Indian traditional medicine to make “karkatshringi”, a herbal medicine used for the treatment of asthma and different disorders of respiratory tract. However, until now, the molecular mechanisms of action of “karkatshringi” and its chemical characterization are partially known. This study deals with the isolation and characterization of the active constituents from the methanolic extract ofP. integerrimagalls and it was also oriented to evaluatein vitroandin silicotheir potential enzymatic inhibitory activity against phosphodiesterase-1 (PDE1), a well-known enzyme involved in airway smooth muscle activity and airway inflammation. Our results showed that the methanolic extract ofP. integerrimagalls and some of its active constituents [naringenin (1) and 3,5,7,4′-tetrahydroxy-flavanone (2)] are ablein vitroto inhibit PDE1 activity (59.20 ± 4.95%, 75.90 ± 5.90%, and 65.25 ± 5.25%, resp.) and demonstratein silicoan interesting interaction with this enzymatic site. Taken together, our results add new knowledge of chemical constituents responsible for the biological activity ofP. integerrimaand contextually legitimate the use of this plant in folk medicine.

scholarly journals First Molecular Identification of Symbiotic Archaea in a Sponge Collected from the Persian Gulf, Iran

2018 ◽  
Vol 12 (1) ◽  
pp. 323-332
Author(s):  
Akram Najafi ◽  
Maryam Moradinasab ◽  
Mohammad Seyedabadi ◽  
Mohammad A. Haghighi ◽  
Iraj Nabipour
Keyword(s):  
16S Rrna ◽  
Persian Gulf ◽  
Molecular Taxonomy ◽  
Marine Sponges ◽  
Molecular Techniques ◽  
Sponge Species ◽  
Ammonium Bromide ◽  
Pcr Cloning ◽  
The Persian Gulf ◽  
Uncultured Archaea

Background: Marine sponges are associated with numerically vast and phylogenetically diverse microbial communities at different geographical locations. However, little is known about the archaeal diversity of sponges in the Persian Gulf. The present study was aimed to identify the symbiotic archaea with a sponge species gathered from the Persian Gulf, Iran. Methods: Sponge sample was collected from a depth of 3 m offshore Bushehr, Persian Gulf, Iran. Metagenomic DNA was extracted using a hexadecyl trimethyl ammonium bromide (CTAB) method. The COI mtDNA marker was used for molecular taxonomy identification of sponge sample. Also, symbiotic archaea were identified using the culture-independent analysis of the 16S rRNA gene and PCR- cloning. Results: In this study, analysis of multilocus DNA marker and morphological characteristics revealed that the sponge species belonged to Chondrilla australiensis isolate PG_BU4. PCR cloning and sequencing showed that all of the sequences of archaeal 16S rRNA gene libraries clustered into the uncultured archaeal group. Conclusion: The present study is the first report of the presence of the genus of Chondrilla in the Persian Gulf. Traditional taxonomy methods, when used along with molecular techniques, could play a significant role in the accurate taxonomy of sponges. Also, the uncultured archaea may promise a potential source for bioactive compounds. Further functional studies are needed to explore the role of the sponge-associated uncultured archaea as a part of the marine symbiosis.

scholarly journals SCREENING OF BIOACTIVE COMPONENTS BY GC-MS ANALYSIS AND THE STUDY ON IN VITRO ANTICANCER EFFICACY OF MICROPORUS AFFINIS (BLUME & T. NEES) KUNT.

2020 ◽  
Vol 11 (12) ◽  
pp. 31-34
Author(s):  
S Aneesh ◽  
J E Thoppil
Keyword(s):  
Biological Sciences ◽  
Bioactive Compounds ◽  
Chemical Characterization ◽  
Bioactive Components ◽  
Anticancer Activities ◽  
Anticancer Efficacy ◽  
Ms Analysis ◽  
Ethidium Bromide Staining ◽  
Leading Compounds

Natural compounds with biological activity are normally present in plants, mushrooms and their natural sources. Applied mycology is one of the most stimulating and rapidly evolving areas of the biological sciences. Hence the present study focussed on exploring Microporus affinis (Blume & T. Nees) Kunt., the least explored and edible bracket fungus. Chemical characterization by GC-MS analysis resulted in the presence of 47 bioactive compounds. 9, 12- Octadecadienoic acid (Z,Z)- methyl ester, Ergosterol, Monolinolein, Thiacremonone, Stellasterol, n- Hexadecanoic acid, Ribitol, Maltol etc., were the leading compounds. Because of the presence of various bioactive compounds which have been already reported to possess antitumor, antioxidant and anticancer activities, M. affinis extract has been tested for in vitro anticancer efficacy on DLD1 cell lines (cultured in DMEM medium) using MTT assay. It resulted in the decrease of percentage of viability as the increase in concentration of the extract. Apoptosis was determined by using Acridine orange and Ethidium bromide staining. Thus, the taxa, M. affinis can be recommended for further anticancer assays for validation.

scholarly journals Antiproliferative Activity and Apoptotic Efficiency of Syzygium cumini Bark Methanolic Extract against EAC Cells In Vivo

2020 ◽  
Vol 20 ◽  
Author(s):  
Mst. Ayesha Siddika ◽  
Plabon K. Das ◽  
Saharia Y. Asha ◽  
Suraiya Aktar ◽  
Abu Rahyan M. Tareq ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Antiproliferative Activity ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Antioxidant Properties ◽  
In Vitro Assays ◽  
Syzygium Cumini ◽  
Anticancer Activities ◽  
Eac Cells

Background: Syzygium cumini, one of the evidence-based traditional medicinal plant used in the treatment of various ailments. Objectives: Herein, the antioxidant property and anticancer property of Syzygium cumini against Ehrlich Ascites Carcinoma (EAC) were examined in search of effective chemotherapeutics. Methods: In vitro assays, phytochemical and chromatographic analysis were used to determine antioxidant properties and chemical constituents of Syzygium cummini bark methanolic extract (SCBME). Functional assays were used to measure the anticancer activity of SCBME. Fluorescence microscopy and RT-PCR were used to examine morphological and molecular changes of EAC cells followed by SCBME treatment. Results: Phytochemical and GC–MS analysis confirmed the presence of compounds with antioxidant and anticancer activities. Accordingly, we have noted a strong antioxidant activity of SCBME with an IC50 value of 10μg/ml. Importantly, SCBME exerted a dose-dependent anticancer activity with significant inhibition of EAC cell growth (71.08 ± 3.53%; p<0.001), reduction of tumour burden (69.50%; p<0.01) and increase of life span (73.13%; p<0.001) of EACbearing mice at 75mg/kg/day. Besides, SCBME restored the blood toxicity towards normal in EAC-bearing mice (p<0.05). SCBME treated EAC cells showed apoptotic features under a fluorescence microscope and fragment DNA in DNA laddering assay. Moreover, up-regulation of the tumour suppressor p53 and pro-apoptotic Bax and down-regulation of NF-κB and anti-apoptotic Bcl-2 genes, implied induction of apoptosis followed by SCBME treatment. Conclusion: The antiproliferative activity of SCBME against EAC cells is likely due to apoptosis, mediated by regulation of p53 and NF-κB signalling. Thus, SCBME can be considered as a useful resource in cancer chemotherapy.

scholarly journals Antiparasitic and Anticancer Carvotacetone Derivatives of Sphaeranthus bullatus

2012 ◽  
Vol 7 (9) ◽  
pp. 1934578X1200700
Author(s):  
Francis Machumi ◽  
Abiy Yenesew ◽  
Jacob O. Midiwo ◽  
Matthias Heydenreich ◽  
Erich Kleinpeter ◽  
...  
Keyword(s):  
2D Nmr ◽  
Specific Rotation ◽  
Anticancer Activities ◽  
2D Nmr Spectroscopy ◽  
Cytotoxic Effects ◽  
H Nmr ◽  
Aerial Parts ◽  
Annual Herb ◽  
Derivatives Of

The CH2Cl2-MeOH (1:1) extract of the aerial parts of Sphaeranthus bullatus, an annual herb native to tropical East Africa, showed activity against chloroquine sensitive D6 (IC50 9.7 μg/mL) and chloroquine resistant W2 (IC50 15.0 μg/mL) strains of Plasmodium falciparum. Seventeen secondary metabolites were isolated from the extract through conventional chromatographic techniques and identified using various spectroscopic methods. The compounds were evaluated for their in vitro antiplasmodial, antileishmanial and anticancer activities revealing activity of four carvotacetone derivatives, namely 3-acetoxy-7-hydroxy-5-tigloyloxycarvotacetone (1), 3,7-dihydroxy-5-tigloyloxycarvotacetone (2), 3-acetoxy-5,7-dihydroxycarvotacetone (3) and 3,5,7-trihydroxy-carvotacetone (4); with antiplasmodial IC50 values of 1.40, 0.79, 0.60 and 3.40 μg/mL, respectively, against chloroquine sensitive D6 strains of P. falciparum; antiplasmodial activity of IC50 2.00, 0.90, 0.68 and 2.80 μg/mL, respectively, against chloroquine resistant W2 strains of P. falciparum; antileishmanial IC50 values of 0.70, 3.00, 0.70 and 17.00 μg/mL, respectively, against the parasite L. donovanii promastigotes, and anticancer activity against human SK-MEL, KB, BT-549 and SK-OV-3 tumor cells, with IC50 values between <1.1 - 5.3 μg/mL for 1-3. In addition, cytotoxic effects of the active compounds were evaluated against monkey kidney fibroblasts (VERO) and pig kidney epithelial cells (LLC-PK11). The structures of carvotacetone derivatives were determined by 1D and 2D NMR spectroscopy; the absolute stereochemical configuration of 3-acetoxy-7-hydroxy-5-tigloyloxycarvotacetone (1) was determined as 3 R, 4 R, 5 S by circular dichroism, specific rotation, 1H NMR and 2D NMR ROESY and NOESY experiments.

scholarly journals A Review of the Ethnomedicinal Uses, Biological Activities, and Triterpenoids of Euphorbia Species

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 4019
Author(s):  
Douglas Kemboi ◽  
Xolani Peter ◽  
Moses Langat ◽  
Jacqueline Tembu
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Structural Diversity ◽  
Pharmacological Properties ◽  
Anticancer Activities ◽  
Sensory Disorders ◽  
Wide Range ◽  
Ethnomedicinal Uses

The genus Euphorbia is one of the largest genera in the spurge family, with diversity in range, distribution, and morphology. The plant species in this genus are widely used in traditional medicine for the treatment of diseases, ranging from respirational infections, body and skin irritations, digestion complaints, inflammatory infections, body pain, microbial illness, snake or scorpion bites, pregnancy, as well as sensory disorders. Their successes have been attributed to the presence of diverse phytochemicals like polycyclic and macrocyclic diterpenes with various pharmacological properties. As a result, Euphorbia diterpenes are of interest to chemists and biochemists with regard to drug discovery from natural products due to their diverse therapeutic applications as well as their great structural diversity. Other chemical constituents such as triterpenoids have also been reported to possess various pharmacological properties, thus supporting the traditional uses of the Euphorbia species. These triterpenoids can provide potential leads that can be developed into pharmaceutical compounds for a wide range of medicinal applications. However, there are scattered scientific reports about the anticancer activities of these constituents. Harnessing such information could provide a database of bioactive pharmacopeia or targeted scaffolds for drug discovery. Therefore, this review presents an updated and comprehensive summary of the ethnomedicinal uses, phytochemistry, and the anticancer activities of the triterpenoids of Euphorbia species. Most of the reported triterpenoids in this review belong to tirucallane, cycloartanes, lupane, oleanane, ursane, and taraxane subclass. Their anticancer activities varied distinctly with the majority of them exhibiting significant cytotoxic and anticancer activities in vitro. It is, therefore, envisaged that the report on Euphorbia triterpenoids with interesting anticancer activities will form a database of potential leads or scaffolds that could be advanced into the clinical trials with regard to drug discovery.

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