scholarly journals Optimization of Microwave-Assisted Extraction Process of Callicarpa candicans (Burm. f.) Hochr Essential Oil and Its Inhibitory Properties against Some Bacteria and Cancer Cell Lines

Processes ◽  
2020 ◽  
Vol 8 (2) ◽  
pp. 173 ◽  
Author(s):  
Quoc Toan Tran ◽  
Thu Le Vu Thi ◽  
Tien Lam Do ◽  
Hong Minh Pham Thi ◽  
Bich Hoang Thi ◽  
...  

Callicarpa candicans (Burm. f.) Hochr. (Callicarpa cana L.) is a medicinal plant that is distributed mainly in the tropics and subtropics of Asia and finds a wide range of uses in traditional medicine. In this study, we attempted and optimized the microwave-assisted hydro-distillation (MAHD) process to obtain essential oil from the leaves of C. candicans. In addition, the obtained oil was analyzed for volatile composition by gas chromatography–mass spectrometry (GC-MS) and assayed for bioactivity against several bacteria and cancer cell lines. To optimize the extraction process, response surface methodology (RSM) in combination with central composite design (CCD) was adopted. Experimental design and optimization were carried out with respect to three experimental factors including the ratio of water to raw material, extraction time, and microwave power. The optimal extraction conditions were obtained as follows: water to raw material ratio of 6/1 (v/w), extraction time 42 min, and microwave power 440 W. Composition determination of the obtained C. candicans essential oil indicated the presence of predominant components including caryophyllene <b-> (10.45%), cadinene <d-> (10.28%), gurjunene <a-> (8.95%), muurolene <g-> (8.92%), selinene <a-> (7.06%), selinene <b-> (5.59%), and copaene <a-> (5.40%). In comparison with the essential oils obtained via traditional hydro-distillation method, the essential oil extracted by MAHD exhibited superior anti-proliferative activity on all tested cancer cell lines. Current results imply that the MAHD is capable of recovering biologically-active natural products of greater quantity than that recovered by the conventional distillation.

2021 ◽  
Vol 16 (10) ◽  
pp. 1934578X2110542
Author(s):  
Xuan Duy Le ◽  
Ngoc Mai Pham Thi ◽  
Thi Inh Cam ◽  
Huu Nghi Do ◽  
Hong Van Nguyen Thi ◽  
...  

This study reports on the optimization of a microwave-assisted distillation process to obtain Dong Van marjoram essential oil, and the determination of its composition, content of constituents, and cytotoxic and antimicrobial activities. Using the response surface method (RSM), the optimal essential oil distillation conditions were determined as material size 0.74 (cm), water to material ratio 4.14:1 (mL/g), microwave power 302.4 (W), and distillation time 2.1 hours. At optimal conditions, the mass of Dong Van marjoram essential oil obtained was 0.887 ± 0.007 g, corresponding to a content of 0.6% essential oil in the material. GC-MS and GC-FID methods showed that the main chemical constituents of Dong Van marjoram essential oils obtained were rosefuran epoxide (44.9%), caryophyllene (10.8%), germacrene D (2.6%), and α-humulene (1.3%). The essential oil exhibited moderate inhibition against both tested cancer cell lines, with IC50 values of 23.9 µg/mL (for PC3) and 56.2 µg/mL (for A549). However, the oil exhibited strong effectiveness against three bacterial strains, Escherichia coli, Bacillus subtilis, and Staphylococcus aureus, and a yeast strain, Saccharomyces cerevisiae, with minimal inhibitory concentration (MIC) values ranged from 50 to 100 µg/mL.


Processes ◽  
2018 ◽  
Vol 6 (11) ◽  
pp. 206 ◽  
Author(s):  
Thien Tran ◽  
Huynh Nguyen ◽  
Duy Nguyen ◽  
Thanh Nguyen ◽  
Huynh Tan ◽  
...  

Basil plant is a common source for linalool and estragole. However, it has been showed that the chemical composition of basil varies considerably depending on many factors including method of extraction, cultivar of the plant or geographical location. In this study, we attempted to extract essential oil from Vietnamese basil and analyze the chemical composition of the obtained oil using gas chromatography–mass spectrometry (GC-MS). The extraction method of choice was microwave-assisted hydro-distillation (MAHD) and the process was optimized with Response Surface Methodology (RSM) with regard to four experimental parameters including raw material size, raw material to water ratio, extraction time and microwave power. The results showed that ground basil leaves, when extracted with optimal conditions of water-to-material ratio of 3.2:1, extraction time of 97 (min) and microwave power of 430 (W), gave the actual essential oil yield of 0.6%. Regarding ANOVA results of the quadratic model, high determination coefficient (R2 = 0.9077), significant F-value of 10.92 and the p-value of less than 0.05 indicate that this model is significant between experimental and predicted variables, and should be fixed. In addition, GC-MS analysis revealed that major components of Vietnamese Basil were Estragole (87.869%), α-Bergamotene (2.922%), τ-Cadinol (2.770%), and Linalool (1.347%).


2019 ◽  
Vol 16 (2) ◽  
pp. 117-121 ◽  
Author(s):  
Peipei Han ◽  
Wenhua Zhou ◽  
Mingxia Chen ◽  
Qiuan Wang

A series of eight polymethoxychalcone Mannich base derivatives 2a-2h was synthesized via the microwave-assisted Mannich reaction of natural product 2&#039;-hydroxy-3,4,4&#039;,5,6&#039;-pentamethoxychalcone (1) with various secondary amines and formaldehyde. Compared to conventional heating method (80&#176;C), the microwave-assisted method (700W, 65&#176;C) is efficient with short reaction time (0.5-1 h) and good yields (74-88%). The antiproliferative activities of eight Mannich base derivatives were evaluated in vitro on a panel of three human cancer cell lines (Hela, HCC1954 and SK-OV-3) by CCK-8 assay. The results showed that all of the Mannich base derivatives exhibited potential antiproliferative activities on tested cancer cell lines with the IC50 values of 9.13-48.51 &#181;M. Some active compounds exhibited more activity as compared to positive control cis-Platin. Among them, compound 2b revealed to have the strongest antiproliferative activity against all the three cancer cell lines with IC50 values ranging from 9.13 to 11.24 &#181;M.


2020 ◽  
Vol 20 (10) ◽  
pp. 1209-1220
Author(s):  
Rafat M. Mohareb ◽  
Ensaf S. Alwan

Background: Recently tetrahydrobenzo[b]thiazole derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the thiazole nucleus were known. Objective: This work aimed to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. The target molecules were obtained starting from the arylhydrazonocyclohexan-1,3-dione followed by their heterocyclization reactions to produce anticancer target molecules. Methods: The arylhydrazone derivatives 3a-c underwent different heterocyclization reactions to produce thiophene, thiazole, pyrazole and 1,2,4-triazine derivatives. The anti-proliferative activity of twenty six compounds among the synthesized compounds toward the six cancer cell lines namely A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721 was studied. Results: Anti-proliferative evaluations, tyrosine and Pim-1 kinase inhibitions were perform for most of the synthesized compounds where the varieties of substituent through the aryl ring and the thiophene moiety afforded compounds with high activities. Conclusion: The compounds with high anti-proliferative activity towards the cancer cell lines showed that compounds 3b, 3c, 5e, 5f, 8c, 9c, 11c, 12c, 14e, 14f and 16c were the most cytotoxic compounds. Further tests of the latter compounds toward the five tyrosine kinases c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR and Pim-1 kinase showed that compounds 3c, 5e, 5f, 8c, 9c, 12c, 14e, 14f and 16c were the most potent of the tested compounds toward the five tyrosine kinases and compounds 6d, 11a, 20b and 21e were of the highest inhibitions towards Pim-1 kinase. Pan Assay Interference Compounds (PAINS) for the most cytotoxic compounds showed zero PAINS alert and can be used as lead compounds.


Author(s):  
Rafat M. Mohareb ◽  
Yara R. Milad ◽  
Reem A. El-Ansary

Background:: Recently multi-component reactions producing pyran and pyridine derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Through the market it was found that many pharmacological drugs containing the pyran and pyridine nucleus were known. Objective:: We are aiming in this work to synthesize target molecules not only possess anti-tumor activities but also kinase inhibitors. The target molecules were obtained starting from cyclohexan-1,3-dione followed by its heterocyclization reactions to produce anticancer target molecules. Methods:: This work demonstrated multi-component reactions of cyclohexan-1,3-dione with aromatic aldehydes and diethylmalonate using triethylamine as a catalyst to give the 7,8-dihydro-4H-chromen-5(6H)-one derivatives 4a-c. The reaction of compounds 4a-c with either of hydrazine hydrate of phenylhydrazine gave the chromeno[2,3-c]pyrazole derivatives 5a-f, respectively. In addition, further heterocyclization reactions were adopted to give the chromeno[3,2-d]isoxazole, chromene-3-carboxamide derivatives. Moreover, the multi-component reaction of cyclohexan-1,3-dione (1) with either of aromatic aldehydes and diethylmalonate using a catalytic amount of ammonium acetate gave the 1,4,5,6,7,8-hexahydroquinoline derivatives 13a-c. The anti-proliferative activities of the synthesized compounds toward the six cancer cell lines namely A549, H460, HT-29, MKN-45, U87MG, and SMMC-7721 were studied. In addition the c-Met enzymatic activities and inhibition toward the prostate cancer cell PC-3 were measured. Results:: Anti-proliferative evaluations, c-Met enzymatic activities and inhibition toward the prostate cancer cell PC-3 were measured and the results obtained in most cases, indicated that the presence of electronegative Cl group through the molecule favour the inhibitions. Conclusion:: The compounds with high anti-proliferative activity towards the cancer cell lines were 4a, 4b, 6d, 6e, 6f, 10e, 10f, 12c, 14e, 14f, 15c, 16d, 16e, 16f, 19c and 20c. Compounds 4b, 6c, 6d, 8b, 10c, 10d, 12b, 13b, 14c, 14d, 15b, 16c, 16d, 17b, 17c, 19b, 20b and 20c exhibited high potency against c-Met kinase and compounds 4a, 4b, 6b, 6c, 6d, 6f, 8b, 8c, 10c, 10d, 10e, 12b, 12c, 13a, 13b, 13c, 14c, 14d, 14e, 14f, 15b, 15c, 16b, 16c, 16d, 17b, 17c, 19c, 19d, 20a, 20b and 20c displayed high inhibitions toward PC-3 cell line.


2013 ◽  
Vol 763 ◽  
pp. 246-249
Author(s):  
Xiao Song ◽  
Peng Zhao

Flavonoids from Tussilago farfara L. was extracted with the assistance of microwave.Box-Behnken design (BBD) was employed to optimize extraction time; microwave power and ratio of water to raw material to obtain a high flavonoids yield.The optimum extraction conditions were as follows: 73.3% ethanol-water solvent, time 16.25 min and ratio of solvent to raw material 36.2ml/g.The yield of flavonoids was 11.37% based on the above mentioned conditions.


2014 ◽  
Vol 1014 ◽  
pp. 61-64
Author(s):  
Xiao Song ◽  
Peng Zhao ◽  
Qing Hua Meng ◽  
Zhi Shu Tang ◽  
Chang Li Wang

Flavonoids from Platycarya Strobi lacea Sieb.et Zucc. was extracted with the assistance of microwave.Box-Behnken design (BBD) was employed to optimize extraction time; microwave power and ratio of solvent to raw material to obtain a high flavonoids yield. The optimum extraction conditions were as follows: 65.32% ethanol-water solvent, time 3.96 min and ratio of solvent to raw material 20.8 ml/g.The yield of flavonoids was 3.41% based on the above mentioned conditions.


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