Xanthones from the latex and twig extracts of Garcinia nigrolineata Planch. ex T. Anderson (Clusiaceae) and their antidiabetic and cytotoxic activities.

A new geranylated xanthone, nigrolineaxanthone AA (1) together with 18 known compounds (2-19) were isolated from latex and twig extracts of Garcinia nigrolineata Planch. ex T. Anderson. Some of the isolated compounds were assessed for their antidiabetic activities and cytotoxicity against three cancer cell lines. Of these, compounds 12 (IC50 value of 25.8 ± 0.2 µM), 16 (IC50 value of 124.8 ± 0.7 µM), and 17 (IC50 value of 44.4 ± 1.1 µM) exhibited the highest α-glucosidase inhibitory, α-amylase inhibitory, and glycation inhibition activities, respectively. Compound 11 showed glucose consumption and glucose uptake with IC50 values of 14.2 ± 0.8 µM and 3.1-fold. Compound 10 displayed cytotoxic activity against colon cancer (SW480) with an IC50 value of 4.3 ± 0.1 µM), while compound 2 showed cytotoxicity against leukemic cancer (K562) with IC50 value of 4.4 ± 0.3 µM.

α-Glucosidase inhibitory and α-amylase inhibitory activities of compounds isolated from Uvaria rufa Blume.

A new C-benzylated flavone, uvariaruflavone (1), along with 13 known compounds (2-14) were isolated from the twig and leaf extracts of Uvaria rufa Blume. Their structures were established by extensive spectroscopic methods. Flavones (5-8) and cyclohexene (10) were isolated from U. rufa for the first time. Most of the isolated compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Of these, uvariaruflavone (1) showed the highest α-glucosidase inhibitory activity with an IC50 value of 44.3 µM, while ferrudiol (12) displayed the highest α-amylase inhibitory activity with an IC50 value of 73.5 µM.

Metabolite profiling and evaluation of CYP450 interaction potential of 'Trimada'- an Ayurvedic formulation.

ETHNOPHARMACOLOGICAL RELEVANCE: Trimada is well-known polyherbal Ayurvedic formulation used in Indian Traditional medicine since ancient times. It consisted of three inebriant herbs including "Chitraka" (Plumbago zeylanica Linn. Family- Plumabaginaceae), "Musta" (Cyperus rotundus Linn. Family- Cyperaceae) and Vidanga (Embelia ribes Burm. F. Family- Myrsinaceae) in equal ratios as mentioned in Ayurveda. Trimada is traditionally used to increase the functioning of the digestive system and metabolism. Along with these, it also assists in the reduction of cholesterol as well as reduces stomach aches and chest pain. AIM OF THE STUDY: This study is aimed to identify the metabolites present in this polyherbal formulation. Further, the cytotoxicity and interaction potential of the formulation and individual herbs with Cytochrome P450 isozymes (CYP3A4, 2D6, 2C9, 1A2) was evaluated by MTT assay and CYP450 enzyme inhibition. The concentration of heavy metals was also determined. MATERIAL AND METHODS: Ultra-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UPLC-QTOF-MS) analysis was performed to detect and identify the phytoconstituents in the formulation. Cytotoxicity of the formulation was evaluated by MTT assay. CYP450 enzyme interaction potential of the individual herbs and the Trimada formulation was carried out through CYP-CO assay and fluorometric high throughput screening (HTS) assay for individual isozymes. The content of heavy metal in the formulation was quantified by Atomic Absorption Spectroscopy. RESULTS: Trimada formulation exhibited lower cytotoxicity to human liver carcinoma cell line (HepG2). CYP-CO assay revealed that the interaction potential of individual herbs and Trimada on the liver microsomes was found to be lesser than the standard inhibitor ketoconazole. Individual herbs and Trimada formulation displayed higher IC50 values than the respective standard inhibitors in the fluorimetric assay. UPLC-QTOF-MS analysis showed the presence of a number of active phytoconstituents including sesquiterpenes, phenolic acids, benzoquinones, triterpenes and flavonoids. The heavy metal concentration in the traditional medicinal herbal formulation was found within the approved limit. CONCLUSIONS: This study suggested that the individual herbs and Trimada formulation exhibited low cytotoxicity and contributes insignificant interaction with CYP450 isozymes. So, the formulation is considered to be safe for its therapeutic management without any potential drug interaction involving CYP 450 isozymes.

α-Glucosidase inhibitory and nitric oxide production inhibitory activities of alkaloids isolated from a twig extract of Polyalthia cinnamomea.

The first phytochemical investigation of Polyalthia cinnamomea led to the isolation and identification of two new oxoprotoberberine alkaloids, (-)-(13aS)-polyalthiacinnamines A and B, together with eleven known compounds. The structures of the new compounds were elucidated by extensive spectroscopic methods. The absolute configuration of miliusacunine E and consanguine B was established by X-ray diffraction analysis using Cu Kα radiation and ECD spectra, whereas the absolute configurations of polyalthiacinnamines A and B were established by comparison of their ECD spectra and specific rotations with those of miliusacunine E and consanguine B. Compounds 1-4, 6, and 8 exhibited α-glucosidase inhibitory activities (IC50 values ranging from 11.3 to 57.9 µM) better than a positive control (acarbose, IC50 83.5 µM). Compound 2 also exhibited NO production inhibitory activity with an IC50 value of 24.4 µM (indomethacin, a positive control, IC50 = 32.2 µM).

Pharmacognostic Specifications and Lawsone Content of Lawsonia inermis Leaves.

BACKGROUND: Lawsonia inermis L. has been used as a traditional or folk medicine for the treatment of a wide range of skin infectious diseases. OBJECTIVE: The objective of this study was to determine the pharmacognostic specifications and lawsone contents of L. inermis leaves. MATERIALS AND METHODS: The pharmacognostic specifications of L. inermis leaves from 12 sources were evaluated according to the WHO guideline of quality control method for medicinal plant materials. The lawsone contents were analyzed by thin-layer chromatography (TLC) coupled with densitometry and image analysis. RESULTS: Microscopic evaluation of L. inermis powders showed the fragment of mesophyll, fragment of parenchyma, epidermis layer with stomata, and the rosette crystal of calcium oxalate. Physicochemical parameters revealed that total ash, acid-insoluble ash, loss on drying, and water content should be not <6.98, 1.12, 8.08, and 9.86% of dried weight, respectively, whereas ethanol and water extractive values should be not < 19.67 and 23.06% of dried weight, respectively. The content of lawsone in L. inermis leaves by TLC-densitometry was found to be 0.76 ± 0.05 g/100 g of dried crude drug, whereas the lawsone content evaluation by TLC image analysis was found to be 0.87 ± 0.11 g/100 g of dried crude drug. The validation of the methods revealed that both TLC-densitometry and TLC image analysis showed a good sensitivity and accuracy for lawsone quantitation in L. inermis. CONCLUSION: The pharmacognostic specifications could be used as the standardization data of L. inermis leaves, and the development of TLC method could be applied to determine lawsone content in this plant material. SUMMARY: The pharmacognostic specification of Lawsonia inermis leaves could be used as the standardization data of L. inermis leaves in Thailand.Both TLC-densitometry and TLC image analysis showed a good sensitivity and accuracy for lawsone quantitation. Abbreviations Used: LOD: Limit of detection; LOQ: Limit of quantitation; RSD: Relative standard deviation; TLC: Thin layer chromatography; UV: Ultraviolet; Rf value: Relative to front value.

Pharmacognostic specification of Zanthoxylum limonella (Dennst.) Alston: Fruits and seeds in Thailand.

Zanthoxylum limonella (Dennst.) Alston. (Rutaceae) or Ma-khwaen is one of the medicinal plants in Thai traditional medicine. To investigate the pharmacognostic specifications and chemical constituents of Z. limonella fruits and seeds. Fruits and seeds of Z. limonella were collected from 15 sources throughout Thailand; then examined the pharmacognostic specification following WHO guideline of quality control method for medicinal plant materials. Microscopic determination of Z. limonella powders demonstrated fragment of mesocarp, fragment of brown vitta, oil glands, fragment of endocarp, and endosperm containing oil globule, trichome and pale brown stone cells. Stomatal index and pellucid dots in mm2 were 19.87 and 4.2 respectively. Physico-chemical parameters unveiled that loss on drying, water content, total ash, and acid-insoluble ash should be not >17.90%, 9.18%, 4.50%, and 0.60% of dried weight respectively; while ethanol, water, and hexane extractive values and volatile oil content should be not <2.24%, 2.27%, 1.57% and 9.63% of dried weight respectively. Rf values of thin-layer chromatographic fingerprint of Z. limonella fruits and seeds ethanolic extract were 0.38, 0.45, 0.90, and 0.97 detected ultraviolet (UV) light 254 nm, 0.30, 0.44, 0.67, and 0.77 detected UV light 366 nm, and 0.24, 0.73, 0.78, and 0.93 detected 10% sulfuric acid. There are three main chemical compounds in Z. limonella oil including limonene (43.63%), (+)-sabinene (16.72%), and terpinen-4-ol (10.95%). The result gained from pharmacognostic specifications and chemical fingerprints could be used as standardization data of Z. limonella fruits and seeds to apply or provide for guarantee of quality.

Pharmacognostic evaluation with reference to catechin content and antioxidant activities of pale catechu in Thailand.

Pale catechu, a well-known crude drug, has been widely used for anti-diarrhea. Due to its medicinal usage, this study was performed to evaluate the pharmacognostic and antioxidant properties as well as catechins contents of pale catechu in Thailand. Twenty samples of pale catechu collected from traditional drug stores throughout Thailand were investigated. Antioxidant activities, total phenolic, nontannin phenolic, and total tannin contents were evaluated. (+)-catechin and (-)-epicatechin were quantitatively analyzed by high performance liquid chromatography. The results revealed that most of pale catechu samples were adulterated according to high ash values. Qualified pale catechu in Thailand were demonstrated for their average contents of total ash, acid insoluble ash, loss on drying, and moisture as 5.20 ± 0.19, 1.61 ± 0.17, 13.14 ± 0.10, and 13.20 ± 1.07 g/100 g of dry weight, respectively. The ethanol and water soluble extractive matters were 91.66 ± 5.16 and 44.59 ± 3.18 g/100 g of dry weight respectively. (+)-catechin in theses samples was 478.87 ± 2.77 µg/mg of crude drug, whereas (-)-epicatechin was found to be trace (

Pharmacognostic specifications and quantification of (+)-catechin and (-)-epicatechin in Pentace burmanica stem bark.

BACKGROUND: According to Thai traditional medicine, Pentace burmanica Kurz. stem bark has been used as crude drug for treating diarrhea. However, the crude drug is also found susceptible to adulteration. OBJECTIVES: To develop specific standardization parameters of P. burmanica stem bark in Thailand and to determine the (+)-catechin and (-)-epicatechin contents of P. burmanica stem bark by HPLC analysis. MATERIALS AND METHODS: P. burmanica stem barks from various sources throughout Thailand were investigated according to WHO guideline of the pharmacognostic specification. High performance liquid chromatography (HPLC) was performed for (+)-catechin and (-)-epicatechin quantification. RESULTS: Macroscopic evaluation was demonstrated as whole plant drawing. Microscopic evaluation of stem bark powdered drug showed fragment of fibers, resin masses, tannin masses, starch grain, calcium oxalate, and fragment of parenchyma. Physico-chemical parameters revealed that total ash, acid insoluble ash, loss on drying, and water content should be not more than 3.58, 0.50, 8.40, and 9.70% of dry weight respectively; while ethanol and water soluble extractive values should not be less than 21.90 and 19.06% of dry weight respectively. Both (+)-catechin and (-)-epicatechin were existed in P. burmanica ethanolic extract. Owing to the small amount of (+)-catechin, quantitation of its content was omitted. However, (-)-epicatechin contents was found as 59.74 ± 1.69µg/mg of crude extract. CONCLUSION: The pharmacognostic investigations can be used to set the standard parameters of P. burmanica stem bark in Thailand. HPLC method can be applied to determine (+)-catechin and (-)-epicatechin content in plant materials.