Medicinal herbs and their metabolites with biological potential to protect and combat liver toxicity and its disorders: A review.

The liver is an essential organ that helps the body with immunity, metabolism, and detoxification, among other functions. Worldwide, liver illnesses are a leading cause of mortality and disability. There are few effective treatment choices, but they frequently have unfavorable side effects. Investigating the potential of medicinal plants and their bioactive phytoconstituents in the prevention and treatment of liver disorders has gained more attention in recent years. An assessment of the hepatoprotective potential of medicinal plants and their bioactive secondary metabolites is the goal of this thorough review paper. To determine their hepatoprotective activity, these plants were tested against liver toxicity artificially induced in rats, mice and rabbits by chemical agents such as carbon tetrachloride (CCl4), paracetamol (PCM), thioacetamide (TAA), N-nitrosodiethylamine, d-galactosamine/lipopolysaccharide, antitubercular medicines (rifampin, isoniazid) and alcohol. To find pertinent research publications published between 1989 and 2022, a comprehensive search of electronic bibliographic databases (including Web of Science, SpringerLink, ScienceDirect, Google Scholar, PubMed, Scopus, and others) was carried out. The investigation comprised 203 plant species from 81 families in total. A thorough discussion was mentioned regarding the hepatoprotective qualities of plants belonging to several families, such as Fabaceae, Asteraceae, Lamiaceae, and Euphorbiaceae. The plant groups Asteraceae and Fabaceae were the most frequently shown to have hepatoprotective properties. The phytochemical constituents namely flavonoids, phenolic compounds, and alkaloids exhibited the highest frequency of hepatoprotective action. Also, some possible mechanism of action of some active constituents from medicinal plants was discussed in brief which were found in some studies. In summary, the information on medicinal plants and their potentially hepatoprotective bioactive phytoconstituents has been consolidated in this review which emphasizes the importance of further research to explore the efficacy and safety of these natural remedies for various liver ailments.

Introduction of chirality at C1 position of 1-substituted-3,4-dihydroisoquinoline by its enantioselective reduction: synthesis of chiral 1-substituted-1,2,3,4-tetrahydroisoquinoline - a review.

There is a wide range of biological activities associated with C1 chiral carbon containing 1-substituted-1,2,3,4-tetrahydroisoquinolines (1-substituted-THIQs) which constitute the isoquinoline alkaloids, a large group of natural products. This work summarizes several novel catalytic stereoselective approaches to enantioselectively reduce the 1-substituted-3,4-dihydroisoquinolines (1-substituted-DHIQs) to produce the desired 1-substituted-THIQs. The 1-substituted-DHIQs were prepared by using the Bischler-Napieralski reaction. The enantioselective reduction of 1-substituted-DHIQs was accomplished by using chiral hydride reducing agents, by hydrogenation with a chiral catalyst, by enantioselective reduction of DHIQs possessing a chiral auxiliary at the imine nitrogen by achiral metallic hydride reducing agents, or by enzymatic catalysis. Among these methods, much more work was carried out on the hydrogenation of 1-substituted-DHIQs in the presence of a chiral catalyst. This review summarizes articles and advancements on this topic from 1972 to 2023.

An insight into the anti-ulcerogenic potentials of medicinal herbs and their bioactive metabolites.

ETHNOPHARMACOLOGICAL RELEVANCE: Peptic ulcer disease (PUD) ranks top among the most prominent gastrointestinal problems prevalent around the world. Long-term use of non-steroidal anti-inflammatory drugs, pathogenic infection by Helicobacter pylori, imbalances between gastrointestinal regulatory factors and pathological hyperacidity are major contributors towards the development of peptic ulcers. Although synthetic drugs of multiple pharmacological classes are abundantly available, inadequacy of such agents in ensuring complete recovery in not uncommon. Therefore, pharmacological explorations of herbal products including plant extracts and their respective isolated phytoconstituents, for potential gastroprotective and antiulcer properties, are regular practice among the scientific community. Moreover, the historical preferences of a significant share of world population towards herbal-based medication over modern synthetic drugs also contribute significantly to such endeavors. AIM OF THE REVIEW: This review has endeavored to present ethnomedicinal and pharmacological prospects of a significant number of authenticated plant species in terms of their capacity to exert gastroprotection and antiulcer activities both in vitro and in vivo. The information delineated along the way was further subjected to critical analysis to ascertain the possible future prospects of such findings into designing plant-derived products in future for the treatment of peptic ulcer. MATERIALS AND METHODS: Electronic version of prominent bibliographic databases, including Google Scholar, PubMed, Scopus, ScienceDirect, Wiley Online Library, SpringerLink, Web of Science, and MEDLINE were explored extensively for the identification and compilation of relevant information. The plant names and respective family names were verified through the Plant List (version 1.1) and World Flora Online 2021. All relevant chemical structures were verified through PubChem and SciFinder databases and illustrated with ChemDraw Ultra 12.0. RESULTS: A colossal number of 97 plant species categorized under 58 diverse plant families have been discussed in the review for their gastroprotective and antiulcer properties. In vivo illustrations of the pharmacological properties were achieved for almost all the species under consideration. 29 individual phytoconstituents from these sources were also characterized with similar pharmacological potentials. Majority of the plant extracts as well as their constituents were found to exert their gastroprotective effects through antioxidative pathway featuring both enzymatic and nonenzymatic mechanism. Moreover, active inhibition of acid secretion, upregulation of gastroprotective mediators and downregulation of pro-inflammatory cytokines, were also associated with a prominent number of plants or products thereof. CONCLUSIONS: Comparative evaluations of the plant sources for their antiulcer activities, both as individual and as combination formulations, are necessary to be conducted in human subjects under properly regulated clinical conditions. Moreover, the efficacy and safety of such products should also be evaluated against those of the currently available treatment options. This will further facilitate in ascertaining their suitability and superiority, if any, in the treatment of peptic ulcer diseases. Implementation of these endeavors may eventually lead to development of more efficient treatment options in the future.

Phytochemical investigations and antioxidant potential of roots of Leea macrophylla (Roxb.).

BACKGROUND: Oleanolic acid (NZ-15), 7 α, 28-olean diol (NZ-38) and Stigmasterol (NZ-14) were isolated from the ethanolic extracts of the roots of Leea macrophylla (Family: Leeaceae) by using chromatographic analysis. This is the first report of isolation of these compounds from this plant. Their structures were constructed by spectroscopic analysis and by comparing the data with the published one. Subsequently the ethanolic extract was fractionated with two organic solvents and all the fractions were studied to evaluate their in vitro antioxidant property. METHODS: The ethanolic extract was fractionated with two organic solvents and all the fractions were studied to evaluate their in vitro antioxidant property by DPPH free radical scavenging assay, superoxide anion radical scavenging assay, nitric oxide radical scavenging assay, and reducing power assay. RESULTS: In the DPPH free radical scavenging assay and superoxide radical scavenging assay, the ethyl acetate soluble fraction of ethanolic extract revealed the highest free radical scavenging activity with IC50 value of 2.65 and 155.62 µg/ml, respectively as compared to standard ascorbic acid (IC50 value of 5.8 and 99.66 µg/ml). Ethyl acetate fraction also possessed highest reducing power activity with an EC50 value of 15.27 µg/ml compared to ascorbic acid (EC50 0.91 µg/ml). On the other hand, the carbon tetrachloride fraction exhibited most significant NO scavenging activity with IC50 value of 277.8 µg/ml that was even higher than that of standard ascorbic acid (IC50 value 356.04 µg/ml). In addition, the total phenolic contents of these extract and fractions were evaluated using Folin-Ciocalteu reagent and varied from 7.93 to 50.21 mg/g dry weight expressed as gallic acid equivalents (GAE). CONCLUSIONS: This study showed that different extracts of roots of L. macrophylla possess potential DPPH, superoxide, and NO free radical scavenging activities. The antioxidant activities of the plant extracts might be due to the presence of oleanolic acid, oleanolic acid derivative 7 α, 28-olean diol and stigmasterol.

In vivo analgesic, antipyretic and anti-inflammatory potential of leaf extracts and fractions of Eria javanica.

Background The objective of the study was to evaluate the antinociceptive, antipyretic and anti-inflammatory activities of ethanolic extract, methanolic extract and n-hexane and chloroform-soluble fractions of methanolic extract of Eria javanica leaves in animal model (rat and mice). Methods The anti-nociceptive potentials of the extracts were studied using the acetic acid-induced writhing test in mice and the antipyretic activity was investigated using yeast-induced pyrexia in rats. Anti-inflammatory activity test was done on rats at a dose by using carrageenan-induced paw edema test. Results In acetic acid-induced writhing inhibition study in Swiss albino mice, the crude methanolic extract at 200 mg/kg and 400 mg/kg doses and the n-hexane soluble fraction of crude methanolic extract at 400 mg/kg showed statistically significant activity with 53.21 % (p<0.001), 50.36 % (p<0.001) and 67.86 % (p<0.001) inhibition respectively compared to control. The crude ethanolic extract showed statistically significant antipyretic activity from 1 hours and onwards after administration at doses of 200 mg/kg body weight (p<0.005 at 1st hour and p<0.001 at 2nd, 3rd and 4th hour respectively) and 400 mg/kg body weight (p<0.05 at 1st hour and p<0.001 at 2nd, 3rd and 4th hour respectively). The crude methanolic extract showed statistically significant antipyretic activity from 2 hours and onwards at 400 mg/kg body weight (p<0.05 at 2nd hour and p<0.001 at 3rd and 4th hour respectively) and 200 mg/kg body weight dose showed statistically significant antipyretic activity from 3 hours and onward(p<0.001) in Brewer's yeast-induced pyrexia test in albino Wister rats. In carrageenan-induced rat's paw edema test, crude methanolic extract showed statistically significant anti-inflammatory activity from 2nd hour and onwards. The chloroform-soluble fraction of methanolic extract also showed significant activity from 1st hour onwards. Conclusions This study thereby indicates that leaves of E. javanica possess peripheral analgesic, antipyretic and anti-inflammatory activities and therefore a suitable candidate for further study.

Ethnopharmacological investigation of the aerial part of Phragmites karka (Poaceae).

BACKGROUND: In this ethnopharmacological study, methanolic extract of the aerial plant parts of Phragmites karka (Family: Poaceae) and its petroleum ether and carbon tetrachloride fractions were investigated for bioactivities in Swiss-albino mice, namely, analgesic, central nervous system (CNS) depressant, hypoglycemic, and antidiarrheal activity. METHODS: The cold methanolic extract of the aerial plant parts of Phragmites karka (MEPK) was first prepared, and it was then further fractionated as petroleum ether (PEFMEPK) and carbon tetrachloride (CTFMEPK) fractions. Analgesic activity was performed employing acidic acid-induced writhing test, central analgesic effect by radiant heat tail-flick method. CNS depressant activity was evaluated by phenobarbitone-induced sleeping time test. Hypoglycemic activity was tested by glucose tolerance test (GTT). Antidiarrheal activity was evaluated by castor oil-induced diarrhea method. For all in vivo tests, doses of 200 and 400 mg/kg body weight were used. RESULTS: In the mice model, the MEPK, PEFMEPK, and CTFMEPK fractions showed significant peripheral analgesic activity at a dose of 400 mg/kg body weight with percentage of inhibition of acetic acid-induced writhing 77.67 (p<0.001), 33.50 (p<0.001), and 40.29 (p<0.001), respectively, compared to the standard dichlofenac (60.68%, p<0.001) group. The hypoglycemic properties of MEPK, PEFMEPK, and CTFMEPK extracts were evaluated in normoglycemic mice where the reduction of blood glucose level after 30 min of glucose load were 69.85%, 78.91%, and 72.73%, respectively, and for standard glibenclamide, the reduction was 72.85%. All results were significant (p<0.05). In the case of the CNS depressant activity by phenobarbitone-induced sleeping time test, the crude ME significantly reduced sleep latency by 57.14% and increased the duration of sleep by 63.29% compared to the control, which were comparable to that of standard diazepam (65.71% and 77.62%, respectively). Among all the extract and fractions, methanolic extract showed the maximum antidiarrheal effect. The methanolic extract at 200 mg/kg dose induced a significant decrease in the total number of defecation in 4 h (69.05% of inhibition, p<0.001) and at 400 mg/kg dose showed 76.19% of inhibition (p<0.001). CONCLUSIONS: In light of the available literature, these findings represent the first experimental investigation of biological activities of P. karka in the perspective of their traditional use.

Evaluation of analgesic, anti-inflammatory, thrombolytic and hepatoprotective activities of roots of Premna esculenta (Roxb).

BACKGROUND: The objective of this study was to investigate the antinociceptive, anti-inflammatory, thrombolytic and hepatoprotective activities of root extracts of Premna esculenta (family: Verbenaceae). METHODS: The analgesic activity was evaluated using the acetic-acid-induced writhing test in mice and radiant heat tail-flick method in rats. The anti-inflammatory activity was investigated by carrageenan-induced rat's paw edema, while the thrombolytic activity was evaluated by in vitro clot lysis model. The hepatoprotective activity was investigated against carbon-tetrachloride-induced liver damage in rats. RESULTS: In acetic-acid-induced writhing test, chloroform and ethyl acetate fraction of ethanolic extract at a dose of 200 mg/kg showed a significant (p<0.001) reduction in the number of writhes with 85.96% and 61.98% of inhibition, respectively. In radiant heat tail-flick method, the ethanolic extract produced 88.49% (p<0.001) elongation of tail-flicking time at 90 min after oral administration at same dose level. In the carrageenan-induced edema test, the ethanolic extract at a dose of 200 mg/kg showed a significant inhibition of paw edema with 22.68% and 17.24% inhibition after the first and third hours of the study period, respectively. In clot lysis model, the ethanolic extract at 5 mg/mL induced a significant clot lysis activity (37.69%, p<0.001). Oral administration of ethanolic extract at the dose of 400 mg/kg/day for 7 days significantly (p<0.001) reduced the elevated levels of serum glutamic pyruvic transaminase, serum glutamyl oxaloacetate transaminase and alkaline phosphatase compared to the CCl4-treated control group. CONCLUSIONS: The results of the study demonstrated the antinociceptive, anti-inflammatory, thrombolytic and hepatoprotective activities of roots of P. esculenta.

Antinociceptive, anti-inflammatory, antimicrobial and central nervous system depressant activities of ethanolic extract of leaves and roots of Gomphostemma parviflorum var. parviflorum wall.

BACKGROUND: Gomphostemma parviflorum (Lamiaceae) is a medicinal plant of Bangladesh which has been used traditionally in the treatment of painful and inflammatory conditions such as asthma, headache, fever, etc. OBJECTIVE: To investigate the antinociceptive, anti-inflammatory, central nervous system (CNS) depressant and antimicrobial activities of ethanolic extracts of leaves (GPLE) and roots (GPRE) of the plant. MATERIALS AND METHODS: The antinociceptive potentials of the extracts were studied using acetic acid-induced writhing test in mice, anti-inflammatory activity was investigated using carrageenan-induced paw edema in rats, CNS depressant activities were evaluated using pentobarbitone-induced sleeping time, Hole cross and Open field tests in mice while the anti-microbial activity was studied by in vitro disc diffusion method. RESULTS: The extracts GPLE and GPRE significantly (P < 0.001) and dose dependently inhibited the acetic acid-induced writhing in mice with 73.15% and 53.69% inhibition, respectively at the dose of 200 mg/kg. At the same dose GPLE and GPRE significantly inhibited carrageenan-induced rats paw edema at the end of 4 hour with 35.54% and 28.17% inhibition, respectively. The extracts significantly prolonged the pentobarbitone-induced sleeping time and decreased the locomotory activities in open field and Hole cross tests in mice. The GPLE showed strong antimicrobial activity against Gram-positive and Gram-negative bacteria with zones of inhibition ranging from 8 to 20 mm at a concentration of 400 µg/disc. CONCLUSION: The findings of the study indicate that the leaves and roots of G. parviflorum possess antinociceptive, anti-inflammatory and CNS depressant activity and revealed the antimicrobial activities of leaves extract of the plant. The results justify the traditional use of the plant in the treatment of painful and inflammatory disorders.

A new C-benzylated chalcone from Desmos chinensis.

A new C-benzylated chalcone was isolated from the leaves of Desmos chinensis. Its structure was established as 2',4'-dihydroxy-3'-(2,6-dihydroxybenzyl)-6'-methoxychalcone on the basis of spectroscopic data.