Bis (Isothiocyanatomethyl) Benzene, A Plant Derived Anti-Neoplastic Compound: Purified from Moringa Oleifera Leaf Extract

2019 ◽  
Vol 19 (5) ◽  
pp. 677-686 ◽  
Author(s):  
Samrat Paul ◽  
Piyali Basak ◽  
Namrata Maity ◽  
Chayan Guha ◽  
Nandan Kumar Jana
Keyword(s):  
Anticancer Activity ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Folk Medicine ◽  
Drug Formulation ◽  
Indigenous Species ◽  
Cancer Cell Growth ◽  
Apoptotic Pathway ◽  
Dimeric Form ◽  
Mcf 7

Background: Moringa oleifera lam, commonly known as “Sajina”, is an indigenous species to India. In our folk medicine, it is used for the treatment of Canker (cancer). The Moringa oleifera leaf extract contains many phyto-compounds, with some being anti-neoplastic in nature. Objective: Our preliminary study showed that the leaf extract significantly kills cancer cells compared to normal cells. On searching for the new phyto-compound, Bis-isothiocyanatomethyl) benzene was purified and isolated. Methods: The sequential process of fractional distillation, column chromatography, followed by TLC and HPLC is performed for purification. Every fraction from each step was tested on HeLa cell line for evaluating the presence of the phyto-compound. Results and Conclusion: FTIR peak analysis of a single phyto-compound shows the presence of thiocyanate group, aromatic carbon group. 1H & 13C NMR peak analysis along with High-resolution mass spectroscopy (HRMS) calculation confirm the chemical structure with IUPAC name [Bis (Isothiocyanatomethyl) benzene]. Previously, Isothiocyanatomethyl- benzene solely or in conjugation with sugar molecule has been reported, but its dimeric form in nature hasnot yet been published anywhere. It shows anticancer activity by retarding cancer cell growth & inhibits carcinogenesis on HeLa, MCF-7, and MDA-MB-231 cell lines by caspase 3 apoptotic pathway and showed comparatively less cytotoxicity to PBMC cell. It shows anticancer activity almost the same as the market available drug Cis-Platin. Therefore, further extrapolating its activity with different concentrations may result in its use as a drug formulation for the treatment of cancer.

7-hydroxyfrullanolide, isolated from Sphaeranthus indicus, inhibits colorectal cancer cell growth by p53-dependent and -independent mechanism

2018 ◽  
Vol 40 (6) ◽  
pp. 791-804
Author(s):  
Praveen Pandey ◽  
Deepika Singh ◽  
Mohammad Hasanain ◽  
Raghib Ashraf ◽  
Mayank Maheshwari ◽  
...  
Keyword(s):  
Cell Growth ◽  
Anticancer Activity ◽  
Cancer Cell ◽  
Molecular Mechanisms ◽  
Target Genes ◽  
Cancer Cell Growth ◽  
Apoptotic Pathway ◽  
Syngeneic Mouse Model ◽  
Sphaeranthus Indicus

Abstract Sphaeranthus indicus Linn. is commonly used in Indian traditional medicine for management of multiple pathological conditions. However, there are limited studies on anticancer activity of this plant and its underlying molecular mechanisms. Here, we isolated an active constituent, 7-hydroxyfrullanolide (7-HF), from the flowers of this plant, which showed promising chemotherapeutic potential. The compound was more effective in inhibiting in vitro proliferation of colon cancers cells through G2/M phase arrest than other cancer cell lines that were used in this study. Consistent with in vitro data, 7-HF caused substantial regression of tumour volume in a syngeneic mouse model of colon cancer. The molecule triggered extrinsic apoptotic pathway, which was evident as upregulation of DR4 and DR5 expression as well as induction of their downstream effector molecules (FADD, Caspase-8). Concurrent activation of intrinsic pathway was demonstrated with loss of ΔΨm to release pro-apoptotic cytochrome c from mitochondria and activation of downstream caspase cascades (Caspase -9, -3). Loss of p53 resulted in decreased sensitivity of cells towards pro-apoptotic effect of 7-HF with increased number of viable cells indicating p53-dependent arrest of cancer cell growth. This notion was further supported with 7-HF-mediated elevation of endogenous p53 level, decreased expression of MDM2 and transcriptional upregulation of p53 target genes in apoptotic pathway. However, 7-HF was equally effective in preventing progression of HCT116 p53+/+ and p53−/− cell derived xenografts in nude mice, which suggests that differences in p53 status may not influence its in vivo efficacy. Taken together, our results support 7-HF as a potential chemotherapeutic agent and provided a new mechanistic insight into its anticancer activity.

scholarly journals The Immuno-modulatory and Thrombocytopaenic Effects of the Varying Concentrations of the Aqueous Leaf Extract of Moringa Oleifera in Male Albino Wistar Rats

2019 ◽  
pp. 1-8
Author(s):  
Ojeka Sunday Ogbu ◽  
Zabbey Victor Zigabelbari
Keyword(s):  
Wistar Rats ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Folk Medicine ◽  
Control Group ◽  
Distribution Width ◽  
Treatment Groups ◽  
Immature Platelet Fraction ◽  
Group A ◽  
Aqueous Leaf Extract

Introduction: Moringa oleifera and related species are commonly used in folk medicine for various human diseases. Aim: The study was undertaken to establish the thrombocytopenic effect of the aqueous leaf extract of moringa oleifera and to find the utilization of platelet parameters in determining the cause of the thrombocytopenia. Methodology: Fresh leaves of moringa were dried and extracted with water. Thirty (30) male albino Wistar rats, weighing between 150-250 g, which were kept under uniform laboratory conditions, were randomly divided into five (5) groups (A-E), based on their weights. The control group (group A) was orally given 0.5 ml of distilled water while the treatment groups (groups B to E) were orally given 250 mg/kg, 450 mg/kg,650 mg/kg and 850 mg/kg body weight respectively of the extract, once a day, for 56days and then sacrificed. At the end of the administration, blood samples were collected from each rat and examined for platelet indices. The effects of treatment with aqueous leaf extract of moringa oleifera on the platelet parameters were compared with the control group. Result: The rats treated with the extract, showed a decrease in platelet count and platelet crit while there was a significant increase in the platelet distribution width, mean platelet volume and immature platelet fraction, concerning the control. Conclusion: The aqueous leaf extract of moringa oleifera is therefore shown to modulate the immune system and cause thrombocytopaenia, through platelet destruction.

scholarly journals Antioxidant and Anticancer Potential of Methanolic Leaf Extract of Moringa concanensis Nimmo Against Human Breast Cancer Cell Line MCF-7

2017 ◽  
Vol 9 (6) ◽  
Author(s):  
S. Vijayakumar ◽  
V. Bhuvaneshwari ◽  
A. Sumathi
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Cell Line ◽  
Leaf Extract ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Cancer Cell Line ◽  
Plant Sample ◽  
Crude Leaf Extract ◽  
Mcf 7

Breast cancer is one of the major health problems among women in both developed and developing countries. The objective of the present investigation is focused on the DPPH Radical Scavenging Activity and anticancer effect of the methanolic extract of Moringa concanensis Nimmo leaves against Breast cancer (MCF-7) cell line. The study was facilitated by collecting the plant sample and subjected to crude extraction. The anticancer activity of the crude methanolic leaf extract of M. concanensis against MCF- 7 cell line was examined by MTT assay. The present study confirms that the crude leaf extract of M. concanensis has potential anticancer activity against MCF- 7 cell lines while compared to the control. M. concanensis leaves possess remarkable anticancer property which may lead to development of novel compounds as natural phytomedicine.

Development of Ultrasensitive and Arsenic (III) Selective Upconverting (NaYF4: Yb3+, Er3+) Platform

2020 ◽  
Author(s):  
Suman Duhan ◽  
Kedar Sahoo ◽  
Sudhir Kumar Singh ◽  
Manoj Kumar
Keyword(s):  
Heavy Ions ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Solid Phase ◽  
Selective Detection ◽  
Arsenic Pollution ◽  
Apparent Effect ◽  
Safe Limit ◽  
Interfering Ions ◽  
Resonance Transfer

The development of a sensitive alpha-NaYF4:Yb3+, Er3+ solid-phase upconverting platform (UCP) has been realized using Moringa oleifera leaf extract for selective detection of arsenic (As III) contamination in drinking water. The presence of polyphenols in the leaves extract is shown to induce luminescence resonance transfer (LRET), diminishing thereby the Er3+ upconverting red and green emissions activated by 980 nm excitation. However, addition of As3+ species interrupts the LRET process and restores emission proportionately. This feature allows platform to selectively detect arsenic pollution in water below the safe limit of 10 ppt. The uniqueness of UCP lies in monitoring the As3+ contamination in samples containing heavy ions (Cd2+, Hg2+) as well, without apparent effect on the signal reproducibility. UCP is also found to be insensitive to other interfering ions like Pb2+, H2PO4-, F-, Cl-, Ca2+, Mg2+, Sn2+, Cr6+, Fe2+ and Co2+, if present.<br><br>

Novel 1,2,3-Triazole-functionalized pyrido[3',2':4,5]furo[3,2-d]pyrimidin- 4(3H)-one Derivatives: Synthesis, Anticancer Activity, CoMFA and CoMSIA Studies

2020 ◽  
Vol 17 (12) ◽  
pp. 969-978
Author(s):  
Balakishan Vadla ◽  
Sailu Betala
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Normal Cell ◽  
Rational Design ◽  
Human Cancer ◽  
Strong Basis ◽  
Hek 293 ◽  
Normal Cell Line ◽  
Human Cancer Cell Lines ◽  
Mcf 7

A series of novel triazole functionalized pyrido [3',2':4,5] furo[3,2-d] pyrimidin-4 (3H)-one derivatives 7a-p were prepared from ethyl furo[2,3-b]pyridine-2-carboxylate 3 on reaction with ammonia to afford furo[2,3-b]pyridine-2-carboxamide 4. This compound, on reaction with triethyl orthoformate TEOF, gave compound 5. Compound 5 on propargylation, followed by a reaction with substituted aryl azides under Sharpless reaction conditions, furnished triazole tagged pyrido [3',2':4,5]furo[3,2-d] pyrimidin-4(3H)-one derivatives. All the products 7a-p were screened against four human cancer cell lines, such as HeLa - Cervical cancer (CCL-2), COLO 205- Colon cancer (CCL-222), HepG2- Liver cancer (HB-8065), and MCF7 - Breast cancer (HTB-22) and one normal cell line (HEK 293). Compounds 7b, 7n, 7o and 7p, which showed promising anticancer activity, were identified and found to be non-toxic to normal cell line. Studies for HeLa, COLO205, HepG2, and MCF-7 using CoMFA and CoMSIA were carried out . Models from 3D-QSAR provided a strong basis for future rational design of more active and selective HeLa, COLO205, HepG2, and MCF-7 cell line inhibitors.

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

2020 ◽  
Vol 17 (5) ◽  
pp. 563-573 ◽  
Author(s):  
Chandrakant Dhondiram Pawar ◽  
Dattatraya Navnath Pansare ◽  
Devanand Baburao Shinde
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Proliferative Activity ◽  
Thiophene Ring ◽  
Amide Group ◽  
Peptide Coupling ◽  
Ic50 Value ◽  
Important Building Block ◽  
Mcf 7

Background: Thiophene ring forms important building block in medicinal chemistry. Literature reveals that thiophene ring in combination with different groups shows different activity. By keeping these things in mind we have designed and synthesized a new series of amide and sulfonamide coupled thiophene. A series of novel substituted 3-sulfamoylbenzo[b]thiophene-4- carboxamide molecules containing sulfonamide and amide group were designed, synthesized and used for anti-proliferative activity study. Methods: The final compounds 16-36 were synthesized by using series of reactions comprising sulfonation, sulfonamide coupling, hydrolysis and peptide coupling. The yields of compounds 16- 36 are in the range of 90-98%. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, 13C NMR, LCMS and the purity was checked through HPLC analysis. The compounds were further tested for their in vitro anticancer activity against a series of cell lines A549, HeLa, MCF-7 and Du-145. Results: The intermediates 8-13, 15 and final compounds 16-36 were synthesized in good yields. The synthesized compounds were further tested for their anticancer activity and most of compounds showed moderate to good anticancer activity against all four cell lines. Conclusion: We have synthesized 21 compounds and were screened for anticancer activity against MCF-7, HeLa, A-549 and Du-145 cancer cell lines. Most of the compounds were active for tested cell lines with IC50 value in the range of 1.81 to 9.73 μM. The compounds 18, 19, 21, 25, 30, 31 and 33 are most active in cell line data with IC50 value in the range of 1.81 to 2.52 μM.

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