Current Bioactive Compounds - Volume 17, Issue 6, 2021

Carbon curvatures are novel therapeutic bio-material that are being studied due to its multifarious applications in a variety of research aspects. All the carbon allotropes were grouped mathematically into three types based upon surface Gaussian curvatures: zero curvature (graphene), negative curvature (schwarzites), and positive curvature (fullerenes, CNTs), because they have physiochemical activities, such as optoelectrical, chemical, thermal and magnetic properties. All these allotropes consist of sp2 hybridization with delocalized π bond electrons. Based on the types and number of aromatic carbon rings, all ofthese have unique geometric structural characteristics, chirality, and solubility, which offers them as a potential candidate for biomedical and therapeutic applications. In this short review, we highlight the basic structural and physicochemical characteristics of carbon allotropes and their biomedical and therapeutic applications recentlystudied by researchers and describe the therapeutic applications of graphene and its derivatives in drug delivery, gene delivery, bio-imaging, biosensors, therapeutic diagnosis, and photo-stimulation therapies.

Oral squamous cell carcinoma (OSCC) is considered the most common neoplasm of the oral cavity and ranked the sixth most prevalent cancer worldwide. Risk factors correlated with the disease are smoking and alcohol drinking as well as HPV-16 infection. Bioactive compounds such as ascorbic acid, quercetin, kaempferol, chlorogenic acid, caffeic acid, ferulic acid, anthocyanins, and β-carotene are authenticated and shown to possess anti-oral cancer activity. Not to mention, anti- oxidant, anti-inflammatory, anti-oxidant, anti-viral, psychostimulant activities, and anti-carcinogenic effects. All of the referred constituents are abundantly found in a plant called Ulam raja, scientifically known as Cosmos caudatus (C. caudatus). C. caudatus is a plant traditionally used in Southeast Asia as an anti-diabetic, anti-arthritic, and anti-hypertensive remedy. This paper describes the substances of C. caudatus that have anti- oral cancer properties. Their properties, mechanism of action, and their most notable bioactive constituents against OSCC and their potential as chemotherapeutic drugs are discussed in this paper.

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives showed excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have shown excellent binding affinity towards DNA gyrase.

Background: Parkinson’s disease (PD) is one of the most common neurodegenerative disorders spread worldwide in elderly people. Methods: The Citrus peels methanolic extract (100 mg/kg body weight) was evaluated as an antiparkinsonism agent in rats through estimation of oxidative stress markers, neurotransmitter levels, energetic indices, DNA fragmentation pattern, inflammatory mediators, adenosine A2A receptor gene expression and the histopathological analysis of the brain. In addition, its effect was compared with ZM241385; an adenosine A2A receptor antagonist, as well as the classical drug; (L-dopa). Results: The methanolic extract of C. sinensis peels constituted 17.59 ± 1.92 mg GAE/g and 4.88 ± 0.43 mg CE/g of total phenolic and flavonoid content, respectively. The polyphenolic composition was qualified and quantified using HPLC/DAD and UPLC/ESI-MS analysis. HPLC/DAD analysis led to identify 8 phenolic acids and 4 flavonoids. UPLC/MS analysis led to identify 20 polyphenolic compounds, including 9 polymethoxylated flavoniods, 7 flavonoidal glycosides and 4 phenolic derivatives. Nobiletin and tangeretin were found as abundant polymethoxylated flavones while, hesperidin and 1-caffeoyl-β-D-glucose were found as abundant glycosyl flavone and phenolic derivatives, respectively. Rotenone induced rats showed a significant decrease in neurotransmitter levels, energetic and antioxidant parameters, while a significant increase in total protein, inflammatory mediators, adenosine A2A receptor gene expression, DNA and lipid peroxidation levels was recorded. Treatments with plant extract, L-dopa and ZM241385 restored these selected parameters to variable extents with a more potent effect of ZM241385 than L-dopa. Rotenone induced rats were left free without treatment; not recorded a noticeable improvement level. Conclusion: Citrus sinensis peels was rich with bioactive valuable-added products. This may lead to the development of new nutraceutical and pharmaceutical agents as well as functional food products used as anti-oxidative, anti-inflammatory and anti-parkinsonian agent.

Background: Constipation is a common, predominant, chronic gastrointestinal functional disorder. The drugs available to treat constipation are limited because of their side effects for long term use. Therefore, we need effective drug to treat constipation. Sapindus emarginatus Vahl belongs to the family Sapindaceae, commonly known as soapnut. It is traditionally used as an antipruritic, antifertility, laxative, and anti-inflammatory agent. Objective: The present study was conducted to evaluate the laxative activity of hydroethanolic pericarp extract of Sapindus emarginatus (HESE) in animal models. Methods: The saponin content in the extract was measured by the gravimetric analysis. The laxative activity of hydroethanolic pericarp extract of Sapindus emarginatus was evaluated by the weight of feces matter, charcoal meal hyperperistalsis test, and loperamide induced constipation model. Results: The saponin content of the soapnut pericarp was 13.48% and the extract was found to be 11.92%. The results obtained from these models showed a significant dose-dependent increase in fecal weight, peristalsis index, and moisture content compared to control animals. Conclusion: The present study concluded that the oral administration of HESE showed a significant laxative activity in different animal models. The presence of triterpene saponins is supposed to be responsible for this activity. Further studies are needed to confirm their mechanism behind the laxative effect. The administration of the extract was found to be effective in constipation therapy.

Background: According to a number of previous studies, citrus fruits are rich in phytochemicals, minerals and bioactive compounds. Objective: The aim of this study was to investigate the antioxidant, antimicrobial and anticoagulant activities, phytonutrients, bioactive compounds, mineral and heavy metals in the peel and pulp of Elachi lemon (Citrus limon). Methods: Phytochemical screening was performed to estimate the total polyphenol, flavonoid, tannin, reducing sugar, total protein and vitamin C contents. High performance liquid chromatography was performed to determine the concentrations of phenolics and ascorbic acid. Antioxidant activities were evaluated by measuring 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, reducing power assay and ferric reducing antioxidant power (FRAP) assay. Antibacterial activity was evaluated by the disc diffusion method and minimum inhibitory concentration (MIC). Besides estimating heavy metals and minerals, activated partial thromboplastin time (aPTT) and prothrombin time (PT) were observed for detecting anticoagulant activity. Results: In the case of antioxidant and antimicrobial activities, the pulp was found to be richer. Both the peel and pulp showed similar anticoagulant activities. Among the phytonutrients, protein content was richer in the peel than in the pulp. Catechin, rutin, tannic, gallic and vanillic acids were detected in the peel, whereas in pulp quercetin, tannic and gallic acids were found. Pb, Cr, Cd were present in a negligible amount whereas, Co, Cu and Fe were high in both the peel and the pulp. Conclusion: This study exhibits that both the peel and the pulp of Citrus limon are a rich source of antioxidant, antimicrobial, anticoagulant, minerals and various bioactive compounds with nutritional values.

Objective: The study was conducted to examine the antimicrobial activity of methanolic crude extract from different parts of the Chlorophytum borivilianum plant against pathogenic microorganisms and toassess antimicrobial activity by MIC and structural characterization of purified saponin of Chlorophytum borivilianum by using spectrophotometric and NMR analysis. Methods: The antimicrobial analysis of the extracts of leaves, roots and stems of C. borivilianum is based on the agar well diffusion method and Minimum Inhibitory Concentration (MIC). The phytochemical screening and characterization of saponin on the basis of structural and antimicrobial activity present in C. borivilianum were analyzed by different spectrophotometric methods such as HPLC, UV-visible, IR, NMR, LC-ESI-MS and pharmacophore modeling. Results: The results revealed that the methanolic leaf, stem and root extracts have inhibitory potential against the growth of K. pneumonia, B. subtilis, M. tuberculosis, E coli and S. aureus in case of bacteria and C. albicans, A. fumigatus and Tricoderma in case of fungus. The MIC values of leaf, stem and root extracts were found in the range of 1 mg/ml to 0.125 mg/ml. Moreover, the purified saponins indicated MIC in the range of 0.5 mg/ml to 0.0625 mg/ml against the selected microbial pathogens. Saponins act as one of the major phytocomponents present in C. borivilianum. The antimicrobial and structural analysis of purified saponins of C. borivilianum was also performed using different spectral analysis methods. Conclusion: The anti-microbial results showed that the extract from the leaf and stems had higher anti-pathogenic activity as compared to the roots. The MIC results showed that the purified saponin also possessed the anti-microbial activity and oleanolic acid content, as detected by spectral analysis the fundamental structure of the extracted saponin.

Background: Schinus molle L. is a medicinal and aromatic plant widely used in folk medicine and commonly found in Algeria and the Mediterranean region. In the present work, we investigated the in vitro antioxidant, anti-cholinesterase, α-glucosidase inhibitory and photoprotective potentials of the Schinus molle L. plant’s extract/fractions. The metabolite profile of Schinus molle L. was analyzed using RP-HPLC and GC-MS. Methods: The antioxidant activity was assessed using different tests. The anticholinesterase activity was investigated by quantifying the acetylcholinesterase and butyrylcholinesterase inhibitory activities. The antidiabetic activity was investigated by α-glucosidase inhibition test, whereas photoprotective activity was evaluated by Sun Protection Factor (SPF) using spectrophotometry UV-Vis. The extracts were then subjected to RP-HPLC–PDA and GC–MS analysis. Results: Ethyl acetate and butanol fractions with high contents of total phenolics and flavonoids exhibited the strongest antioxidant activity. Ethyl acetate extract exhibited considerable enzyme inhibition potential on acetylcholinesterase, butyrylcholinesterase and α-glucosidase with percentages of inhibition of 99.08 ± 0.79%, 100% and 98.80 ± 0.18%, respectively. Furthermore, the ethyl acetate fraction showed high photoprotective activity with the Sun Protection Factor (SPF) value = 38,26 ± 0.73. Three phenolic acids (gallic, tannic and vanillic acids) and five flavonoids (myricetin, apigenin, naringenin, rutin and quercetin) were identified with RP-HPLC–PDA. Conclusion: These findings suggest that Schinus molle L. may be useful in the development of an alternative agent for oxidative stress, Alzheimer’s disease, diabetes and could be used as a natural sunscreen in pharmaceutics or cosmetic formulations.