Current Bioactive Compounds - Volume 17, Issue 3, 2021

Background: Tuberculosis is a granulomatous irresistible bacterial infection caused by Mycobacterium tuberculosis. The present anti-TB antibiotics are less useful in the treatment of Multi- Drug-Resistant (MDR) strains. Methods: We focused on distinguishing phyto-bioactive compounds dependent on customary uses and testing their concentrates against MDR strains. This will help abbreviate the present remedial regimens for TB and for treating HIV-TB co-disease. Results: This article is an endeavor to examine the antimycobacterial and immunomodulatory role of phyto-bioactive compounds as another option and feature them for additional examination for the management of drug-resistant tuberculosis. Conclusion: This review focused on the tubercle bacilli utilizing bioactive compounds as the therapeutic vehicle against MDR strains and also the synergistic action with available TB medications.

Background: Cephaelis ipecacuanha and Cephaelis acuminate commonly called Ipecac are the important medicinal plants of Cephaelis species belonging to Rubiaceae family. Ipecac is cultivated throughout the world due to their vast of therapeutic applications in gastrointestinal disorders and poisoning cases. Methods: In the present review paper medicinal importance of Ipecac and their main active phytoconstituents cephaeline have been discussed and presented in concise manner to explore their hidden potential. Phytochemical aspects of Ipecac and overview of cephaeline have been also discussed in the present paper. However important Pharmacological activities of cephaeline on gastrointestinal tract, cardiovascular system, Zika virus, Ebola virus, leishmania and malaria have been mainly focused in the present paper. Further important analytical techniques of detection and separation of cephaeline have also been presented in the present paper. Present paper also contains information of Tissue culture techniques of Ipecac for the better production of cephaeline to fulfil the industrial demands. Results: Cephaeline is colourless crystalline active compound of Ipecac plant which is having chemical formula C28H38O4N2. Claimed pharmacological activities of Ipecac such as diaphoretic, expectorant and anti-amoebic are mainly due to the presence of alkaloidal class chemical emetine and cephaeline. Result also revealed that ethanol extract of Ipecac has been used as emetic agents. Phytochemical analysis of the Ipecac revealed the presence of emetine, cephaeline, protoemetine, psychotrine, emetamine, O-methylpsychotrine and psychotrine methyl ether. Pharmacologically cephaeline induces vomiting through acting on stomach lining but it is more toxic and irritant compared to the emetine. Conclusion: The presented information will be beneficial to the scientific communities to know the importance of Ipecac and their main active phytoconstituents cephaeline for the treatment of numerous health related complication.

Eugenol is a bioactive compound commonly found in many herbal plants. The different reported sources of eugenol are clove, cinnamon, holy basil, and pepper. Several therapeutic activities of eugenol like antioxidant, antimicrobial, anesthetic, anti-inflammatory, anti-carcinogenic, neuroprotective agent, anti-diabetic and anti-cancer activities have been reported. However, due to limited aqueous solubility, it has poor bioavailability. Its therapeutic potential can be enhanced by developing eugenol nano-formulations like liposome, nanoparticles, microemulsions and micelles. This article extensively reviews the chemical and pharmacological properties of eugenol and its nano-formulations along with their biological activities.

Background: Seeds of Mung bean (Vigna radiata (L.) R.Wilczek) have been recognized as a 'Green pearl' of Asian cuisine due to abundance of dietary fibres, protein, minerals,vitamins and wide variety of bioactive agents. Methods: Literature has been collected through SciFinder, Web of Science, Google Scholar, Pubmed, and a library. This review shares updated information on the botany, distribution, health benefits, phytochemistry and pharmacology of Mung bean seeds. Results: Bioactive components of mung bean seeds exhibited a wide array of activities such as anticancer, antihyperlipidemic, antihypertensive, antidiabetic, anti-microbial, antioxidant, treatment of alcoholism, reducing obesity, increasing muscular strength, rheumatism, piles, liver and neurological diseases. This curative potential highlighted its various beneficial outcomes in the field of drug research and increasing scientific interest in the identification of bioactive compounds responsible for various pharmacological activities. This legume is gaining importance for its use in the pharmaceutical, food and cosmetic products. Conclusion: Existing literature authenticates the potential benefits of mung bean seeds from nutritional as well as medicinal perspective. This food grain needs to be explored for identification, isolation, and characterization of bioactive compounds against varied ailments.

Aims: This study aims to elucidate the structural difference and biochemical properties of bioactive compounds of microalgal biomasses. Background: The structural difference and biochemical properties of bioactive compounds termed as Water-Soluble Macromolecules (WSMs) are interested in evaluating their biological activities. Methods: This study was performed to elucidate the structural difference and biochemical properties of bioactive compounds termed as Water-Soluble Macromolecules (WSMs) isolated from defatted microalgal biomasses of Botryococcus braunii and Dunaliella tertiolecta. Results: The compositional analysis of both WSMs revealed that WSM-Bb is a hetero-macromolecule consisting of various monosaccharides, whereas WSM-Dt was characterized as a homo-- macromolecule that mainly consists of glucose. Interestingly, WSM-Bb showed the significant tyrosinase inhibitory activity with the increase of both the concentration and reaction time. Whereas there was no significant inhibitory activity observed by WSM-Dt. Conclusion: Inhibitory action of WSM-Bb toward both tyrosinase and tyrosine in either simultaneous or separate reaction may be mainly due to the physical affinity of WSM-Bb. These results emphasize the identification of the primary components of these WSMs and their relevance with the antioxidant function.

Background: Recent studies have provided evidence that marine algae sulfated polysaccharides and phlorotannins play an important role in human health. The aim of this study was to evaluate the anticoagulant activity of five marine algae extracts from Bejaia’s coast (Algeria). Methods: Phenolic and sugar contents of the five marine algae were assessed using folin ciocalteu and anthrone reagents, respectively. The anticoagulant activity was evaluated by the Activated Partial Thromboplastin Time (APTT) and Prothrombin Time (PT). Results: Higher contents of phenolic compounds were obtained with ethanol for Cystoseira humilis, Halopteris scoparia, Padina pavonica, and Rhodomela confervoides (8.55±0.29, 7.84±0.47, 6.41±0.14 and 4.16±0.04 mg CE/g of dw, respectively). Whereas, for Sargassum vulgare, the extraction with acetone showed higher content (3.04±0.071 mg CE/g of dw). The determination of sugar content showed that acetone extract of the five seaweeds was the richest in sugar, this rate increasingly dropped in ethanol extract and the fractions A and B. The red algae Rhodomela confervoides showed a significant anticoagulant activity in ethanol extract and the fractions A, B, and C, with elongation up to 407.97±58.12 s in the fraction C, at a concentration of 10 mg/mL. Anticoagulant activity was observed in the fractions A, B, and C of all the brown seaweeds. Procoagulant activity was observed in the fractions A and B of Cystoseira humilis and Sargassum vulgare, as well as the fraction B of Padina pavonica for an indeterminate period, at 10 mg/mL. Conclusion: The sulfated polysaccharides present in the fractions A, B and C of the studied marine algae may be responsible for the anticoagulant activity. So, they can be developed as a novel anticoagulant in the pharmaceutical industry.

Objective: Ziziphora clinopodioides is an edible medicinal plant belonging to the Labiatae family that is widespread all over Iran. It used in culinary and also in cold and cough treatments in Iran. The aim of the present work was to evaluate the effect of different timeframes during hydrodistillation on essential oil composition, antimicrobial and antioxidant activity. Materials and Methods: The essential oil of Z. clinopodiodes was extracted via hydrodistillation with Clevenger apparatus. The fractions of essential oil were captured at 6 times from the beginning of the distillation: (10, 20, 60, 120, 180 and 240 min). The fractions of essential oil were analyzed by GC/MS and their antibacterial, antifungal and antioxidant activities were studied by Disk - well diffusion and DPPH methods, respectively. Results: Six distillation times and whole essential oil were captured during hydrodistillation. Essential oil yield dropped off significantly during distillation progressed (1.0% for 10 min and 0.025 for 240 min). 1,8 Cineol, Isomenthone, Pulegone, Piperitenone and Citronellic acid were major compounds in fractions and they were affected by distillation times. Pulegone was a major compound in all of the essential oils. In antioxidant activity assay, whole essential oil was stronger than positive control and fractions of essential oil, because of higher levels of Isomenthone, Piperitenone and Citronellic acid. Strongest antimicrobial activity against S. aureus, E. coli and C. albicans was observed from 10 min fraction. Conclusion: Our results indicated that distillation time can create essential oils with specific properties and we can achieve more efficient essential oil in short times.

Background: Oxadiazole derivatives are the biologically active heterocyclic compounds. Thus, we synthesized a series of Mannich bases, 3-(arylaminomethyl)-5-(pyridin- 4-yl)-1,3,4-oxadiazole-(3H)-thi-2-one derivatives(3a-3g) were synthesized from Isoniazid [INH (1)], a first line antimycobacterial drug, and these compounds were evaluated as antimycobacterial agents. Methods: The INH was reacted with potassium hydroxide and carbon disulfide to give 5-(pyridin- 4-yl)-1,3,4-oxadiazole-2(3H)-thione (2), followed by reacting compound 2 with appropriate aromatic amines in the presence of formaldehyde to obtain desired compounds (3a-3g). The structures of these compounds have been established by IR, ¹H-NMR, Mass spectral and elemental analysis. These synthesized compounds (3a-3g) were evaluated for their antimycobacterial activity against M. tuberculosis H37Rv strain. Results: All the synthesized compounds (3a-3g) exhibited antimycobacterial activity and were compared to reference drugs Streptomycin (MIC value of 6.25μg/mL), INH (MIC value of 3.125μg/mL) and pyrazinamide (MIC value of 3.125μg/mL). Compounds 3c and 3e exhibited the most promising antimycobacterial activity. Conclusion: All the title compounds were synthesized and exhibited promising antimycobacterial activity against M. tuberculosis H37Rv strain.

Background: Huperzia phlegmaria has been used for the treatment of the neurological disorder. Alkaloids are the main bioactive compounds found in Huperzia phlegmaria. We aimed to investigate the Acetylcholinesterase (AChE) inhibitory activity in vitro of Huperzia phlegmaria Alkaloid Extract (HpAE) and protective effects on mice that were induced cognitive deficits by scopolamine. Methods: AChE inhibitory activity and kinetic inhibition mechanism were investigated by Ellman's assay. Mice were administrated orally HpAE (30 mg/kg and 60 mg/kg) for fourteen days, injected scopolamine at a dose of 3 mg/kg one day for Y- maze test and 1 mg/kg four days for Morris water maze test intraperitoneally to induce cognitive impairment. The Y-maze and the Morris water maze were used for evaluating memory behaviors. Acetylcholine (ACh) levels and AChE activity were measured in brain tissue. Glutathione Peroxidase (GPx), Superoxide Dismutase (SOD) activities, and Malondialdehyde (MDA) groups were also evaluated in the mouse brain tissues. Results: Our data showed that HpAE had a strong AChE inhibitory activity with an IC50 value of 5.12 ± 0.48 μg/mL in a concentration-dependent manner. Kinetic inhibition analysis demonstrated that HpAE inhibited AChE followed the mixed inhibition type with Ki (representing the affinity of the enzyme and inhibitor) was 4.37 ± 0.35 μg/mL. Scopolamine induced the cognitive impairment in the Morris Water Maze and Y-maze test along with reduced brain levels of ACh and antioxidant enzyme and increased AChE activity in mouse brain tissues. Treatment with HpAE at both doses (30 mg/kg and 60 mg/kg) decreased the SCP-induced cognitive impairment in both behavioral tests along with decreased acetylcholinesterase activity and MDA level, and increased ACh level and antioxidant enzyme in mouse brain tissues. Conclusion: Our results suggested that the HpAE at both doses (30 mg/kg and 60 mg/kg) may be used for prevention and treatment of Alzheimer’s disease.