scholarly journals Morphology, Anatomy and Secondary Metabolites Investigations of Premna odorata Blanco and Evaluation of Its Anti-Tuberculosis Activity Using In Vitro and In Silico Studies

Plants ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1953
Author(s):  
Fadia S. Youssef ◽  
Elisa Ovidi ◽  
Nawal M. Al Musayeib ◽  
Mohamed L. Ashour

In-depth botanical characterization was performed on Premna odorata Blanco (Lamiaceae) different organs for the first time. The leaves are opposite, hairy and green in color. Flowers possess fragrant aromatic odors and exist in inflorescences of 4–15 cm long corymbose cyme-type. In-depth morphological and anatomical characterization revealed the great resemblance to plants of the genus Premna and of the family Lamiaceae, such as the presence of glandular peltate trichomes and diacytic stomata. Additionally, most examined organs are characterized by non-glandular multicellular covering trichomes, acicular, and rhombic calcium oxalate crystals. P. odorata leaves n-hexane fraction revealed substantial anti-tuberculous potential versus Mycobacterium tuberculosis, showing a minimum inhibition concentration (MIC) of 100 μg/mL. Metabolic profiling of the n-hexane fraction using gas-chromatography coupled to mass spectrometry (GC/MS) analysis revealed 10 major compounds accounting for 93.01%, with trans-phytol constituting the major compound (24.06%). The virtual screening revealed that trans-phytol highly inhibited MTB C171Q receptor as M. tuberculosis KasA (β-ketoacyl synthases) with a high fitting score (∆G = −15.57 kcal/mol) approaching that of isoniazid and exceeding that of thiolactomycin, the co-crystallized ligand. Absorption, distribution, metabolism, excretion and toxicity predictions (ADME/TOPKAT) revealed that trans-phytol shows lower solubility and absorption levels when compared to thiolactomycin and isoniazid. Still, it is safer, causing no mutagenic or carcinogenic effects with higher lethal dose, which causes the death of 50% (LD50). Thus, it can be concluded that P. odorata can act as a source of lead entities to treat tuberculosis.

2016 ◽  
Vol 11 (5) ◽  
pp. 1934578X1601100
Author(s):  
Wei Luo ◽  
Yaya Wen ◽  
Yanbei Tu ◽  
Hongjian Du ◽  
Qin Li ◽  
...  

Ten flavonoids (1–10), including a new glycoside (nevadensin-7-sambubioside, 7), together with a phenylpropanoid glycoside (11) were isolated from Lysionotus pauciflorus. Their structures were elucidated by a combination of spectroscopic methods and comparing with literature data. Five compounds (1, 3, 4, 8, and 9) were obtained from the family Gesneriaceae for the first time. The new compound was evaluated in vitro for anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), but was found to be inactive.


Cancers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 427 ◽  
Author(s):  
Ranjini Sankaranarayanan ◽  
Chaitanya Valiveti ◽  
D. Kumar ◽  
Severine Van slambrouck ◽  
Siddharth Kesharwani ◽  
...  

Flavonoids have emerged as promising compounds capable of preventing colorectal cancer (CRC) due to their anti-oxidant and anti-inflammatory properties. It is hypothesized that the metabolites of flavonoids are primarily responsible for the observed anti-cancer effects owing to the unstable nature of the parent compounds and their degradation by colonic microflora. In this study, we investigated the ability of one metabolite, 2,4,6-trihydroxybenzoic acid (2,4,6-THBA) to inhibit Cyclin Dependent Kinase (CDK) activity and cancer cell proliferation. Using in vitro kinase assays, we demonstrated that 2,4,6-THBA dose-dependently inhibited CDKs 1, 2 and 4 and in silico studies identified key amino acids involved in these interactions. Interestingly, no significant CDK inhibition was observed with the structurally related compounds 3,4,5-trihydroxybenzoic acid (3,4,5-THBA) and phloroglucinol, suggesting that orientation of the functional groups and specific amino acid interactions may play a role in inhibition. We showed that cellular uptake of 2,4,6-THBA required the expression of functional SLC5A8, a monocarboxylic acid transporter. Consistent with this, in cells expressing functional SLC5A8, 2,4,6-THBA induced CDK inhibitory proteins p21Cip1 and p27Kip1 and inhibited cell proliferation. These findings, for the first time, suggest that the flavonoid metabolite 2,4,6-THBA may mediate its effects through a CDK- and SLC5A8-dependent pathway contributing to the prevention of CRC.


2006 ◽  
Vol 188 (21) ◽  
pp. 7488-7499 ◽  
Author(s):  
Daniel Pérez-Mendoza ◽  
María Lucas ◽  
Socorro Muñoz ◽  
José A. Herrera-Cervera ◽  
José Olivares ◽  
...  

ABSTRACT Genetic and biochemical characterization of TraA, the relaxase of symbiotic plasmid pRetCFN42d from Rhizobium etli, is described. After purifying the relaxase domain (N265TraA), we demonstrated nic binding and cleavage activity in vitro and thus characterized for the first time the nick site (nic) of a plasmid in the family Rhizobiaceae. We studied the range of N265TraA relaxase specificity in vitro by testing different oligonucleotides in binding and nicking assays. In addition, the ability of pRetCFN42d to mobilize different Rhizobiaceae plasmid origins of transfer (oriT) was examined. Data obtained with these approaches allowed us to establish functional and phylogenetic relationships between different plasmids of this family. Our results suggest novel characteristics of the R. etli pSym relaxase for previously described conjugative systems, with emphasis on the oriT cis-acting preference of this enzyme and its possible biological relevance.


2015 ◽  
Vol 3 (4) ◽  
pp. 721-726
Author(s):  
Md. Moinul Abedin Shuvo ◽  
Mohammad AL - Mamun ◽  
Tuhina Chowdhury ◽  
Nurul Absar ◽  
Md. Hasanuzzaman

Stevia rebaudiana, belongs to the family of Asteraceae, is a perennial and medicinal shrub. It’s leaves dry powder widely used as a natural sweetener which has no calories but reported to be 50– 300 times sweetener as sweet as sugar, that are said to be having insulin balancing properties without any side effects. This research was first time conducted in Bangladesh where a quantitative analysis were performed for determining the major constituents of in vitro propagated Stevia rebaudiana plant leaves dry powder that was prepared through oven dry after sun dry. The analysis revealed the powder as mild acidic (PH 5.345). Total chlorophyll contents were found to be 0.845mg% where chlorophyll–a and -b were 0.088 and 0.761 mg% respectively.  The major macro nutrients such as ash, crude fiber, total carbohydrate, total protein and fat were determined at the amount of 7.05, 10.5, 53.52, 13.13 and 3.55 gm% respectively where the micro nutrients like Iron (Fe), Sodium (Na), Potassium (K), Calcium (Ca), Magnesium (Mg), Phosphorus (P) and Chloride (Cl) were found at the amount of 34.2, 184.3, 2500, 534.43, 465.34, 304.7 and 49.6 mg% accordingly.  Screening for secondary metabolites showed the presence of alkaloids, flavonoids, saponins and tannins as the amount of 2.83, 17.20, 6.69 and 5.84 mg% respectively in dry powder. These findings also have been compared with the other reported values on Stevia from different countries of the world.   Int J Appl Sci Biotechnol, Vol 3(4): 721-726


2017 ◽  
Vol 61 (4) ◽  
Author(s):  
L. Mueller ◽  
P. M. Hauser ◽  
F. Gauye ◽  
G. Greub

ABSTRACT Lausannevirus belongs to the family Marseilleviridae within the group of nucleocytoplasmic large DNA viruses (NCLDVs). These giant viruses exhibit unique features, including a large genome, ranging from 100 kb to 2.5 Mb and including from 150 to more than 2,500 genes, as well as the presence of genes coding for proteins involved in transcription and translation. The large majority of Lausannevirus open reading frames have unknown functions. Interestingly, a bifunctional dihydrofolate reductase-thymidylate synthase (DHFR-TS) is encoded in the Lausannevirus genome. The enzyme plays central roles in DNA precursor biosynthesis. DHFR is the pharmacological target of antifolates, such as trimethoprim, pyrimethamine, and proguanil. First, the functionality of Lausannevirus DHFR-TS was demonstrated by the successful complementation of a DHFR-deficient Saccharomyces cerevisiae strain with a plasmid expressing the heterologous gene. Additionally, using this heterologous expression system, we demonstrated the in vitro susceptibility of Lausannevirus DHFR-TS to proguanil and its resistance to pyrimethamine and trimethoprim. Proguanil may provide a unique and useful treatment if Lausannevirus proves to be a human pathogen. To our knowledge, this is the first time that a DHFR-TS has been described and characterized in an NCLDV.


2015 ◽  
Vol 1 (2) ◽  
Author(s):  
Titi Hariyati ◽  
Dwi Soelistya Dyah Jekti ◽  
Yayuk Andayani

Syzygium aqueum plant of the family Myrtaceae is native of Malaysia and Indonesia and is known as the water rose. The active compound is useful as an antibacterial. This study aimed to determine the effects of ethanol extracts of guava leaves (S. aqueum) as an antimicrobial against clinical isolates bacteria in vitro. The design used in experiment was a Completely Randomized Design (CRD). Data were analyzed using the Kruskal-Wallis test. Results of statistical analysis using SPSS 20 for windows indicated that the ethanol extract of guava leaves has a significant (P<0,05) effect in inhibiting the growth of clinical isolates bacteria. MIC (Minimum Inhibition Concentration) of ethanol extracts for each bacterium can not be determined because the guava leaf extract was very dark. The MBC (Minimum Bacterisidal Concentration) of ethanol extract of guava leaf  for both S. aureus and S. dysenteriae was 20%.  The MBC of the extract for E. coli, S. thypi, V. cholerae was 25%, where as for B. cereus was at concentration of 50%. It can be concluded that guava leaf has highly potential as a source of antimicrobial agent.Keywords:Antibacteria, Guava Leaf, Clinical Isolates Bacteria, Ethanol Extract


2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Aline Lopes Ribeiro ◽  
Carolini Kaid ◽  
Patrícia B. G. Silva ◽  
Beatriz A. Cortez ◽  
Oswaldo Keith Okamoto

Pericytes are important cellular components of the tumor microenviroment with established roles in angiogenesis and metastasis. These two cancer hallmarks are modulated by enzymes of the LOX family, but thus far, information about LOX relevance in tumor-associated pericytes is lacking. Here, we performed a comparative characterization of normal and tumoral pericytes and report for the first time the modulatory effects of LOX enzymes on activated pericyte properties. Tumoral pericytes isolated from childhood ependymoma and neuroblastoma specimens displayed angiogenic properties in vitro and expressed typical markers, including CD146, NG2, and PDGFRβ. Expression of all LOX family members could be detected in both normal and tumor-associated pericytes. In most pericyte samples, LOXL3 was the family member displaying the highest transcript levels. Inhibition of LOX/LOXL activity with the inhibitor β-aminopropionitrile (βAPN) significantly reduced migration of pericytes, while proliferation rates were kept unaltered. Formation of tube-like structures in vitro by pericytes was also significantly impaired upon inhibition of LOX/LOXL activity with βAPN, which induced more prominent effects in tumor-associated pericytes. These findings reveal a novel involvement of the LOX family of enzymes in migration and angiogenic properties of pericytes, with implications in tumor development and in therapeutic targeting tumor microenvironment constituents.


Molecules ◽  
2021 ◽  
Vol 26 (1) ◽  
pp. 203
Author(s):  
Hamdoon A. Mohammed ◽  
Mohammed F. Abdelwahab ◽  
El-Sayed M. El-Ghaly ◽  
Ehab A. Ragab

Pulicaria jaubertii is a medicinal herb that alleviates inflammations and fever. Chromatographic separation, phytochemical characterization, and in vitro biological activities of the plant n-hexane extract were conducted for the first time in this study. Six compounds were isolated for the first time from the n-hexane fraction of Pulicaria jaubertii aerial parts and were identified on the bases of NMR and MS analyses as pseudo-taraxaterol (1), pseudo-taraxasterol acetate (2), 3β-acetoxytaraxaster-20-en-30-aldehyde (3), calenduladiol-3-O-palmitate (4), stigmasterol (5), and α-tocospiro B (6). Compound (6) was a rare tocopherol-related compound and was isolated for the first time from family Asteraceae, while compound (3) was isolated for the first time from genus Pulicaria. The total alcoholic extract and n-hexane fraction were tested for their anti-inflammatory, antidiabetic, and cytotoxic activities. The n-hexane fraction has dose dependent red blood cells (RBCs) membrane stabilization and inhibition of histamine release activities with IC50: 60.8 and 72.9 µg/mL, respectively. As antidiabetic activity, the alcoholic extract exerted the most inhibition on the activity of yeast α-glucosidase, with an IC50: 76.8 µg/mL. The n-hexane fraction showed cytotoxic activity against hepatocarcinoma (HepG-2), breast carcinoma (MCF-7), and prostate carcinoma (PC-3) cell lines with IC50: 51.8, 90.8 and 62.2 µg/mL, respectively. In conclusion, the anti-inflammatory effect of Pulicaria jaubertii might be attributed to the triterpenoid constituents of the n-hexane extract of the plant.


2018 ◽  
Vol 2018 ◽  
pp. 1-8
Author(s):  
Javid A. Parray ◽  
Azra N. Kamili ◽  
Sumira Jan ◽  
Mohammad Yaseen Mir ◽  
Nowsheen Shameem ◽  
...  

Arnebia benthamii of the family Boraginaceae is a critically endangered nonendemic plant of the Kashmir Himalayas and is used to treat a number of human diseases. The current study was based on developing an in vitro micropropagation protocol vis-à-vis induction of various secondary metabolites under in vitro conditions for the possible biological activity. A tissue culture protocol was developed for A. benthamii for the first time in the Himalayan region using varied combinations and proper media formulations, including various adjuvants: Murashige and Skoog (MS) media, growth hormones, sugars, agar, and so forth. The influence of different media combinations was estimated, and the MS + thidiazuron (TDZ) + indole 3-acetic acid (IAA) combination favors a higher regeneration potential. The higher amounts of chemical constituents were also recorded on the same treatment. The in vitro plant samples also showed a noteworthy effect of scavenging of hydroxyl radicals vis-à-vis protection from oxidative DNA damage. The in vitro raised plants are good candidates for the development of antioxidant molecules.


2021 ◽  
Vol 16 (9) ◽  
pp. 1934578X2110314
Author(s):  
Le Minh Ha ◽  
Ngo Thi Phuong ◽  
Nguyen Thi Phuong Trang ◽  
Dinh Thi Thu Thuy ◽  
Le Ngoc Hung

Premna flavescens Wall. ex C. B. Clarke, a medicinal plant in the family Lamiaceae, was used for the treatment of arthritis in folk medicine. From the essential oil extracted from the leaves of this plant we have identified 51 components, with β-caryophyllene as the major component (26.3%). The essential oil showed a strong anti-inflammatory effect in vitro with an IC50 of 5.88 µg/mL. DNA barcoding is an useful tool for species identification based on the standardized genomic DNA fragments, but the molecular database of P flavescens is still lacking from Genebank. A molecular species identification tool for P flavescens was developed for the first time using DNA barcoding. The sequences of rbcL, trnH–psbA, internal transcribed spacer, and 18S barcodes of P flavescens were submitted to the Genebank with the accession numbers MW553265, MW553266, MT935698.1, and MW485128.1, respectively. This will be highly useful for the molecular authentication of the marker samples.


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