HPLC-DAD Based Polyphenolic Profiling and Evaluation of Pharmacological Attributes of Putranjiva roxburghii Wall.

The current study was intended to explore the phytochemical profiling and therapeutic activities of Putranjiva roxburghii Wall. Crude extracts of different plant parts were subjected to the determination of antioxidant, antimicrobial, antidiabetic, cytotoxic, and protein kinase inhibitory potential by using solvents of varying polarity ranges. Maximum phenolic content was notified in distilled water extracts of the stem (DW-S) and leaf (DW-L) while the highest flavonoid content was obtained in ethyl acetate leaf (EA-L) extract. HPLC-DAD analysis confirmed the presence of various polyphenols, quantified in the range of 0.02 ± 0.36 to 2.05 ± 0.18 μg/mg extract. Maximum DPPH scavenging activity was expressed by methanolic extract of the stem (MeOH-S). The highest antioxidant capacity and reducing power was shown by MeOH-S and leaf methanolic extract (MeOH-L), respectively. Proficient antibacterial activity was shown by EA-L extract against Bacillus subtilis and Escherichia coli. Remarkable α-amylase and α-glucosidase inhibition potential was expressed by ethyl acetate fruit (EA-F) and n-Hexane leaf (nH-L) extracts, respectively. In case of brine shrimp lethality assay, 41.67% of the extracts (LC50 < 50 µg/mL) were considered as extremely cytotoxic. The test extracts also showed mild antifungal and protein kinase inhibition activities. The present study explores the therapeutic potential of P. roxburghii and calls for subsequent studies to isolate new bioactive leads through bioactivity-guided isolation.

Antitumor Potential of Annona muricata Linn. An Edible and Medicinal Plant in Mexico: In Vitro, In Vivo, and Toxicological Studies

Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine.

Essential Oil Blends: The Potential of Combined Use for Respiratory Tract Infections

This study investigated the potential efficacy of 369 commercial essential oil combinations for antimicrobial, anti-toxic and anti-inflammatory activity with the aim of identifying synergy among essential oils commonly used in combination by aromatherapists for respiratory purposes. Essential oil combinations were assessed for their antimicrobial activities using a panel of Gram-positive, Gram-negative, and yeast strains associated with respiratory tract infections. The antimicrobial activity was measured by determining the minimal inhibitory concentration (MIC) of microbial growth. The fractional inhibitory concentration index (ΣFIC) was calculated to determine the antimicrobial interactions between the essential oils in the combination. The toxicity of the essential oil combinations was tested in vitro using the brine shrimp lethality assay, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on RAW 264.7 mouse macrophage cells and A549 lung cancer cell lines. In addition, an inflammatory response was evaluated measuring nitric oxide production. The essential oils, when in combination, demonstrated an increased antimicrobial effect, a reduction in toxicity and provided improved anti-inflammatory outcomes. Five distinct combinations [Cupressus sempervirens (cypress) in combination with Melaleuca alternifolia (tea tree), Hyssopus officinalis (hyssop) in combination with Rosmarinus officinalis (rosemary), Origanum marjorana (marjoram) in combination with M. alternifolia, Myrtus communis (myrtle) in combination with M. alternifolia and Origanum vulgare (origanum) in combination with M. alternifolia] were found to be the most promising, demonstrating antimicrobial activity, reduced cytotoxicity and improved anti-inflammatory effects. With the increased prevalence of respiratory tract infections and the growing antimicrobial resistance development associated with antimicrobial treatments, this study provides a promising complementary alternative for the appropriate use of a selection of essential oil combinations for use in the respiratory tract.

Preparation of Boerhaavia diffusa Mediated Selenium Based Mouthwash-A Comparative Microbial and Cytotoxic Effect

Introduction: The extract of Boerhaavia diffusa root, a plant used in Indian traditional medicine, has significant immunomodulatory Potential. Selenium, a nutrient element that has a massive function in biological systems, is one of the interesting compounds to integrate with antibacterial agents. Recently several studies have pointed out the ability of selenium nanoparticles to exhibit anticancer, antioxidant, antibacterial and antibiofilm properties. Aim: To analyze the antimicrobial and cytotoxic activity of Boerhaavia diffusa mediated selenium nanoparticles based mouthwash. Materials and Methods: 1 g of Boerhavia diffusa was added in 100 ml of distilled water. It was boiled; the plant extract was filtered using Whatman’s no.1 filter paper. In 250 ml conical flask, 60 ml of 20 millimolar sodium selenite was prepared and 40 ml of the filtered plant extract was mixed. This flask was kept in a magnetic stirrer. The nanoparticle solution was centrifuged at 8000rpm to prepare nanoparticle pellets. The nanoparticle pellet was dried in a hot air oven at 80 degree celsius. The dried powder was sent for Characterization. A mouthwash is prepared. The prepared mouthwash was tested for cytotoxic activity by brine shrimp lethality assay and antimicrobial activity evaluated the zone of inhibition of agar well diffusion method. Results and Discussion: It was proved that cytotoxic activity of selenium bound mouthwash was less compared to the commercial mouthwash. The antibacterial activity of the selenium bound mouthwash against C. albicans and S. mutans was significant when compared to the standard antimicrobial agent. Conclusion: Based on the results, this mouthwash has the required qualities to be commercially be used. Therefore further studies can be done to prove that this mouthwash can be used commercially.

Ethnobotanical Documentation, Phytochemical Screening, and Cytotoxicity Evaluation of Medicinal Plants Used to Manage Snakebite Envenomation in Mwingi West Subcounty, Kenya

Snakebite envenomation (SBE) is a life-threatening global public health problem affecting over 2.7 million persons annually, with a bigger burden lying in the developing world. Despite the successful management of SBE by antivenom therapy in conventional medicine, it is of low efficacy due to the diverse venom composition across snake types, which limits its usefulness. As a result, inhabitants of the sub-Sahara region, where SBE incidence is high, utilise medicinal plants as an alternative remedy for SBE. However, most plants have not been ethnobotanically documented and validated empirically and hence this study is needed. An ethnobotanical survey to document medicinal plants used to manage SBE in Migwani ward, Mwingi West Subcounty, Kitui County, was conducted between January and February, 2021. Ethnobotanical data were collected from 45 purposefully sampled respondents from Migwani ward using semistructured questionnaires, field walks, and oral interviews. In this study, 14 medicinal plants which are used to manage SBE were documented. Four plants with the highest Relative Frequency of Citation (RFC) (Entada leptostachya Harms-stem bark (0.58), Senna singueana-roots (0.53), Securidaca longipendunculata-roots (0.36), and Strychnos henningsii-stem bark (0.46)) were selected and extracted using water, methanol, and dichloromethane according to the standard procedures. Qualitative phytochemical analysis of the plant extracts and their cytotoxic effects on brine shrimp nauplii (brine shrimp lethality assay) was conducted according to the standard techniques. Qualitative phytochemical screening revealed the presence of anti-SBE-associated phytochemicals, such as alkaloids, saponins, tannins, phenols, and flavonoids, in the aqueous and methanolic extracts of the studied plant extracts. However, the tested phytochemicals were not detected in dichloromethane extracts of all the studied extracts. The anti-SBE effects of the documented plants could be attributable to these associated bioactive phytocompounds, which are synthesized by the studied plants and transfered to humans when consumed. Furthermore, the aqueous and methanolic extracts of Entada leptostachya and Senna singueana had high LC50 of >1000 µg/ml and were considered noncytotoxic. However, Securidaca longipendunculata had an LC50 of <1000 µg/ml and was considered slightly cytotoxic. Further empirical investigations to characterise the bioactive phytochemicals and their safety should be done.

Antibacterial and Cytotoxic Potential of Two Steroids from the Indonesian Soft Coral Sinularia polydactila

Background: Soft corals of the genus Sinularia are well recognized as a rich source of steroidal compounds. These constituents, mainly steroids, have been reported as possessing antitumor, antimicrobial, and antiviral activities. Objectives: This study was designed to isolate and elucidate antibacterial and cytotoxic compounds from the soft coral Sinularia polydactila. Methods: Structure elucidation of steroids was determined based on spectroscopic data through 1D and 2D NMR analyses and mass spectrometry, with the results compared to data in the literature. Antibacterial activity was determined using four human bacterial pathogens, namely B. subtilis (ATCC 6633), P. aeruginosa (ATCC 27853), S. aureus (ATCC 25923), and E. coli (ATCC 25922). Cytotoxic activity was evaluated using the human colon cancer cell HCT 116 and brine shrimp lethality assay (BSLA). Results: Two steroids (Compounds 1 - 2) were isolated from the Indonesian soft coral Sinularia polydactila. (22R,23R,24R)-22,23-methylene-24-methylcholest-6-en-5α,8α-epidioxy-3β-ol (1) and 5α,8α-Epidioxy-24(R)-methylcholesta-6,22-dien-3α-ol (2) showed moderate activity against colon carcinoma cancer HCT 116 at the concentrations of 24.8 and 27.3 μg/mL, respectively. Furthermore, compounds 1 and 2 showed cytotoxic activity using the brine shrimp lethality assay with the concentrations of 57.1 and 121.3 3 μg/mL, respectively. Compound 2 showed moderate activity against S. aureus and B. subtilis at the 250 μg/mL concentration. Conclusions: Two steroids isolated from soft coral Sinularia polydactila were found to possess moderate cytotoxic and antibacterial activities.

Phytochemical analysis and cytotoxicity evaluation of flowering buds of Bauhinia variegata L.

Summary Introduction: Bauhinia variegata is used in traditional medicine in Pakistan. Objective: The present study was designated to analyze phytochemical screening and cytotoxicity assay of crude aqueous and methanol extracts of flowering buds of Bauhinia variegata. Methods: Qualitative and quantitative phytochemical screening of both extracts were performed by using standard protocols while brine shrimp lethality assay was conducted for cytotoxicity analysis of both extracts. Results: The highest levels of phenolics, flavonoids and terpenoids were observed in methanol extract with respective standard drugs. The aminoacid content was highest followed by phenol and flavonoids in crude aqueous extract of the raw materials. In cytotoxic studies (brine shrimp lethality assay) the use of methanol extract was reported as potent with LD50 of 241.778 µg/ml as compared to aqueous extract with LD50 of 489.7061 µg/ml. Conclusion: This study reveals that the presence of bioactive compounds in both extracts are responsible for the treatment of various ailments and being utilized by the traditional folks as a food as well. And showed that methanol extract possess cytotoxic activity and thus needs further scientific intervention for its value addition.

Phytochemical and pharmacological investigations of different extracts of leaves and stem barks of Macropanax dispermus (Araliaceae): a promising ethnomedicinal plant

Background Macropanax dispermus is traditionally used to treat various diseases by ethnic people. The present research reports the pharmacological properties with phytochemical profiling of the crude extracts of M. dispermus leaves (MDML), its n-hexane (MDHL), carbon tetrachloride (MDTL), chloroform (MDCL), ethyl acetate (MDEL), and aqueous (MDAL) fractions, and crude methanol extracts of its stem barks (MDMS). The in vitro thrombolytic activity was done on human erythrocytes whereas the cytotoxic activity was done by brine shrimp lethality assay. The in vivo analgesic activity was examined by acetic acid-induced writhing, tail immersion, and formalin-induced paw licking method. In contrast, antipyretic activity was done by the brewer’s yeast-induced pyrexia method. Results MDHL and MDMS showed 37.05% and 42.21% of significant (p < 0.01) thrombolytic activity, respectively. MDCL and MDMS showed the lower LC50 values of 23.15 and 37.11 µg/ml during cytotoxicity test, respectively. In acetic acid writhing method, MDTL and MDEL showed significant (p < 0.001) inhibition of writhing by 79.34% and 80.17%, respectively. MDMS showed significant (p < 0.001) maximal possible effect (%MPE) of 45.95%, 62.26%, 65.79%, 89.69% and elongation of time in pain reaction of 48.53%, 60.28%, 58.76%, and 70.14% at 30, 60, 90, and 120 min intervals, respectively. MDML at 400 mg/kg exhibited significant (p < 0.001) 82.72% of inhibition of pain at the late phases. MDEL at 400 mg/kg of dose exhibited significant (p < 0.001) reduction of rectal temperature by 36.31%, 62.42%, 89.81%,, and 96.82% at 1, 2, 3, and 4 h intervals, respectively. Conclusion The current research suggests that the plant extracts possess potential thrombolytic, cytotoxic, analgesic, and antipyretic activities.

New Insights on Euphorbia dendroides L. (Euphorbiaceae): Polyphenol Profile and Biological Properties of Hydroalcoholic Extracts from Aerial Parts

Euphorbia dendroides L. is a rounded shrub commonly found in the Mediterranean area well-known, since ancient times, for its traditional use. The aim of the present study was to investigate the phytochemical profile as well as the antioxidant and anti-inflammatory properties of flower (FE), leaf (LE), fruit (FrE), and branch (BE) hydroalcoholic extracts. For this purpose, a preliminary phytochemical screening followed by RP-LC-DAD-ESI-MS analysis, as well as several in vitro cell-free colorimetric assays, were carried out. Moreover, the toxicity of the extracts was investigated by the brine shrimp lethality assay. All extracts showed a high content of polyphenols, in particular phenolic acids (chlorogenic acid 0.74–13.80 g/100 g) and flavonoids (rutin 0.05–2.76 g/100 g and isovitexin 8.02 in BE). All the extracts showed strong and concentration-dependent antioxidant and anti-inflammatory activity with, on average, the following order of potency: FE, LE, FrE, and BE. Interestingly, all the extracts investigated did not show any toxicity on Artemia salina. Moreover, the only LD50 found (BE, 8.82 mg/mL) is well above the concentration range, which has been shown the biological properties. Considering this, this study offers the first evidence of the possible use of the polyphenol extracts from the aerial parts of E. dendroides as promising antioxidant and anti-inflammatory agents.

Phytochemical Analysis and Investigation of the Antimicrobial and Cytotoxic Activities of Croton dichogamus Pax Crude Root Extracts

Background. Increasing antimicrobial resistance has led to an arduous search for new potent drugs from nature. In this search, plants have proved to be rich reservoirs of efficacious medicinal components that manage ailments. The current study is designed to investigate the phytochemical composition, antimicrobial activity, and the cytotoxicity of the crude root extracts of Croton dichogamus, a shrub that is commonly used in the eastern Africa for the management of infectious diseases. Methods. The roots of Croton dichogamus were obtained, dried, ground, and extracted using three solvents (acetone, distilled water, and 50% ethanol). The antimicrobial activity was tested using agar well diffusion and microbroth dilution techniques against five human pathogens. The brine shrimp lethality assay was used to assess the toxic effect. Results. The phytochemical screening indicated the presence of terpenoids, flavonoids, tannins, phenols, polyuronides, saponins, and anthracenes. The brine shrimp lethality assay indicated that all the extracts were highly cytotoxic with LC50 values below 100 μg/ml. Acetonic extract had an LC50 value of 4.148 μg/ml, hydroethanolic extract had 76.09 μg/ml, and aqueous extract had 42.61 μg/ml. All extracts showed the antibacterial activity against Gram-positive bacteria (B. cereus and S. aureus) and a fungal organism, C. albicans. The extracts showed no antibacterial effect on the Gram-negative bacterial strains (P. aeruginosa and E. coli) at a concentration of 250 mg/ml. The highest antimicrobial activity was demonstrated by the acetonic extract on B. cereus which had an MIC of 10.42 mg/ml and a zone of inhibition of 17.33 ± 0.58 at a concentration of 250 mg/ml. Conclusion. In this research work, we report that C. dichogamus had the antimicrobial activity confirming the folklore claim. The results made a strong case for isolation of novel anticancer lead compounds.