PURIFICATION AND BIOLOGICAL ACTIVITIES OF COMBINATION OF HEMI-SYNTHESIZED THIOSEMICARBAZONES OF MITRACARPUS SCABER ZUCC

Objective: The harvested Mitracarpus Scaber plants are identified in the national herbarium and registered under the number AA. 6252/HLB. During this work, three crude extracts are prepared from three organic solvents, namely dichloromethane; ethanol and hydroethanol in 50/50 v/v proportion. Methods: The respective alkaloid extracts obtained from the corresponding crude extracts served as substrates for the hemi synthesis of thiosemicarbazone totals from thiosemicarbazides. The three hemi-synthesis products obtained were tested on eight (08) strains of germs, namely E. coli ATCC 25922, S. aureus ATCC 25923, E. faecalis ATCC 22921, P. aeruginosa ATCC 27853, C. albicans ATCC 10231, S. typhi, K. pneumoniae and Dermatophilus 146. Results: The ethanolic extract of thiosemicarbazones exhibited the best bioactive activity and was found to be the most selective. By a series of bioguided chromatographies: TLC thin layer chromatography; CPA atmospheric pressure chromatography and medium pressure liquid chromatography. MPLC (medium pressure liquid chromatography), separation on dextran gel: Sephadex® LH20). The use of available spectral data, cross-checked with that of the literature, made it possible to identify and purify three (03) molecules of thiosemicarbazones, making it possible to study the biological activity of their combination. Conclusion: On the basis of results, this work has made it possible to confirm the concept which affirms that medicinal plants are libraries of several thousand molecules.                             Peer Review History: Received 2 December 2019;   Revised 20 December; Accepted 5 January, Available online 15 January 2020 Academic Editor: Ahmad Najib, Universitas Muslim Indonesia,  Indonesia, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 5.5/10 Average Peer review marks at publication stage: 8.0/10 Reviewer(s) detail: Prof. Dr. Ali Gamal Ahmed Al-kaf, Sana'a university, Yemen, [email protected] Prof. Dr. Amani S. Awaad, Prince Sattam Bin Abdulaziz University, Al-Kharj. KSA., [email protected] Similar Articles: ANTIFUNGAL, CYTOTOXIC AND PHYTOTOXICITY OF AERIAL PART OF RANUNCULUS MURICATUS ANTI-INFLAMMATORY AND ANTI-OXIDANT ACTIVITIES OF METHANOL EXTRACT OF BAPHIA NITID

IDENTIFICATION AND QUANTIFICATION OF PHOSPHODIESTERASE-5 INHIBITOR AS FALSIFIED IN ‘‘NATURAL’’ MALAYSIAN HERBAL APHRODISIACS SOLD IN SOME BENINESE MARKETS

Objective: Nowadays, there have been several reports of herbal products falsified with well-known synthetic molecules, leading to harmful health consequences for the consumer. The aim of this study was to assess the profile of ‘natural' herbal aphrodisiacs in the local markets of the municipalities of Cotonou and Abomey-Calavi in Benin and to screen some of them for the presence of additives such as sildenafil and tadalafil. Methods: A non-probability survey was conducted to identify the available aphrodisiacs and their characteristics. Some of them were then selected for analysis. Thin Layer Chromatography (TLC) was adopted for qualitative detection. The TLC positive extracts were then analyzed by HPLC on a C18 column with a mobile phase consisting of a mixture of 0.05M phosphate buffer (pH 5.8), acetonitrile and methanol (30:50:20). The Detection was performed at 290 nm. Results: Seventy-seven aphrodisiacs were identified and from these, 18 were selected for analysis. Six of them were adulterated with tadalafil. The concentration of tadalafil in the samples was 1.7 to 4.6 times higher than the recommended dose of 20 mg. Conclusion: This work opens the door to the need to control ‘‘natural’’ labeled products in order to ensure their quality

Chemical Identification, In vitro Antidiarrheal Potential, and Toxicological Study of the Leaves of Combretum grandiflorum G. Don (Combretaceae), a Beninese Medicinal Plant

Combretum grandiflorum G. Don is traditionally used in ethnic medicines for the treatment of different diseases in Benin. Despite its wide use, no studies have been undertaken on its potential toxicity. The study was designed to assess the antimicrobial activity and potential toxicity of aqueous and hydroethanolic extracts of C. grandiflorum. Qualitative phytochemistry was carried out by a differential staining or precipitation method. The antibacterial and antifungal effects were evaluated by the solid medium diffusion method. Cytotoxicity was evaluated on Artemia salina larvae while acute toxicity was evaluated with Wistar strain rats via the oral route. The qualitative screening revealed the presence in the plants of Polyphenols, Flavonoids, Tannins, catechic and gallic tannins. Both types of extracts inhibited microbial growth. The hydroethanolic extract was active on all the bacterial strains used with a high inhibition diameter compared to the aqueous extract. On strains of Shigella Sonnei and Salmonella spp, the antibacterial effect of the hydroethanolic extract is significantly (p˂0.05) better compared to that of the aqueous extract. Cytotoxicity tests showed no toxic effects at the doses evaluated. At a dose of 2000 mg/kg, the aqueous and hydroethanolic extracts of C. grandiflorum induced neither mortality nor alteration of the physiological parameters of Wistar rats (renal, hepatic parameters, hematological constants, body weight). These extracts therefore do not present acute oral toxicity for Wistar rats at the limit dose of 2000 mg/Kg/bw in Wistar rats. These results justify some therapeutic indications for these plants. They could therefore be used for the development of improved phytomedicines

Formulation and Optimization of Matrix Tablets Based on Spirulina and Vitamin C

Spirulina is a type of algae widely consumed around the world as a dietary supplement due to its great nutritional potential. However, it does not contain vitamin C, a vital vitamin for the proper functioning of the human body, particularly given its immunostimulant potential. The objective of this work was to formulate sustained release spirulina–vitamin C matrix tablets that would enhance particularly a prolonged release and better absorption of vitamin C. A galenic formula based only on vitamin C was made, and then the proportion of vitamin C was reduced in favor of spirulina powder. The manufactured tablets were then subjected to various pharmacopeial quality control tests. The results of these tests showed a good distribution of the powder mixtures in the formulated tablets (i.e., mass uniformity test) and satisfactory outcomes were found for the content uniformity, disintegration and dissolution tests (with 45 % of vitamin C dissolved after 4 hours). Only the results for the friability test were unsatisfactory, indicating the need to improve the physical properties of the powders before compression. These findings open a new area for developing supplementary dietary.            Keywords: Spirulina, Vitamin C, Matrix tablet, Quality control

Fractionation Coupled to Molecular Networking: Towards Identification of Anthelmintic Molecules in Terminalia leiocarpa (DC.) Baill

Terminalia leiocarpa is a medicinal plant widely used in ethnoveterinary medicine to treat digestive parasitosis whose extracts were shown to be active against gastrointestinal nematodes of domestic ruminants. The objective of our study was to identify compounds responsible for this activity. Column fractionation was performed, and the activity of the fractions was assessed in vitro on Haemonchus contortus and Caenorhabditis elegans as well as their cytotoxicity on WI38 fibroblasts. Two fractions were the most active on both nematode models and less cytotoxic. LC-MS/MS analysis and manual dereplication coupled to molecular networking allowed identification of the main compounds: ellagic acid and derivatives, gallic acid, astragalin, rutin, quinic acid, and fructose. Other potentially identified compounds such as shikimic acid, 2,3-(S)-hexahydroxydiphenoyl-D-glucose or an isomer, quercetin-3-O-(6-O-galloyl)-β-D-galactopyranoside or an isomer, and a trihydroxylated triterpenoid bearing a sugar as rosamultin are reported in this plant for the first time. Evaluation of the anthelmintic activity of the available major compounds showed that ellagic and gallic acids were the most effective in inhibiting the viability of C. elegans. Their quantification in fractions 8 and 9 indicated the presence of about 8.6 and 7.1 µg/mg ellagic acid and about 9.6 and 2.0 µg/mg gallic acid respectively. These concentrations are not sufficient to justify the activity observed. Ellagic acid derivatives and other compounds that were found to be positively correlated with the anthelmintic activity of the fractions may have additive or synergistic effects when combined, but other unidentified compounds could also be implicated in the observed activity

Anthelmintic Activity, Cytotoxicity, and Phytochemical Screening of Plants Used to Treat Digestive Parasitosis of Small Ruminants in Benin (West Africa).

Medicinal plants continue to be used alone or in combination with veterinary drugs to treat animal ailments, especially in developing countries where livestock farmers often lack access to modern veterinary services and drugs. In addition, digestive parasitosis remain a major constraint for small ruminant livestock. The objective of this study was to screen the anthelmintic activity of the main plants used in the treatment of the digestive parasitosis of small ruminants in Benin. A total of 40 extracts were prepared using the successive maceration of 10 plants in four solvents of increasing polarity. The phytochemical screening of the plants was performed, and the anthelmintic activity of the extracts was evaluated on L3 larvae of . The cytotoxicity of the 40 extracts was determined on WI38 noncancerous fibroblast cells using the MTT assay, and the total phenol content (TPC), total flavonoid content (TFC), and condensed tannin content (CTC) were quantified in the most effective extracts using colorimetric methods. The results show that the plants contained tannins, flavonoids, and triterpenoids which may, in part, justify their anthelmintic activities. All plants gave active extracts at the highest concentration tested (1200 µg/mL). Methanol (MeOH) extracts were, in general, more effective than the hexane (HEX), dichloromethane (DCM), and aqueous (HO) ones in inhibiting larval migration, with the MeOH extracts of , , and being the most effective. Nevertheless, the MeOH extract of was highly cytotoxic at the concentration of 100 µg/mL. The anthelmintic activity of , , and was studied on for the first time. These results provide scientific information that can be used for better valorization of the anthelmintic potential of the studied plants and to initiate the process of the identification of new anthelmintic molecules