scholarly journals South Africa’s Best BARK Medicines Prescribed at the Johannesburg Muthi Markets for Skin, Gut, and Lung Infections: MIC’s and Brine Shrimp Lethality

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 681
Author(s):  
Gugulethu P. Khumalo ◽  
Nicholas J. Sadgrove ◽  
Sandy F. Van Vuuren ◽  
Ben-Erik Van Wyk
Keyword(s):  
South Africa ◽  
Brine Shrimp ◽  
Bark Extract ◽  
Respiratory Pathogens ◽  
Medicinal Uses ◽  
Brine Shrimp Lethality ◽  
Sclerocarya Birrea ◽  
Lung Infections ◽  
Tract Infections

Indigenous trade of medicinal plants in South Africa is a multi-million-rand industry and is still highly relevant in terms of primary health care. The purpose of this study was to identify today’s most traded medicinal barks, traditionally and contemporaneously used for dermatological, gastrointestinal, and respiratory tract infections; then, to investigate the antimicrobial activity and toxicity of the respective extracts and interpret outcomes in light of pharmacokinetics. Thirty-one popularly traded medicinal barks were purchased from the Faraday and Kwa Mai-Mai markets in Johannesburg, South Africa. Information on the medicinal uses of bark-based medicines in modern commerce was recorded from randomly selected traders. The minimum inhibitory concentration (MIC) method was used for antimicrobial screening, and brine shrimp lethality was used to determine toxicity. New medicinal uses were recorded for 14 bark species. Plants demonstrating some broad-spectrum activities against tested bacteria include Elaeodendron transvaalense, Erythrina lysistemon, Garcinia livingstonei, Pterocelastrus rostratus, Rapanea melanophloeos, Schotia brachypetala, Sclerocarya birrea, and Ziziphus mucronata. The lowest MIC value of 0.004 mg/mL was observed against Staphylococcus epidermidis for a dichloromethane bark extract of E. lysistemon. The tested medicinal barks were shown to be non-toxic against the Artemia nauplii (brine shrimp) bioassay, except for a methanol extract from Trichilia emetica (69.52% mortality). Bacterial inhibition of bark extracts with minimal associated toxicity is consistent with the safety and valuable use of medicinal barks for local muthi market customers. Antimicrobial outcomes against skin and gastrointestinal pathogens are feasible because mere contact-inhibition is required in vivo; however, MIC values against respiratory pathogens require further explaining from a pharmacokinetics or pharmacodynamics perspective, particularly for ingested rather than smoked therapies.

scholarly journals Pharmacokinetics of EDP-420 after Multiple Oral Doses in Healthy Adult Volunteers and in a Bioequivalence Study

2009 ◽  
Vol 53 (8) ◽  
pp. 3218-3225 ◽  
Author(s):  
Li-Juan Jiang ◽  
Yat Sun Or
Keyword(s):  
Systemic Exposure ◽  
Bioequivalence Study ◽  
Respiratory Pathogens ◽  
Capsule Formulation ◽  
Dose Study ◽  
Effect Of Food ◽  
Tract Infections ◽  
Oral Doses

ABSTRACT EDP-420 (also known as EP-013420, or S-013420) is a first-in-class bridged bicyclolide currently in clinical development for the treatment of respiratory tract infections (RTI) and has previously shown favorable pharmacokinetic (PK) and safety profiles after the administration of single oral doses of a suspension to healthy volunteers. Here we report its PK profile after the administration of multiple oral doses of a suspension to healthy adults. Bioequivalence between suspension and capsule formulations, as well as the effect of food, is also reported. The most important PK features of EDP-420 observed in these clinical studies are its long half-life of 17 to 18 h and its high systemic exposure, which support once-daily dosing and treatment durations potentially shorter than those of most other macrolide antibiotics. EDP-420 is readily absorbed following oral administration in both suspension and capsule formulations. In the multiple-oral-dose study, steady state was achieved on day 1 by using a loading dose of 400 mg/day, followed by 2 days of 200 mg/day. A high-fat meal had no effect on the bioavailability of EDP-420 administered in a capsule formulation. EDP-420 was well tolerated, with no serious or severe adverse events reported, and no subject was discontinued from the study due to an adverse event. Based on its human PK and safety profiles, together with its in vitro/in vivo activities against common respiratory pathogens, EDP-420 warrants further development, including trials for clinical efficacy in the treatment of RTI.

Pengaruh Penggunaan Jenis Pelarut dalam Uji Sitotoksistas Metode Brine Shrimp Lethality Test (BSLT) pada Wound Dressing Kolagen-Kitosan

al-Kimiya ◽  
2021 ◽  
Vol 8 (1) ◽  
pp. 15-20
Author(s):  
Ary Andini ◽  
Endah Prayekti ◽  
Fadillah Triasmoro ◽  
Indah Nur Kamaliyah
Keyword(s):  
Brine Shrimp ◽  
Wound Dressing ◽  
Artemia Salina ◽  
Lethal Concentration ◽  
Brine Shrimp Lethality

Kolagen dan kitosan dapat digunakan sebagai bahan pembalut luka karena memiliki karakteristik yang baik. Namun, pembalut luka kolagen-kitosan perlu dilakukan uji sitotoksisitas sebelum diaplikasikan secara in vivo, seperti Brine Shrimp Lethally Test (BSLT). Pembalut luka kolagen-kitosan tidak dapat larut dalam Dimetil Sulfoksida (DMSO) dan aquadest dengan mudah, oleh karena itu perlu pertimbangan alternatif pelarut karena kolagen dan kitosan lebih mudah larut dalam pelarut asam seperti asam klorida (HCl) dan asam asetat ( CH3COOH). Penelitian ini bertujuan untuk mengetahui Lethal Concentration  50 (LC50) dari pembalut luka kolagen-kitosan yang dilarutkan dalam pelarut DMSO, HCl, CH3COOH dengan metode Brine Shrimp Lethality Test (BSLT). Pembalut luka kolagen-kitosan didapatkan dengan mencampurkan larutan kitosan 2% dan kolagen dengan perbandingan 1:1 w/w kemudian dihomogenkan, dicetak, dan dikeringkan.  Penelitian ini menggunakan uji sitotoksisitas dengan metode BSLT dan LC50 dihitung menggunakan Analisis Probit. Pembalut luka dilarutkan dalam pelarut DMSO 1%, CH3COOH 1%, dan HCl 1% hingga homogen, kemudian diencerkan dengan berbagai konsentrasi yaitu 100 ppm, 250 ppm, 250 ppm, 500 ppm, dan 1000 ppm dengan tiga kali ulangan untuk setiap perlakuan. Setelah itu uji BSLT dilakukan dengan menggunakan Artemia salina. Hasil penelitian menunjukkan bahwa pembalut luka yang dilarutkan dalam DMSO 1% memiliki LC50 > 1000 ppm, sedangkan pada pelarut CH3COOH dan pelarut  HCl menunjukkan  LC50< 30. Kesimpulan dari penelitian ini adalah pelarut DMSO bersifat non-toksik (LC50  > 1000 ppm), tetapi pelarut CH3COOH 1% dan HCl 1% bersifat sangat toksik (LC50 < 30 ppm) sebagai pelarut alternatif pembalut luka kolagen-kitosan pada uji BSLT.

scholarly journals Brine Shrimp Lethality Assay of the Aqueous and Ethanolic Extracts of the Selected Species of Medicinal Plants

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 47
Author(s):  
Sandeep Waghulde ◽  
Mohan K. Kale ◽  
VijayR. Patil
Keyword(s):  
Medicinal Plants ◽  
Brine Shrimp ◽  
Pharmacological Effects ◽  
Bioactive Components ◽  
Pharmacological Activities ◽  
Brine Shrimp Lethality ◽  
Brine Shrimp Lethality Assay ◽  
Ethanolic Extracts ◽  
Annona Reticulata

The present study was conducted to test for in vivo Brine Shrimp Lethality Assay (BSLA) of the Aqueous and ethanolic extracts of Annona reticulata with Allium fistolisum and Brassica oleraceaeand correlate cytotoxicity results with known pharmacological activities of the plants. Cytotoxicity was evaluated in terms of LC50 (lethality concentration). Ten nauplii were added into three replicates of each concentration of the plant extract. After 24 h the surviving brine shrimp larvae were counted and LC50 was assessed. Results showed that the extracts of Annona reticulata with Allium fistolisumand Brassica oleraceaewere potent against the brine shrimp when compared alone with combined extracts. It indicated that bioactive components are present in these plants that could be accounted for its pharmacological effects. Thus, the results support the uses of these plant species in traditional medicine.

scholarly journals Macrolones Are a Novel Class of Macrolide Antibiotics Active against Key Resistant Respiratory PathogensIn VitroandIn Vivo

2016 ◽  
Vol 60 (9) ◽  
pp. 5337-5348 ◽  
Author(s):  
Hana Čipčić Paljetak ◽  
Donatella Verbanac ◽  
Jasna Padovan ◽  
Miroslava Dominis-Kramarić ◽  
Željko Kelnerić ◽  
...  
Keyword(s):  
Murine Model ◽  
Bacterial Resistance ◽  
Volume Of Distribution ◽  
Macrolide Antibiotics ◽  
Respiratory Pathogens ◽  
Protein Synthesis Inhibitors ◽  
Content Type ◽  
Tract Infections

ABSTRACTAs we face an alarming increase in bacterial resistance to current antibacterial chemotherapeutics, expanding the available therapeutic arsenal in the fight against resistant bacterial pathogens causing respiratory tract infections is of high importance. The antibacterial potency of macrolones, a novel class of macrolide antibiotics, against key respiratory pathogens was evaluatedin vitroandin vivo. MIC values againstStreptococcus pneumoniae,Streptococcus pyogenes,Staphylococcus aureus, andHaemophilus influenzaestrains sensitive to macrolide antibiotics and with defined macrolide resistance mechanisms were determined. The propensity of macrolones to induce the expression of inducibleermgenes was tested by the triple-disk method and incubation in the presence of subinhibitory concentrations of compounds.In vivoefficacy was assessed in a murine model ofS. pneumoniae-induced pneumonia, and pharmacokinetic (PK) profiles in mice were determined. Thein vitroantibacterial profiles of macrolones were superior to those of marketed macrolide antibiotics, including the ketolide telithromycin, and the compounds did not induce the expression of inducibleermgenes. They acted as typical protein synthesis inhibitors in anEscherichia colitranscription/translation assay. Macrolones were characterized by low to moderate systemic clearance, a large volume of distribution, a long half-life, and low oral bioavailability. They were highly efficacious in a murine model of pneumonia after intraperitoneal application even against anS. pneumoniaestrain with constitutive resistance to macrolide-lincosamide-streptogramin B antibiotics. Macrolones are the class of macrolide antibiotics with an outstanding antibacterial profile and reasonable PK parameters resulting in goodin vivoefficacy.

IN VIVO AND IN VITRO EVALUATION OF PHARMACOLOGICAL ACTIVITIES OF Hedychium coccineum RHIZOMES EXTRACT

2021 ◽  
Vol 9 (3) ◽  
pp. 335-342
Author(s):  
Sadia Islam Nishi ◽  
◽  
Niloy Barua ◽  
Mohammed Aktar Sayeed ◽  
Abu Montakim Tareq ◽  
...  
Keyword(s):  
Gastrointestinal Motility ◽  
Brine Shrimp ◽  
Castor Oil ◽  
Anthelmintic Activity ◽  
Tubifex Tubifex ◽  
Clot Lysis ◽  
Thrombolytic Activity ◽  
Brine Shrimp Lethality

The study reports the in vivo antidiarrheal and in vitro anthelmintic, cytotoxic, and thrombolytic activity of methanol extract of Hedychium coccineum rhizomes (MEHC). The antidiarrheal activity was determined using Castor oil-induced diarrhea and Gastrointestinal motility test in mice at the doses of 200 and 400 mg/kg body weight, whereas an aquarium worm, Tubifex tubifex, was used to determine the anthelmintic activity. The cytotoxic and thrombolytic activity of MEHC was performed by Brine shrimp lethality bioassay and clot lysis method respectively. In antidiarrheal, castor oil-induced diarrhea and gastrointestinal motility exhibited a significant reduction in diarrhea and defecation and an extremely significant inhibition in intestinal motility and peristalsis index by 200 and 400 mg/kg of MEHC. The MEHC (5, 10, and 20 mg/mL) showed a significant dose-dependent manner paralysis time and times to death in multiple comparisons to the different levamisole concentrations (0.5, 0.8, and 1 mg/mL) at in vitro anthelmintic activity. The brine shrimp lethality bioassay exhibited a weak LC50 (681.95 µg/mL; R² = 0.951) while in thrombolytic a significant percentage of clot lysis (32.70%, P < 0.05) demonstrated. The findings demonstrate that H. coccineum rhizomes could be potential sources for biological activity.

scholarly journals Uji Aktivitas Sitotoksik dan Analisis Fitokimia Ekstrak Etanol Daun Sampare (Glochidion sp.)

2018 ◽  
Vol 9 (2) ◽  
pp. 49-54
Author(s):  
Ganis Oktalia ◽  
Linus Y. Chrystomo ◽  
Aditya K. Karim
Keyword(s):  
Herbal Medicine ◽  
Key Words ◽  
Brine Shrimp ◽  
Chemical Substance ◽  
Phytochemical Analysis ◽  
Phytochemical Screening ◽  
Brine Shrimp Lethality ◽  
In Vivo Test ◽  
Phytochemical Compounds

Sampare (Glochidion sp., Family: Phyllantaceae) is a plant which grows dominant in Biak, Papua. Based on the local wisdom of the community, by hereditary, it can be used as an herbal medicine to treat the malaria disease. This study aims to determine the toxicity of LC50 and to know the phytochemical compounds of extracted leaf of Glochidion sp using ethanol. The Brine Shrimp Lethality Test (BSLT) and phytochemical screening using reagent chemical substance methods were used in this research. The results of this study can be concluded that the toxicity of extracted leaf of Glochidion sp. using ethanol was low, with LC50 = 758.58 ppm and the results of phytochemical analysis showed the existence of the content of alkaloids, flavonoids, saponins, tannins and quinones. But, the steroids and triterpenoids could not be found in the extracted leaf of Glochidion sp using ethanol. Therefore, for further research is needed to isolate the bioactive compounds and in vivo test on the plasmodium, which cause the malaria disease. Key words: Glochidion sp., malaria desease, Brine Shrimp Lethality Test (BSLT), LC50, phytochemical analysis

scholarly journals Phytochemical and Cytotoxic Screening of Selected Medicinal Plants (Byrsocarpus coccineus, Terminalia avicennioides and Anogeissus leiocarpus) Using Brine Shrimp (Artemia salina) Lethality Assay

2020 ◽  
pp. 60-71
Author(s):  
C. E. Ukwade ◽  
O. A. T. Ebuehi ◽  
R. A. Adisa
Keyword(s):  
Medicinal Plants ◽  
Plant Extracts ◽  
Brine Shrimp ◽  
Antioxidant Activities ◽  
Ethanol Extract ◽  
Medicinal Uses ◽  
Brine Shrimp Lethality ◽  
Root Extracts ◽  
Anogeissus Leiocarpus ◽  
Mineral Analyses

Three medicinal plants, were investigated based on their ethno-medicinal uses. Byrsocarpus coccineus (B.C), Terminalia avicennioides (T.A) and Anogeissus leiocarpus (A.L) are used traditionally in the treatment of various ailments in Nigeria. Proximate and mineral analyses were carried out on the leaf, stem and root of the three plants. Phytochemical composition and antioxidant activities of the aqueous, ethanol and pet ether (leaf, stem and root) extracts, of the three plants were determined and the extracts were subjected to cytotoxic screening using the in vivo brine shrimp lethality tests. The proximate and mineral analyses show appreciable dietary nutrients in the three plants. Phytochemical analyses of B.C, T.A and A.L (leaf, stem and root) extracts, showed the presence of bioactive compounds, such as alkaloids, tannins, saponins, flavonoids, steroid and phenol. Antioxidant activities (2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide, lipid peroxidation and reducing power), increase in all the plant extracts in a dose dependent manner. The results of brine shrimp lethality tests indicate that plant extracts of B.C, T.A and A.L except A.L stem aqueous extract (130.72 µg/ml), T.A leaf aqueous (130.15 µg/ml) and root aqueous extracts were moderately cytotoxic, while the others were highly cytotoxic. B. coccineus leaf ethanol extract (17.31 µg/ml) was the most cytotoxic. The result shows that B. coccineus leaf ethanol extract has significant antioxidant activity and is cytotoxic to brine shrimp even at low concentration giving credence to its ethno-medicinal uses.

scholarly journals In Vivo Activity of HSR-903, a New Fluoroquinolone, against Respiratory Pathogens

1998 ◽  
Vol 42 (4) ◽  
pp. 785-788 ◽  
Author(s):  
Satoshi Yoshizumi ◽  
Haruki Domon ◽  
Shuichi Miyazaki ◽  
Keizo Yamaguchi
Keyword(s):  
Streptococcus Pneumoniae ◽  
Respiratory Tract ◽  
Haemophilus Influenzae ◽  
Pharmacokinetic Study ◽  
Clinical Studies ◽  
Respiratory Tract Infections ◽  
Respiratory Pathogens ◽  
Pulmonary Clearance ◽  
Tract Infections

ABSTRACT The in vivo activity of HSR-903, a new fluoroquinolone, against major bacteria which cause respiratory tract infections was evaluated. HSR-903 was active against experimental respiratory tract infections in mice challenged with penicillin-susceptible and penicillin-resistantStreptococcus pneumoniae and Haemophilus influenzae strains. Treatment with HSR-903 reduced the bacterial numbers in infected murine lungs. In accord with the pulmonary clearance results, the rates of survival for mice treated with HSR-903, sparfloxacin, levofloxacin, ciprofloxacin, and benzylpenicillin were 50, 30, 10, 0, and 0%, respectively, 14 days after being infected with penicillin-resistant S. pneumoniae. A pharmacokinetic study with pneumonic mice showed that the levels of HSR-903 in the lungs were seven to eight times higher than those in the plasma. These results indicate that clinical studies of HSR-903 against respiratory tract infections may be warranted.

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