The tubers and roots of Aconitum (Ranunculaceae) are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease, chronic heart failure, rheumatoid arthritis and neuropathic pain since ancient times. As a type of natural products mainly extracted from Aconitum plants, Aconitum alkaloids have complex chemical structures and exert remarkable biological activity, which are mainly responsible for significant effects of Aconitum plants. The present review is to summarize the progress of the pharmacological, toxicological, and pharmacokinetic studies of Aconitum alkaloids, so as to provide evidence for better clinical application. Research data concerning pharmacological, toxicological and pharmacokinetic studies of Aconitum alkaloids were collected from different scientific databases (PubMed, CNKI, Google Scholar, Baidu Scholar, and Web of Science) using the phrase Aconitum alkaloids, as well as generic synonyms. Aconitum alkaloids are both bioactive compounds and toxic ingredients in Aconitum plants. They produce a wide range of pharmacological activities, including protecting the cardiovascular system, nervous system, and immune system and anti-cancer effects. Notably, Aconitum alkaloids also exert strong cardiac toxicity, neurotoxicity and liver toxicity, which are supported by clinical studies. Finally, pharmacokinetic studies indicated that cytochrome P450 proteins (CYPs) and efflux transporters (ETs) are closely related to the low bioavailability of Aconitum alkaloids and play an important role in their metabolism and detoxification in vivo.
Aconitum/chemistry* ; Alkaloids/toxicity* ; Biological Availability ; Phytochemicals/toxicity* ; Plant Roots/chemistry*

Chimonanthus plants widely distributed in southern area of China, which have a long history of edibles and medicine. Phytochemical investigations have shown that Chimonanthus produced 143 non-volatile constituents, including alkaloids, flavonoids, terpenoids, coumarins and others, which exhibit significant anti-oxidant, anti-bacterial, anti-cancer, anti-inflammatory, antihyperglycemic, antihyperlipidemic and other biological activities. On the basis of systematic reviewing of literatures, this article overviews the non-volatile constituents and pharmacology of Chimonanthus from domestic and foreign over the last 30 years (until June 2018), and may provide a useful reference for the further development of Chimonanthus.
Animals ; Calycanthaceae ; chemistry ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Humans ; Medicine, Chinese Traditional ; Phytochemicals ; chemistry ; pharmacology ; therapeutic use ; toxicity ; Phytotherapy

OBJECTIVETo evaluate the anti-inflammatory and analgesic activities of leaf extract of Melanthera scandens (M. scandens).

METHODSThe crude leaf extract (39-111 mg/kg) of M. scandens was investigated for anti-inflammatory and analgesic activities using various experimental models. The anti-inflammatory activity was investigated using carragenin, egg-albumin induced oedema models, while acetic acid, formalin-induced paw licking and thermal-induced pain models were used to evaluate the antinociceptive property.

RESULTSThe extract caused a significant (P<0.05 - 0.001) dose-dependent reduction of inflammation and pains induced by different agents used.

CONCLUSIONSThe leaf extract possesses anti-inflammatory and analgesic effects which may be mediated through the phytochemical constituents of the plant.

Acetic Acid ; toxicity ; Albumins ; adverse effects ; Analgesics ; therapeutic use ; Animals ; Anti-Inflammatory Agents ; therapeutic use ; Asteraceae ; metabolism ; Carrageenan ; toxicity ; Edema ; drug therapy ; Formaldehyde ; toxicity ; Inflammation ; chemically induced ; drug therapy ; Mice ; Pain ; chemically induced ; drug therapy ; Phytochemicals ; therapeutic use ; Phytotherapy ; Plant Extracts ; therapeutic use ; Plant Leaves ; metabolism

OBJECTIVETo investigate the antioxidant, antibacterial and cytotoxic activity of whole Leucas aspera (Labiatae) (L. aspera) alcoholic extract.

METHODSWhole L. aspera powder was extracted by absolute ethanol (99.50%). The ethanolic extract was subjected to antioxidant, antibacterial and brine shrimp lethality assay.

RESULTSThe extract showed potent radical scavenging effect (antioxidant) with IC50 value of (99.58±1.22) µg/mL which was significant (P<0.01) in comparison to ascorbic acid with IC50 value of (1.25±0.95) µg/mL. In case of antibacterial screening, the extract showed notable antibacterial effect against the tested microbial strains. Significant (P<0.05) zone of inhibitions against Gram positive Bacillus subtilis [(12.00±1.32) mm] and Bacillus megaterium [(13.00±1.50) mm], Staphylococcus aureus [(8.00±0.50) mm] and Gram negative Salmonella typhi [(6.00±0.50) mm], Salmonella paratyphi [(8.00±1.00) mm], Shigella dysenteriae [(9.00±1.32) mm] and Vibrio cholerae [(9.00±0.66) mm] was observed. In brine shrimp lethality bioassay, the extract showed the LC50 value as (181.68±2.15) µg/mL which was statistically significant (P<0.01) compared to positive control vincristine sulfate [LC50=(0.76±0.04) µg/mL].

CONCLUSIONSThe results demonstrate that the ethanolic extract of L. aspera could be used as antibacterial, pesticidal and various pharmacologic actives.

Animals ; Anti-Bacterial Agents ; chemistry ; pharmacology ; Antioxidants ; chemistry ; pharmacology ; Artemia ; drug effects ; Biphenyl Compounds ; antagonists & inhibitors ; Dose-Response Relationship, Drug ; Inhibitory Concentration 50 ; Lamiaceae ; chemistry ; Microbial Sensitivity Tests ; Phytochemicals ; chemistry ; pharmacology ; Picrates ; antagonists & inhibitors ; Plant Extracts ; chemistry ; pharmacology ; Toxicity Tests

OBJECTIVETo explore the efficacy of ethanolic leaf extract of Typhonium trilobatum L. Schott in treating diarrhea, pain and inflammation using experimental models.

METHODSIn the present study, acetic acid-induced writhing, xylene-induced ear edema and castor oil-induced diarrheal model were used to evaluate the analgesic, anti-inflammatory and anti-diarrheal activities, respectively. Acute toxicity test was carried out to fix the safe doses of the plant extract.

RESULTSThe plant extract demonstrated a significant inhibition of writhing (P<0.01) compared with the control group in acetic acid-induced writhing test in mice. The extract also significantly inhibited the xylene induced ear edema formation (P<0.05). In anti-diarrheal test, the extract significantly decreased the frequency of defecation and increased the mean latent period (P<0.01) in castor oil-induced diarrheal model mice at the doses of 250 and 500 mg/kg body weight.

CONCLUSIONSThese results suggest that the extract possesses significant analgesic, anti-inflammatory and anti-diarrheal activities that support to the ethnopharmacological uses of this plant.

Analgesics ; chemistry ; pharmacology ; Animals ; Anti-Inflammatory Agents ; chemistry ; pharmacology ; Antidiarrheals ; chemistry ; pharmacology ; Diarrhea ; chemically induced ; drug therapy ; Disease Models, Animal ; Edema ; chemically induced ; drug therapy ; Female ; Magnoliopsida ; chemistry ; Male ; Mice ; Phytochemicals ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Plant Leaves ; chemistry ; Rats ; Toxicity Tests, Acute

OBJECTIVETo explore and identify the most potent antihyperglycemic fraction from the ethanol extract of Rhododendron arboreum (R. arboreum) flowers.

METHODSNormal and streptozotocin induced diabetic rats were treated with all four fractions of R. arboreum flowers for short term and with fraction 3 for long term study. On completion of the treatment, a range of indicators were tested including fasting blood glucose, plasma protein, haemoglobin A1C, insulin secretion, body weight, blood lipid profile and carbohydrate metabolism regulating enzymes of liver.

RESULTSIn short term study, the fraction 3 (Active fraction) produced a significant (P<0.000 1) reduction (73.6%) in blood glucose level at a dose of 200 mg/kg after the treatment in the diabetic rats. Administration of active fraction (200 and 400 mg/kg) once daily for 30 d in streptozotocin diabetic rats resulted in a significant (P<0.001 to P<0.000 1) fall in blood glucose level, hemoglobin A1C, serum urea and creatinine with significant but a increase in insulin level similar to standard drug glybenclamide. Further, the active fraction showed antihyperlipidemic activity as evidenced by significant (P<0.001 to P<0.000 1) decreases in serum serum total cholesterol, triglycerides, low density lipoprotein cholesterol and very low density cholesterol levels coupled together with elevation of high density lipoprotein cholesterol in the diabetic rats.

CONCLUSIONSThe active fraction of R. arboreum flowers decreases streptozotocin induced hyperglycemia by promoting insulin secretion and glycolysis and by decreasing gluconeogenesis.

Animals ; Blood Glucose ; drug effects ; Carbohydrate Metabolism ; drug effects ; Diabetes Mellitus, Experimental ; drug therapy ; metabolism ; Disease Models, Animal ; Flowers ; chemistry ; Hypoglycemic Agents ; chemistry ; pharmacology ; Hypolipidemic Agents ; chemistry ; pharmacology ; Lipids ; blood ; Male ; Phytochemicals ; chemistry ; Plant Extracts ; chemistry ; pharmacology ; Rats ; Rhododendron ; chemistry ; Toxicity Tests, Acute