@article {2169, title = {Novel Coumarin-Indole Hybrids as Cytotoxic Candidates: Synthesis and Antiproliferative Activity}, journal = {Pharmacognosy Journal}, volume = {15}, year = {2023}, month = {December 2023}, pages = {1105-1111}, type = {Research Article}, chapter = {1105}, abstract = {

Cancer is regarded as a nightmare for humanity and a challenging task for medical professionals. Twelve hydrides (2a-2l), made of trifunctionalized coumarin and various substituted indoles, were created in an effort to realize the hope of a cancer cure. The 4,5-dimethoxysalicylaldehyde and ethyl acetoacetate were combined in a Knoevenagel reaction to create the coumarin component. The construction of the indole component involved converting various aminoindoles through diazotization and Sandmeyer reactions to twelve substituted indoles (1a-1l). These two components were combined through a Michael addition reaction to create the desired hybrids. Investigating their spectra released from various spectroscopical instruments allowed researchers to determine the 2D molecular frameworks of these hybrids. Studying the survival of nine tumor cell types after treatment with the synthesized hybrids enabled researchers to estimate there in vitro impact as cytotoxic candidates. By checking the cell viability using an MTT marker, it was possible to see that this effect was antiproliferative. The cytotoxicity measurements, IC50 scores, revealed a number of intriguing facts. To start, the synthetic hybrids displayed a relatively similar cytotoxic pattern against the cancerous cell lines under investigation. Second, compared to hybrids with chloride, hydroxyl, or methoxy substituents, fluorinated hybrids are more toxic to cancerous cells. Finally, hybrids with indole substituted at position-6 (2i-2l) have the highest cytotoxicity among those with indole functionalized at position-4 (2a-2d) or position-5 (2e-2h). From these facts, the authors concluded that hybrids with indole substituted at position-4 can represent potential candidates as antiproliferative applicants. Moreover, hybrid 2i may serve as a valuable model for creating potent anti-breast cancer therapies.

}, keywords = {Anti-breast cancer, Coumarin, Cytotoxicity, Indole, Michael addition, MTT}, doi = {10.5530/pj.2023.15.201}, author = {Sarah S. Ismael and Noor Ahmed M. Waheed and Seema Mahmood Kasim and Yasser Fakri Mustafa} } @article {1341, title = {Determination of Lupeol, a Cytotoxic Compound Against SW620 Cells in the Extracts of Ha-Rak Recipe}, journal = {Pharmacognosy Journal}, volume = {13}, year = {2021}, month = {January 2021}, pages = {133-138}, type = {Research Article}, chapter = {133}, abstract = {

Introduction: Ha-Rak is an herbal recipe that has been stated by Ministry of Public Health, Thailand to utilize as the herbal medicines for the treatment of fever. The recipe comprises the roots of five plants including Capparis micracantha, Clerodendrum indicum, Ficus racemosa, Harrisonia perforata and Tiliacora triandra as its ingredients. Methods: The extracts of Ha-Rak and its five herbal principles were evaluated for their potential on the cytotoxicity against SW620 cancer cell lines using the MTT assay and an active compound, lupeol which was found as a cytotoxic compound in the herbal ingredients of Ha-Rak was further determined. A chromatographic method for investigating that compound in the extracts was developed herein. The analytical method comprised a cholesterol-coated C18 column, a mixture of acetonitrile and methanol (70:30) with a flow rate of 2 mL/min, and a diode-array UV wavelength at 210 nm as a stationary phase, mobile phase, and detector, respectively. Results: The amount of lupeol in the extracts of Ha-Rak and the herbal principles, which possessed cytotoxicity against SW620 cell lines with the IC50 values of 30.10-212.24 μg/mL displayed variously in the range of 4.50-250.62 mg/100g. The difference of the contents among the extracts was noted significantly (P \< 0.05). The correlation between the lupeol contents and their cytotoxic performances on the tested cell lines was observed in our investigation. Conclusion: Our findings demonstrated that Ha-Rak recipe contains a promising cytotoxic compound, lupeol and it will support the recipe to subject further pharmacological studies on anticancer activity.

}, keywords = {Benchalokawichian, Cancer Cell Lines, Cytotoxicity, Ha-Rak, Lupeol, MTT}, doi = {10.5530/pj.2021.13.18}, author = {Pathom Somwong and Chomnapas Chuchote} } @article {1249, title = {The Effect of Carthamus tenuis Extracts on the Cell Proliferation of Different Tumor Cell Lines}, journal = {Pharmacognosy Journal}, volume = {12}, year = {2020}, month = {September 2020}, pages = {1332-1339}, type = {Research Article}, chapter = {1332}, abstract = {

Background: Carthamus tenuis is one of the medicinal plants that was used traditionally to treat skin diseases, hemorrhoids, abortion, infertility. It also showed an immunosuppressive role as well as antifungal, antibacterial, anti-inflammatory activity. Although this plant is widespread, there are few studies about its medical applications. Objectives: This study was done to explore the anticancer activity of this plant. Materials and Methods: The aerial parts of the plant were dried, grinded and extracted with hexane, ethyl acetate, and methanol. The extracts were applied in different concentrations to cell cultures of breast (MCF-7), colon (HT-29), prostate (PC-3) and colorectal (CaCo-2) cell lines and fibroblast (MRC- 5) was used as a control. The anticancer activity was evaluated by 3-(4,5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium (MTT) reduction assay that was measured by spectrophotometer. Results: The results showed that methanol extract significantly (p\<0.05) have the highest inhibitory activity on MCF-7, HT-29, PC-3, and CaCo-2 with IC50; (25.52 μg/ml), (17.37 μg/ml), (25.77 μg/ml), (24.49 μg/ml), respectively. Followed by ethyl acetate extract that moderately inhibit cell growth of PC-3 and CaCo-2 with IC50; (28.99 μg/ml) and (21.45 μg/ml), respectively. n-hexane extract showed no significant inhibitory effect on all cell lines; IC50 (125.52 -152.34 μg/ml) when compared to Tamoxifen drug activity as a positive control. Conclusion: Results of this study showed the anticancer activity of the plant extracts in four different kinds of cancers that need further study.

}, keywords = {Anticancer, Carthamus tenuis, IC50, Methanolic extract, MTT}, doi = {10.5530/pj.2020.12.183}, author = {Maissa{\textquoteright} Taleb Shawagfeh} } @article {854, title = {Assessment of Phyto-Constituents by GC-MS and Anti-Tumour Activity of Garlic Grown in Different Altitude: A Comparative Study}, journal = {Pharmacognosy Journal}, volume = {11}, year = {2019}, month = {February 2019}, pages = {350-354}, type = {Original Article}, chapter = {350}, abstract = {

Background: Garlic (Allium sativum L.) is most important spice containing highest sources of total phenolic compounds. It has been used as a component of traditional and modern medicine. Pharmacological properties of garlic is mainly depend on its phyto-constituents content, which varies between geographical regions. The aim of this study was to evaluate and compare the phyto-constituents content of garlic sample collected from high ranges of Idukki (Kanthallur) with that of Tamil Nadu (Mettupalayam market) garlic sample. Materials and Methods: garlic clove sample were collected from high ranges of kanthallur region (GSK) and Mettupalayam region (GSM). The garlic oil was extracted from the collected garlic sample by solvent extraction method. The phytochemical study of extracted garlic oil were conducted using standard methods of analysis and subjected GC-MS analysis. Further, the extracted oil samples were studied for their anti-tumour activity against Dalton Lymphoma Cell Lines (DLA) in an in vitro model. Results: The obtained results revealed that garlic oil of GSK showed highest percentage of yield of oil (1.1\%) than garlic oil of GSM (0.6\%). The phytochemical screening of GSK indicated the presence of alkaloids and flavonoid, whereas GSM showed presence of alkaloids only. GC-MS analysis of garlic oil study indicated that garlic oil of GSK was found to have eugenol as a novel source compared with garlic oil of GSM. Garlic oil of GSK showed significant anti-tumour activity against DLA cells, compared with garlic oil of GSM. Conclusion: Garlic oil of GSK exhibited potential anti-tumour activity against DLA cells due to presence of eugenol compound as novel source.

}, keywords = {Anti-tumour, Garlic oil, GC-MS, MTT, Phyto-constituents}, doi = {10.5530/pj.2019.11.52}, author = {Susha Antony and Kunnambath Krishna Kumar and Jalaja Sudhi Menon} } @article {683, title = {Antibacterial and Cytotoxic Activities of Sponges Collected off the Coast of Togean Islands, Indonesia}, journal = {Pharmacognosy Journal}, volume = {10}, year = {2018}, month = {August 2018}, pages = {988-992}, type = {Original Article}, chapter = {988}, abstract = {

Context: Marine sponges (Porifera: Demospongia) have astonishing structural diversity and broad biological activities. Aims: To evaluate the antibacterial and cytotoxic activities of five sponges collected off the coast of Togean Islands, Indonesia, identified as Spheciospongia inconstan, Melophlus sarasironum, Oceanapia amboinensis, Biemna sp and Axinella sp. Methods and Material: All dried sponges materials were extracted by maceration method using methanol and then evaporated by the rotary evaporator to obtain viscous extracts. The determination of antibacterial activity was performed by well agar diffusion method against Staphylococcus aureus and Escherichia coli while the cytotoxic activity was determined by MTT methods on human breast adenocarcinoma (MCF-7) and human colon colorectal carcinoma (HCT-116), followed by determination of the apoptosis mechanism by Annexin V-FTIC assay. Results: M. sarasinorum and Axinella sp showed strong inhibition against S.aureus and E.coli with the diameter of inhibition of 14.21 \± 0.92 mm and 14.36 \± 0.92 mm, and 10.01 \± 2.65 mm and 12.07 \± 1.54 mm, respectively. Moreover, they also exhibited potent cytotoxicity on HCT-116 with IC50 values of 0.002 and 8.518 \μg/mL, respectively. Meanwhile, on MCF-7, only M. sarasinorum showed moderate inhibition with an IC50 value of 87.35 \μg/mL. Annexin V-FTIC assay clearly showed that the cytotoxic mechanism of M. sarasinorum and Axinella sp on HCT-116 and MCF-7 was via apoptosis induction. Conclusion: The sponges of M. Sarasinorum and Axinella sp are undergoing further analysis to identify the active constituents which could be developed as potential antibacterial and anticancer agents.

}, keywords = {Antibacterial, Cytotoxicity, MTT, Sponges, Togean Islands}, doi = {10.5530/pj.2018.5.168}, author = {Muhammad Sulaiman Zubair and Subehan Lallo and Masteria Yunovilsa Putra and Tri Aryono Hadi and Ibrahim Jantan} } @article {350, title = {Cytotoxic Activity of Antioxidant-Riched Dendrobium longicornu}, journal = {Pharmacognosy Journal}, volume = {9}, year = {2017}, month = {May 2017}, pages = {499-503}, type = {Original Article}, chapter = {499}, abstract = {

Context: Dendrobium longicornu is a traditional medicinal plant widely used in Asia. It has many bioactive compounds like bibenzyl, phenanthrenes, phenolic compounds. There has been little research in the cytotoxic and antioxidant effects of D. longicornu. Aims: The aim of this study was to investigate the cytotoxic and antioxidant activities of this plant. Settings and Design: Antioxidant and cytotoxic activity of Dendrobium longicornu extracts. Methods and Material: The plant extracts were prepared by soxhlet\’s extractor in organic solvents, acetone and ethanol. The total polyphenol content (TPC) in the extracts was determined spectrophotometrically by the Folin-Ciocalteu method and the total flavonoid content (TFC) by aluminium chloride method. The antioxidant activity was determined using DPPH (2,2-diphenyl-1-picrylhydrazyl) method. The cytotoxic activity was evaluated against human brain tumor cells (U251) and cervical cancer cells (HeLa) using MTT assay. Statistical analysis used: Regression analysis was done for calculation of IC50. Duncan multiple range test and Dunnett test were done to compare the data. Results: The Dendrobium longicornu acetonic extract (DLA) showed significantly highest TPC and TFC than Dendrobium longicornu ethanolic extract (DLE). The antioxidant activity was also significantly higher in DLA followed by DLE. Highest cytotoxicity (i.e., lowest IC50 value) was found for the DLA on U251 cells and DLE on HeLa cells. Conclusions: This result concluded that D. longicornu is a potential source of antioxidant and cytotoxic agents.

}, keywords = {Dendrobium longicornu, DPPH, Flavonoid, MTT, Polyphenol}, doi = {10.5530/pj.2017.4.81}, url = {/files/PJ-9-4/10.5530pj.2017.4.81}, author = {Mukti R Paudel and Mukesh B Chand and Basant Pant and Bijaya Pant} } @article {457, title = {In vitro Antioxidant and Hepatoprotective Activity of Bridelia scandens (Roxb.)Willd}, journal = {Pharmacognosy Journal}, volume = {9}, year = {2017}, month = {November 2017}, pages = {s117-s121}, type = {Original Article}, chapter = {s117}, abstract = {

Natural products are emerging out as potent and alternative therapies for many diseases. Today herbs have become the part of mankind, because of its manifold ways in targeting diseased cells with minimal effects on normal cells and tissues. The present research investigated the in vitro antioxidant activity and hepatoprotective of B.scandens leaf. Preliminary phytochemical analysis exhibited the presence of most of the constituent in ethanol extract (BSE). Antioxidant capacity of various extracts of B.scandens was examined. DPPH assay revealed that ethanol extract has a good antioxidant with IC50 value of 31.68\μg/ml, whereas standard ascorbic acid with 8.78 \μg/ml. BSE revealed dose dependent response with increase in concentration for reducing power assay. ORAC assay directly measured the scavenging capacity and BSE (2485 trolox eq/gm) was found to be potent than other extracts. In vitro hepatoprotective activity was performed for BSE using MTT assay in BRL 3A cell line, which revealed nontoxic dose with CTC50 value more than 1000 \μg/ml. At the dose 200 \μg/ml, BSE and standard silymarin offered cell protection of 57\% and 76 \% respectively. Present study concludes that B.scandens leaf extract possess antioxidant potential and protect the liver cells against CCl4 damage. However in vivo studies are being carried out to validate the traditional usage of Bridelia scandens.

}, keywords = {Bridelia scandens, BRL3A, Hepatoprotective, MTT, ORAC}, doi = {10.5530/pj.2017.6s.167}, url = {http://fulltxt.org/article/392}, author = {Preetham Jinadatta and Kiran Sundera Raja Rao and Sharath Rajshekarappa and Sujan Ganapathy Pasura Subbaiah and Mruthunjaya Kenganora} } @article {1479, title = {Free Radical Scavenging and Cytotoxic Potential of Celosia argentea}, journal = {Pharmacognosy Journal}, volume = {7}, year = {2015}, month = {09th Mar, 2015}, pages = {191-197}, type = {Original Article}, chapter = {191}, abstract = {

Introduction: Oxidative stress due to reactive oxygen species often leads to pathogenesis of chronic diseases such as cancer. Research states that a diet rich in polyphenols renders many health benefits by scavenging such harmful reactive species. Celosia argentea (Amaranthaceae), a common weed in India has been reported as a potential source of cheap, natural antioxidants due to its phenolic abundance. In this research work efforts were made to identify and screen the phenolic rich fractions of Celosia argentea for their antioxidant and anticancer potential. Materials and Methods: Various solvent fractions with increasing polarity were subjected to total phenolic content, followed by antioxidant assays- DPPH, ABTS and anti proliferative assays- Brine shrimp Bioassay, Antimitotic and MTT assays. Results: IC50 value of methanolic fraction for DPPH assay was statistically significant (26.25; ***P\<0.001) when compared with ascorbic acid (12.50; ***P\<0.001). Also TEAC values for methanolic fraction and BHT (standard) for ABTS assay were similar (2.1; ***P\<0.001) Methanolicfraction at 400 \μg/ml exhibited strong cytotoxicity (9.0 \± 0.81; ***P\<0.001) against brine shrimps comparable to Methotrexate at 50 \μg/ml(10; ***P\<0.001) and significantly reduced mitotic index from 96.8 to 38.0 (***P\<0.001) which was further confirmed by MTT assay where IC50 value of methanolic fraction for SiHa and MCF-7 cells was found to be 28 \μg/ml with no cytotoxicity to normal cells proving its anticancer potential. Conclusion: This research proves antioxidant and anticancer potential of phenolic rich fraction of Celosia argentea and suggests it to be useful in cancer management as antifroliferative, chemo preventive and in cancer chemotherapy induced immune suppression and oxidative stress.

Key words: Antioxidant, Brine shrimp, Mitotic index, MTT, Phenolics.

}, keywords = {Antioxidant, Brine shrimp, Mitotic index, MTT, Phenolics.}, author = {Rukhsana Abdul Rub and Manohar Janardhan Patil and Areej Abdul Siddiqui and Priyanka Rambhau Ghorpade and Alpana Subhod Moghe} } @article {55, title = {Free Radical Scavenging and Cytotoxic Potential of Celosia argentea}, journal = {Pharmacognosy Journal}, volume = {7}, year = {2015}, month = {01/2015}, pages = {191-197}, type = {Original Article}, chapter = {191}, abstract = {

Introduction: Oxidative stress due to reactive oxygen species often leads to pathogenesis of chronic diseases such as cancer. Research states that a diet rich in polyphenols renders many health benefits by scavenging such harmful reactive species. Celosia argentea (Amaranthaceae), a common weed in India has been reported as a potential source of cheap, natural antioxidants due to its phenolic abundance. In this research work efforts were made to identify and screen the phenolic rich fractions of Celosia argentea for their antioxidant and anticancer potential. Materials and Methods: Various solvent fractions with increasing polarity were subjected to total phenolic content, followed by antioxidant assays-DPPH, ABTS and anti proliferative assays- Brine shrimp Bioassay, Antimitotic and MTT assays. Results: IC50 value of methanolic fraction for DPPH assay was statistically significant (26.25; ***P\<0.001) when compared with ascorbic acid (12.50; ***P\<0.001). Also TEAC values for methanolic fraction and BHT (standard) for ABTS assay were similar (2.1; ***P\<0.001) Methanolicfraction at 400 \μg/ml exhibited strong cytotoxicity (9.0 \± 0.81; ***P\<0.001) against brine shrimps comparable to Methotrexate at 50 \μg/ml(10; ***P\<0.001) and significantly reduced mitotic index from 96.8 to 38.0 (***P\<0.001) which was further confirmed by MTT assay where IC50 value of methanolic fraction for SiHa and MCF-7 cells was found to be 28 \μg/ml with no cytotoxicity to normal cells proving its anticancer potential. Conclusion: This research proves antioxidant and anticancer potential of phenolic rich fraction of Celosia argentea and suggests it to be useful in cancer management as antifroliferative, chemo preventive and in cancer chemotherapy induced immune suppression and oxidative stress.

}, keywords = {Antioxidant, Brine shrimp, Mitotic index, MTT, Phenolics.}, doi = {10.5530/pj.2015.3.8}, author = {Rukhsana Abdul Rub and Manohar Janardhan Patil and Areej Abdul Siddiqui and Priyanka Rambhau Ghorpade and Alpana Subhod Moghe} } @article {1521, title = {The In-Vitro Toxic Effect of The Glycoalkaloids for Some Solanum Species Against The LIM-1863 Cell Line}, journal = {Pharmacognosy Journal}, volume = {6}, year = {2014}, month = {26th May 2014}, pages = {23-31}, type = {Research Article}, abstract = {

Background The LIM-1863 Cell Line is one of the colon cancer types considered to be responsible for a high rate of deaths, and the glycoalkaloids being natural substances existing in the Solanum species have anticancer effects. Objective This research aims at studying the effect of the glycoalkaloids on viability of the LIM-1863 cancerous cells in-vitro. Materials and Methods The glycoalkaloids in this study are extracted by the ultrasonic waves technique and detecting them by the Thin Layer Chromatography (TLC) in addition to incubating of the LIM-1863 cells with different concentrations of the glycoalkaloids for 48 hours and then assessing of the cell viability using the MTT assay. Results The findings showed that the glycoalkaloids have a toxic effect on the LIM-1863 cells and that half of the inhibiting concentration (IC50) of the Solanum fruits extract: (Solanum nigrum L.), (Solanum villosum Mill.) and (Solanum elaeagnifolium Cav.) on the LIM-1863 cells have the (164.7, 35.91 and 12.14 \μg/ml) values successively. Conclusion The observations indicated that the glycoalkaloids are able to inhibit the colon cancer cell proliferation.

Key words:Solanum, Glycoalkaloids, TLC, LIM-1863, Viability, MTT.

}, keywords = {Glycoalkaloids, LIM-1863, MTT, Solanum, Viability}, author = {Ahmad Sammani and Esam Shammaa and Fawaz Chehna and Abdulkader Rahmo} }